PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 15565299-17 2005 CYP2D6 polymorphisms did not predict clinical response, but predicted a tendential increase in the plasma risperidone to 9-OH-risperidone ratio (0.5 +/- 0.6 vs. 1.9 +/- 1.8; p = 0.120). Paliperidone Palmitate 121-137 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 16321618-2 2005 The aim of this study was to evaluate the effect of itraconazole, a CYP3A inhibitor, on the plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients in relation to CYP2D6 genotype. Paliperidone Palmitate 133-153 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-73 16321618-2 2005 The aim of this study was to evaluate the effect of itraconazole, a CYP3A inhibitor, on the plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients in relation to CYP2D6 genotype. Paliperidone Palmitate 133-153 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 195-201 16321618-8 2005 In addition, the active moiety (risperidone plus 9-hydroxyrisperidone) also increased similarly, by 71% (P < .001) and 73% (P < .05), respectively, with itraconazole, without a significant difference between CYP2D6 genotypes. Paliperidone Palmitate 49-69 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 214-220 16321618-10 2005 CONCLUSIONS: Our results provide in vivo evidence of the involvement of CYP3A in the disposition of risperidone and 9-hydroxyrisperidone. Paliperidone Palmitate 116-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-77 16118767-0 2005 P-glycoprotein interaction with risperidone and 9-OH-risperidone studied in vitro, in knock-out mice and in drug-drug interaction experiments. Paliperidone Palmitate 48-64 phosphoglycolate phosphatase Mus musculus 0-14 16118767-3 2005 Here we compared the in vitro P-gp interactions of Risp and its major metabolite, 9-OH-Risperidone (OH-Risp), with their distribution over the BBB in P-gp knock-out mice and in rats where P-gp was inhibited. Paliperidone Palmitate 82-98 phosphoglycolate phosphatase Mus musculus 30-34 15565299-19 2005 The observed CYP2D6 polymorphisms did not contribute to altered clinical efficacy, but affected risperidone to 9-OH-risperidone ratios. Paliperidone Palmitate 111-127 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 13-19 15260906-10 2004 The number of CYP2D6 active genes was related to the dose-corrected plasma concentration of risperidone (p < 0.05), the active moiety (risperidone plus 9-OH-risperidone) (p < 0.05) and the risperidone/9-OH-risperidone ratio (p < 0.05). Paliperidone Palmitate 155-171 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 14-20 15767244-3 2005 In humans, risperidone is metabolized by cytochrome P450 2D6 to 9-hydroxyrisperidone; together these constitute the active moiety. Paliperidone Palmitate 64-84 cytochrome P450 2D6 Homo sapiens 41-60 15270204-3 2004 Risperidone in humans is mainly metabolized to 9-hydroxyrisperidone by the polymorphic cytochrome enzyme P450 2D6 (CYP2D6). Paliperidone Palmitate 47-67 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 115-121 15270204-4 2004 Plasma concentrations of risperidone and 9-hydroxyrisperidone show large interindividual variability, which may be partly related to the activity of the CYP2D6 enzyme. Paliperidone Palmitate 41-61 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 153-159 15270204-8 2004 Since risperidone/9-hydroxyrisperidone ratio strongly correlates with CYP2D6 enzyme activity and the number of CYP2D6 active genes, thus it might be a useful tool in clinical practice to estimate the possible risk of drug interactions due to impaired CYP2D6 enzyme activity. Paliperidone Palmitate 18-38 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 70-76 15270204-8 2004 Since risperidone/9-hydroxyrisperidone ratio strongly correlates with CYP2D6 enzyme activity and the number of CYP2D6 active genes, thus it might be a useful tool in clinical practice to estimate the possible risk of drug interactions due to impaired CYP2D6 enzyme activity. Paliperidone Palmitate 18-38 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 111-117 15270204-8 2004 Since risperidone/9-hydroxyrisperidone ratio strongly correlates with CYP2D6 enzyme activity and the number of CYP2D6 active genes, thus it might be a useful tool in clinical practice to estimate the possible risk of drug interactions due to impaired CYP2D6 enzyme activity. Paliperidone Palmitate 18-38 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 111-117 15683552-0 2004 The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein. Paliperidone Palmitate 35-55 phosphoglycolate phosphatase Mus musculus 78-92 15683552-5 2004 These results indicate that P-gp in the blood-brain barrier significantly influences the brain concentrations of risperidone and 9-OH-risperidone by limiting their CNS access. Paliperidone Palmitate 129-145 phosphoglycolate phosphatase Mus musculus 28-32 15260906-10 2004 The number of CYP2D6 active genes was related to the dose-corrected plasma concentration of risperidone (p < 0.05), the active moiety (risperidone plus 9-OH-risperidone) (p < 0.05) and the risperidone/9-OH-risperidone ratio (p < 0.05). Paliperidone Palmitate 207-223 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 14-20 15089809-8 2004 Multiple regression analyses including CYP2D6 genotypes, sex, and age revealed that steady-state plasma concentration of risperidone correlated with the number of mutated alleles for CYP2D6 (standardized partial correlation coefficients (beta) = 0.540, P < 0.001) and those of 9-hydroxyrisperidone (standardized beta = 0.244, P = 0.038) and active moiety (standardized beta = 0.257, P = 0.027) correlated with age. Paliperidone Palmitate 280-300 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 183-189 12616663-0 2003 Effects of CYP2D6 genotypes on plasma concentrations of risperidone and enantiomers of 9-hydroxyrisperidone in Japanese patients with schizophrenia. Paliperidone Palmitate 87-107 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 11-17 12616663-8 2003 The concentration ratio of risperidone to 9-hydroxyrisperidone was strongly dependent on the CYP2D6 genotypes. Paliperidone Palmitate 42-62 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 93-99 12616663-9 2003 This study suggests that CYP2D6 activity strongly influences the steady-state plasma concentrations of risperidone and risperidone/9-hydroxyrisperidone concentration ratios but is unlikely to determine enantio-selectivity in the steady-state plasma concentrations of 9-hydroxyrisperidone in the clinical situation. Paliperidone Palmitate 131-151 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 25-31 12616663-9 2003 This study suggests that CYP2D6 activity strongly influences the steady-state plasma concentrations of risperidone and risperidone/9-hydroxyrisperidone concentration ratios but is unlikely to determine enantio-selectivity in the steady-state plasma concentrations of 9-hydroxyrisperidone in the clinical situation. Paliperidone Palmitate 267-287 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 25-31 12518271-9 2002 According to the present data, the evaluation of the risperidone/9-hydroxy-risperidone ratio may reflect the actual enzyme activity of CYP2D6. Paliperidone Palmitate 65-86 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 135-141 10771452-5 2000 IC50 values for the inhibition of specific probe substrates for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, by ziprasidone, risperidone and 9-hydroxyrisperidone were also determined using human liver microsomes from three subjects. Paliperidone Palmitate 140-160 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 64-70 11791898-1 2001 OBJECTIVE: Risperidone is known to be biotransformed to its active metabolite, 9-hydroxyrisperidone, by the polymorphic CYP2D6 in Caucasians. Paliperidone Palmitate 79-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 120-126 11791898-2 2001 This study aimed to investigate the relationship between the CYP2D6*10 allele and the plasma levels of risperidone and 9-hydroxyrisperidone in Korean schizophrenic patients. Paliperidone Palmitate 119-139 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 61-67 12107617-6 2002 The changes in risperidone concentrations were positively correlated to the concentration ratios of risperidone/9-hydroxyrisperidone (r(s)=0.90, P<0.01), which were closely associated with CYP2D6 genotypes. Paliperidone Palmitate 112-132 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 192-198 11560868-1 2001 The antipsychotic agent risperidone, is metabolized by different cytochrome P-450 (CYP) enzymes, including CYP2D6, to the active 9-hydroxyrisperidone, which is the major metabolite in plasma. Paliperidone Palmitate 129-149 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 65-81 11560868-1 2001 The antipsychotic agent risperidone, is metabolized by different cytochrome P-450 (CYP) enzymes, including CYP2D6, to the active 9-hydroxyrisperidone, which is the major metabolite in plasma. Paliperidone Palmitate 129-149 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 83-86 11560868-1 2001 The antipsychotic agent risperidone, is metabolized by different cytochrome P-450 (CYP) enzymes, including CYP2D6, to the active 9-hydroxyrisperidone, which is the major metabolite in plasma. Paliperidone Palmitate 129-149 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 107-113 11560868-2 2001 Two enantiomers, (+)- and (-)-9-hydroxyrisperidone might be formed, and the aim of this study was to evaluate the importance of CYP2D6 and CYP3A4/CYP3A5 in the formation of these two enantiomers in human liver microsomes and in recombinantly expressed enzymes. Paliperidone Palmitate 26-50 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 128-134 11560868-2 2001 Two enantiomers, (+)- and (-)-9-hydroxyrisperidone might be formed, and the aim of this study was to evaluate the importance of CYP2D6 and CYP3A4/CYP3A5 in the formation of these two enantiomers in human liver microsomes and in recombinantly expressed enzymes. Paliperidone Palmitate 26-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 11560868-2 2001 Two enantiomers, (+)- and (-)-9-hydroxyrisperidone might be formed, and the aim of this study was to evaluate the importance of CYP2D6 and CYP3A4/CYP3A5 in the formation of these two enantiomers in human liver microsomes and in recombinantly expressed enzymes. Paliperidone Palmitate 26-50 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 146-152 11560868-5 2001 The formation of (+)-9-hydroxyrisperidone was strongly inhibited by quinidine, a potent CYP2D6 inhibitor, whereas ketoconazole, a CYP3A4 inhibitor, strongly inhibited the formation of (-)-9-hydroxyrisperidone. Paliperidone Palmitate 17-41 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 88-94 11560868-5 2001 The formation of (+)-9-hydroxyrisperidone was strongly inhibited by quinidine, a potent CYP2D6 inhibitor, whereas ketoconazole, a CYP3A4 inhibitor, strongly inhibited the formation of (-)-9-hydroxyrisperidone. Paliperidone Palmitate 184-208 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 130-136 11560868-6 2001 Recombinant human CYP2D6 produced only (+)-9-hydroxyrisperidone, whereas a lower formation rate of both enantiomers was detected with expressed CYP3A4 and CYP3A5. Paliperidone Palmitate 39-63 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 18-24 11360029-8 2001 The authors" findings indicate that paroxetine, a potent inhibitor of CYP2D6, may impair the elimination of risperidone, primarily by inhibiting CYP2D6-mediated 9-hydroxylation and to a lesser extent by simultaneously affecting the further metabolism of 9-OH-risperidone or other pathways of risperidone biotransformation. Paliperidone Palmitate 254-270 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 70-76 10771452-5 2000 IC50 values for the inhibition of specific probe substrates for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, by ziprasidone, risperidone and 9-hydroxyrisperidone were also determined using human liver microsomes from three subjects. Paliperidone Palmitate 140-160 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 72-78 10771452-5 2000 IC50 values for the inhibition of specific probe substrates for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, by ziprasidone, risperidone and 9-hydroxyrisperidone were also determined using human liver microsomes from three subjects. Paliperidone Palmitate 140-160 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 80-87 10771452-5 2000 IC50 values for the inhibition of specific probe substrates for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, by ziprasidone, risperidone and 9-hydroxyrisperidone were also determined using human liver microsomes from three subjects. Paliperidone Palmitate 140-160 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 89-95 10771452-5 2000 IC50 values for the inhibition of specific probe substrates for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, by ziprasidone, risperidone and 9-hydroxyrisperidone were also determined using human liver microsomes from three subjects. Paliperidone Palmitate 140-160 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 10771452-11 2000 Similar in vitro inhibition of CYP2D6 (Ki 6.9-16 microM) and CYP3A4 (Ki 64-80 microM) was obtained with ziprasidone, risperidone and 9-hydroxyrisperidone. Paliperidone Palmitate 133-153 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 31-37 10771452-11 2000 Similar in vitro inhibition of CYP2D6 (Ki 6.9-16 microM) and CYP3A4 (Ki 64-80 microM) was obtained with ziprasidone, risperidone and 9-hydroxyrisperidone. Paliperidone Palmitate 133-153 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-67 10453802-2 1999 The ratio between risperidone and 9-hydroxyrisperidone characterizes cytochrome P450 2D6 (CYP2D6) status. Paliperidone Palmitate 34-54 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 69-88 10639689-0 1999 Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Paliperidone Palmitate 79-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-19 10639689-1 1999 The role of the polymorphic cytochrome P450 2D6 (CYP2D6) in the metabolism of risperidone to its major active metabolite, 9-hydroxyrisperidone (9-OH-risperidone), has been documented after single oral doses of the drug. Paliperidone Palmitate 122-142 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 28-47 10639689-1 1999 The role of the polymorphic cytochrome P450 2D6 (CYP2D6) in the metabolism of risperidone to its major active metabolite, 9-hydroxyrisperidone (9-OH-risperidone), has been documented after single oral doses of the drug. Paliperidone Palmitate 122-142 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 10639689-1 1999 The role of the polymorphic cytochrome P450 2D6 (CYP2D6) in the metabolism of risperidone to its major active metabolite, 9-hydroxyrisperidone (9-OH-risperidone), has been documented after single oral doses of the drug. Paliperidone Palmitate 144-160 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 28-47 10639689-1 1999 The role of the polymorphic cytochrome P450 2D6 (CYP2D6) in the metabolism of risperidone to its major active metabolite, 9-hydroxyrisperidone (9-OH-risperidone), has been documented after single oral doses of the drug. Paliperidone Palmitate 144-160 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 10639689-2 1999 In this study, the influence of the CYP2D6 polymorphism on the steady-state plasma concentrations of risperidone and 9-OH-risperidone was investigated. Paliperidone Palmitate 117-133 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 36-42 10639689-8 1999 The risperidone/9-OH-risperidone ratio was strongly associated with the CYP2D6 genotype, with the highest ratios in PM (median 0.79). Paliperidone Palmitate 16-32 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 72-78 10639689-11 1999 In conclusion, the steady-state plasma concentrations of risperidone and the risperidone/9-OH-risperidone ratio are highly dependent on the CYP2D6 genotype. Paliperidone Palmitate 89-105 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 140-146 10453802-2 1999 The ratio between risperidone and 9-hydroxyrisperidone characterizes cytochrome P450 2D6 (CYP2D6) status. Paliperidone Palmitate 34-54 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 90-96 7545821-1 1995 The hydroxylation of the new antipsychotic drug risperidone to its main, active metabolite 9-hydroxyrisperidone is catalyzed by the hepatic cytochrome P450 enzyme CYP2D6, and cosegregates with the polymorphic hydroxylation of debrisoquin. Paliperidone Palmitate 91-111 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 163-169 10048600-5 1999 Of these enzymes, CYPs 2D6, 3A4 and 3A5 were found to be the ones capable of metabolising risperidone to 9-hydroxyrisperidone, with activities of 7.5, 0.4 and 0.2 pmol pmol(-1) CYP min(-1), respectively. Paliperidone Palmitate 105-125 cytochrome P450, family 3, subfamily a, polypeptide 23-polypeptide 1 Rattus norvegicus 18-21 10048600-6 1999 A correlation study using a panel of human liver microsomes showed that the formation of 9-hydroxyrisperidone is highly correlated with CYP2D6 and 3A activities. Paliperidone Palmitate 89-109 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 136-142 10048600-8 1999 This observation is confirmed by the findings that both quinidine (inhibitor of CYP2D6) and ketoconazole (inhibitor of CYP3A4) can inhibit the formation of 9-hydroxyrisperidone. Paliperidone Palmitate 156-176 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 80-86 10048600-8 1999 This observation is confirmed by the findings that both quinidine (inhibitor of CYP2D6) and ketoconazole (inhibitor of CYP3A4) can inhibit the formation of 9-hydroxyrisperidone. Paliperidone Palmitate 156-176 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 119-125 10048600-9 1999 Furthermore, inducers of CYP can significantly increase the formation of 9-hydroxyrisperidone in rat. Paliperidone Palmitate 73-93 cytochrome P450, family 3, subfamily a, polypeptide 23-polypeptide 1 Rattus norvegicus 25-28 10048600-10 1999 The formation of 9-hydroxyrisperidone is highly correlated with testosterone 6beta-hydroxylase activities, suggesting that inducible CYP3A contributes significantly to the metabolism of risperidone in rat. Paliperidone Palmitate 17-37 cytochrome P450, family 3, subfamily a, polypeptide 2 Rattus norvegicus 64-94 10048600-10 1999 The formation of 9-hydroxyrisperidone is highly correlated with testosterone 6beta-hydroxylase activities, suggesting that inducible CYP3A contributes significantly to the metabolism of risperidone in rat. Paliperidone Palmitate 17-37 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 133-138 8935801-8 1996 Subnanomolar affinity for human 5HT2A receptors was observed for ORG-5222, sertindole, risperidone, 9-OH-risperidone and ziprasidone. Paliperidone Palmitate 100-116 5-hydroxytryptamine receptor 2A Homo sapiens 32-37 8935801-16 1996 In vivo, ORG-5222, risperidone, pipamperone, 9-OH-risperidone, sertindole, olanzapine, zotepine and clozapine maintained a higher potency for occupying 5HT2A than D2 receptors. Paliperidone Palmitate 45-61 5-hydroxytryptamine receptor 2A Homo sapiens 152-157 7512019-8 1994 The resulting 9-hydroxy-risperidone (9-OH-RIS) was the main metabolite in the excreta of dogs. Paliperidone Palmitate 14-35 RAS like family 12 Homo sapiens 42-45 7520908-2 1994 In vitro, risperidone and 9-hydroxyrisperidone had similar binding profiles, and their highest affinity was for 5-HT2A receptors (cloned human, Ki 0.4 nM); affinities for other 5-HT-receptor subtypes were at least 100 times lower. Paliperidone Palmitate 26-46 5-hydroxytryptamine receptor 2A Homo sapiens 114-118 34081288-12 2021 Clozapine and paliperidone were associated with hepatic steatosis (CAP + 23.3 db/m, p 0.013 and CAP + 25.5, p 0.037, respectively). Paliperidone Palmitate 14-26 brain abundant membrane attached signal protein 1 Homo sapiens 67-75 34787912-0 2022 Prospective analysis of serum prolactin levels, clinical symptomatology and sexual functions in patients with schizophrenia switched to paliperidone palmitate 3-monthly from paliperidone palmitate 1-monthly: Preliminary findings of the first 3 months. Paliperidone Palmitate 136-158 prolactin Homo sapiens 30-39 34787912-0 2022 Prospective analysis of serum prolactin levels, clinical symptomatology and sexual functions in patients with schizophrenia switched to paliperidone palmitate 3-monthly from paliperidone palmitate 1-monthly: Preliminary findings of the first 3 months. Paliperidone Palmitate 174-196 prolactin Homo sapiens 30-39 34481200-9 2021 Newer antipsychotics (risperidone, amisulpride and paliperidone) and older antipsychotics (chlorpromazine, haloperidol and sulpride) increase prolactin levels with large effect sizes. Paliperidone Palmitate 51-63 prolactin Homo sapiens 142-151 7690693-2 1993 The formation of the equipotent major metabolite, 9-hydroxyrisperidone, exhibited CYP2D6-related polymorphism. Paliperidone Palmitate 50-70 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 82-88 34690776-6 2021 As the dose-corrected plasma levels of risperidone, 9-OH-risperidone, and the active moiety increased, prolactin levels in patients carrying the H1/H3 diplotype were significantly higher than those of the other diplotypes. Paliperidone Palmitate 52-68 prolactin Homo sapiens 103-112 34189861-6 2021 We compared the prolactin and testosterone levels in patients receiving risperidone or paliperidone and patients receiving aripiprazole. Paliperidone Palmitate 87-99 prolactin Homo sapiens 16-25 34189861-12 2021 Testosterone concentrations were associated with elevated prolactin levels in patients receiving risperidone or paliperidone. Paliperidone Palmitate 112-124 prolactin Homo sapiens 58-67 34503167-0 2021 Paliperidone Inhibits Glioblastoma Growth in Mouse Brain Tumor Model and Reduces PD-L1 Expression. Paliperidone Palmitate 0-12 CD274 antigen Mus musculus 81-86 34503167-2 2021 The present study showed that prescribed psychotropic medicine paliperidone reduced GBM growth and immune checkpoint protein programmed death ligand (PD-L)1 expression and increased survival in an intracranial xenograft mouse model. Paliperidone Palmitate 63-75 CD274 antigen Mus musculus 150-156 34503167-5 2021 The enhancement of PD-L1 in GBM was antagonized by paliperidone and risperidone as well as DRD2 selective inhibitor L741426. Paliperidone Palmitate 51-63 CD274 molecule Homo sapiens 19-24 34503167-7 2021 Importantly, treatment with paliperidone effectively decreased CD206 and also dramatically increased CD80 (M1 phenotype marker) in BMDMs. Paliperidone Palmitate 28-40 mannose receptor, C type 1 Mus musculus 63-68 34503167-7 2021 Importantly, treatment with paliperidone effectively decreased CD206 and also dramatically increased CD80 (M1 phenotype marker) in BMDMs. Paliperidone Palmitate 28-40 CD80 antigen Mus musculus 101-105 34503167-12 2021 Our results provide a valuable therapeutic strategy and indicate that treatments combining DRD2 antagonist paliperidone with standard immunotherapy may be beneficial for GBM treatment. Paliperidone Palmitate 107-119 dopamine receptor D2 Mus musculus 91-95 35224877-12 2022 Risperidone (9 nM) and paliperidone (14 nM) have the highest alpha2C-adrenoceptor affinity however this is only 5-fold selective over alpha2A, and both have a higher affinity for alpha1A (2 nM and 4 nM, respectively). Paliperidone Palmitate 23-35 adrenoceptor alpha 2C Homo sapiens 61-81 35224877-12 2022 Risperidone (9 nM) and paliperidone (14 nM) have the highest alpha2C-adrenoceptor affinity however this is only 5-fold selective over alpha2A, and both have a higher affinity for alpha1A (2 nM and 4 nM, respectively). Paliperidone Palmitate 23-35 serpin family A member 1 Homo sapiens 179-186 34054556-9 2021 Long-term paliperidone was able to counteract MIA-induced changes in 5-HT and KMO, and to increase tryptophan availability and tryptophan hydroxylase-2 expression in poly (I:C) mice but not in controls. Paliperidone Palmitate 10-22 kynurenine 3-monooxygenase (kynurenine 3-hydroxylase) Mus musculus 78-81 35266856-7 2022 Out of 1576, FDA-approved compounds, our study suggests three compounds: netupitant, paliperidone and vilazodone as possible inhibitors with a potential to inhibit both sites (monomeric and dimeric) of the Mpro. Paliperidone Palmitate 85-97 NEWENTRY Severe acute respiratory syndrome-related coronavirus 206-210 33400943-6 2021 RESULTS: The risperidone Cmax,ss, Cmin,ss, AUC0-tau,ss, and the ratio of risperidone to 9-hydroxyrisperidone (9-OH-R) in CYP2D6 intermediate metabolizers (IMs) were significantly different compared with those in normal metabolizers (NMs) in both the LY03004 and Risperdal Consta groups (P < 0.05). Paliperidone Palmitate 88-108 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 121-127 34054556-9 2021 Long-term paliperidone was able to counteract MIA-induced changes in 5-HT and KMO, and to increase tryptophan availability and tryptophan hydroxylase-2 expression in poly (I:C) mice but not in controls. Paliperidone Palmitate 10-22 tryptophan hydroxylase 2 Mus musculus 127-151 32971359-7 2020 Additionally, scores on CPAD depth perception (number of correct responses), divided attention, digit span test, and trail-making test B subtests were significantly better for the aripiprazole and paliperidone groups than for the haloperidol and risperidone groups. Paliperidone Palmitate 197-209 TNF superfamily member 10 Homo sapiens 117-122 33549979-0 2021 Factors influencing the effect of aripiprazole on prolactin levels in patients treated with risperidone or paliperidone. Paliperidone Palmitate 107-119 prolactin Homo sapiens 50-59 32682874-4 2021 CYP2D6 normal/ultrarapid metabolizers (NM/UM) (vs. other) had lower risperidone (29%) and active moiety levels (24%) (9-OH-risperidone not affected). Paliperidone Palmitate 118-134 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 33312997-5 2020 LEARNING POINTS: Paliperidone and mirtazapine are associated with first-degree heart block, which may be a harbinger of torsades de pointes and ventricular fibrillation.Paliperidone and mirtazapine may potentiate each other"s proarrhythmic effects since the metabolism of both involve the cytochrome P450 2D6 enzyme.A history of psychiatric illness makes it difficult to rule out atypical chest pain without ECG or troponins and often leads to increased resource utilization, even during times of heavy use like the COVID-19 pandemic. Paliperidone Palmitate 17-29 cytochrome P450 2D6 Homo sapiens 289-308 32519344-1 2020 BACKGROUND: Risperidone is a second-generation antipsychotic drug metabolized to an active metabolite, 9-hydroxyrisperidone, primarily by cytochrome P4502D6 (CYP2D6) and to a lesser extent by CYP3A4. Paliperidone Palmitate 103-123 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 138-156 32198935-4 2020 Genetic variants of P-glycoprotein with changed functional activity might influence the potential of risperidone and paliperidone to cause hyperprolactinemia as the altered blood/brain concentration ratio would lead to a reduced therapeutic drug level within essential brain areas making dose adaptations necessary. Paliperidone Palmitate 117-129 ATP binding cassette subfamily B member 1 Homo sapiens 20-34 32198935-13 2020 CONCLUSION: This study revealed a significant association between the ABCB1 gene polymorphism rs2032582 (G2677T) and risperidone/paliperidone-induced hyperprolactinemia. Paliperidone Palmitate 129-141 ATP binding cassette subfamily B member 1 Homo sapiens 70-75 32657631-7 2021 When patients were subdivided into those who were treated with risperidone, haloperidol, paliperidone, amisulpride, and a group that was not treated with these antipsychotics, aggressive patients in both groups had significantly higher PRL concentrations than non-aggressive patients. Paliperidone Palmitate 89-101 prolactin Homo sapiens 236-239 32519344-1 2020 BACKGROUND: Risperidone is a second-generation antipsychotic drug metabolized to an active metabolite, 9-hydroxyrisperidone, primarily by cytochrome P4502D6 (CYP2D6) and to a lesser extent by CYP3A4. Paliperidone Palmitate 103-123 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 158-164 32519344-1 2020 BACKGROUND: Risperidone is a second-generation antipsychotic drug metabolized to an active metabolite, 9-hydroxyrisperidone, primarily by cytochrome P4502D6 (CYP2D6) and to a lesser extent by CYP3A4. Paliperidone Palmitate 103-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 192-198 32519344-11 2020 CONCLUSION: Genetically defined impaired CYP2D6 activity is associated with increased exposure of both risperidone and risperidone+9-hydroxyrisperidone in adults receiving oral formulations. Paliperidone Palmitate 131-151 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 41-47 32476097-0 2020 Modelling Age-Related Changes in the Pharmacokinetics of Risperidone and 9-Hydroxyrisperidone in Different CYP2D6 Phenotypes Using a Physiologically Based Pharmacokinetic Approach. Paliperidone Palmitate 73-93 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 107-113 32476097-2 2020 Based on the genetic polymorphism of cytochrome P 450 (CYP) 2D6 genetically and age-related changes cause differences in the pharmacokinetics of risperidone and 9-hydroxyrisperidone. Paliperidone Palmitate 161-181 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 37-63 32446424-5 2020 Case 2 was also very sensitive to CYP3A4 inducers as indicated by very low C/D ratios for carbamazepine, risperidone and paliperidone. Paliperidone Palmitate 121-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 31359271-0 2020 Physiologically Based Pharmacokinetic Modelling to Describe the Pharmacokinetics of Risperidone and 9-Hydroxyrisperidone According to Cytochrome P450 2D6 Phenotypes. Paliperidone Palmitate 100-120 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 134-153 31359271-3 2020 The goal of this study was to develop a physiologically based pharmacokinetic (PBPK) model considering the CYP2D6 genetic polymorphism for risperidone and 9-hydroxyrisperidone (9-OH-RIS) taking CYP3A4 into account. Paliperidone Palmitate 155-175 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 107-113 31359271-3 2020 The goal of this study was to develop a physiologically based pharmacokinetic (PBPK) model considering the CYP2D6 genetic polymorphism for risperidone and 9-hydroxyrisperidone (9-OH-RIS) taking CYP3A4 into account. Paliperidone Palmitate 155-175 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 194-200 31480671-5 2019 Among the top 10 most probable inhibitors of TRPA1 with good blood brain barrier (BBB) permeability, desvenlafaxine, paliperidone, and febuxostat emerged as the most promising repurposable agents for treating MS. Molecular docking studies indicated that desvenlafaxine, paliperidone, and febuxostat are likely to induce allosteric TRPA1 channel inhibition. Paliperidone Palmitate 117-129 transient receptor potential cation channel subfamily A member 1 Homo sapiens 45-50 31480671-5 2019 Among the top 10 most probable inhibitors of TRPA1 with good blood brain barrier (BBB) permeability, desvenlafaxine, paliperidone, and febuxostat emerged as the most promising repurposable agents for treating MS. Molecular docking studies indicated that desvenlafaxine, paliperidone, and febuxostat are likely to induce allosteric TRPA1 channel inhibition. Paliperidone Palmitate 270-282 transient receptor potential cation channel subfamily A member 1 Homo sapiens 45-50 31000417-1 2019 BACKGROUND: The polymorphic CYP2D6 enzyme metabolises the antipsychotic drugs risperidone and aripiprazole to their active metabolites, 9OH-risperidone and dehydroaripiprazole. Paliperidone Palmitate 136-151 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 28-34 30848967-8 2019 CONCLUSIONS: Our study confirmed the effects of LAI paliperidone and risperidone on PRL levels. Paliperidone Palmitate 52-64 prolactin Homo sapiens 84-87 31106995-7 2019 Results: Risperidone, paliperidone, and amisulpride are associated with higher prolactin levels than would be anticipated from striatal dopamine receptor occupancy studies. Paliperidone Palmitate 22-34 prolactin Homo sapiens 79-88 31106995-10 2019 Conclusions: The anatomy of the portal circulation, the presence of P-gp, and the high affinity of this protein to risperidone, paliperidone, and amisulpride all conspire to concentrate the antipsychotic concentration in the anterior pituitary to levels higher than in other parts of the brain, with consequent increase of prolactin above expectations. Paliperidone Palmitate 128-140 prolactin Homo sapiens 323-332 30967134-9 2019 Furthermore, the rs40184 and rs3863145 variants in SLC6A3 gene appeared to be associated with HPRL in the subgroup of patients using the risperidone/paliperidone, but not with HPRL induced by other antipsychotic drugs. Paliperidone Palmitate 149-161 solute carrier family 6 member 3 Homo sapiens 51-57 31110832-4 2019 Paliperidone is a D2, 5HT2A receptor antagonist with additional antagonist activity at alpha-1 and alpha-2, H-1 receptor sites, and four metabolic pathways identified for its metabolism. Paliperidone Palmitate 0-12 5-hydroxytryptamine receptor 2A Homo sapiens 22-36 31110832-4 2019 Paliperidone is a D2, 5HT2A receptor antagonist with additional antagonist activity at alpha-1 and alpha-2, H-1 receptor sites, and four metabolic pathways identified for its metabolism. Paliperidone Palmitate 0-12 adrenoceptor alpha 1D Homo sapiens 87-94 30506237-10 2019 Prolactin elevation is highest with paliperidone, risperidone, and amisulpride. Paliperidone Palmitate 36-48 prolactin Homo sapiens 0-9 30758986-4 2019 RESULTS: During the 12-month study period significant improvement was registered in patients receiving both paliperidone palmitate and risperidone in the following scales: PANSS, PSP, CGI-I, and CGI-S. Paliperidone Palmitate 108-130 BPI fold containing family A member 2 Homo sapiens 179-182 30758986-5 2019 Patients receiving paliperidone palmitate had significantly greater improvement in PANSS, CGI-S, and PSP compared with the risperidone group. Paliperidone Palmitate 19-41 BPI fold containing family A member 2 Homo sapiens 101-104 30426252-0 2019 Genetic variations in the ADCK1 gene predict paliperidone palmitate efficacy in Han Chinese patients with schizophrenia. Paliperidone Palmitate 45-67 aarF domain containing kinase 1 Homo sapiens 26-31 30426252-1 2019 Genome-wide association study results have linked ADCK1 genetic variation with paliperidone efficacy in a European cohort. Paliperidone Palmitate 79-91 aarF domain containing kinase 1 Homo sapiens 50-55 30426252-4 2019 Examination of 13 ADCK1 genetic variants revealed two single nucleotide polymorphisms (rs12590199, rs11159291) and one haplotype (rs2364747-rs12590199) associated with paliperidone palmitate response. Paliperidone Palmitate 168-190 aarF domain containing kinase 1 Homo sapiens 18-23 30426252-5 2019 Future work into ADCK1"s function and its potential interaction with paliperidone is warranted. Paliperidone Palmitate 69-81 aarF domain containing kinase 1 Homo sapiens 17-22 29914302-0 2018 Prolactin levels: sex differences in the effects of risperidone, 9-hydroxyrisperidone levels, CYP2D6 and ABCB1 variants. Paliperidone Palmitate 65-85 prolactin Homo sapiens 0-9 30246715-0 2018 Effects of Risperidone and Paliperidone on Brain-Derived Neurotrophic Factor and N400 in First-Episode Schizophrenia. Paliperidone Palmitate 27-39 brain derived neurotrophic factor Homo sapiens 43-76 30246715-1 2018 Background: Risperidone and paliperidone have been the mainstay treatment for schizophrenia and their potential role in neuroprotection could be associated with brain-derived neurotrophic factor (BDNF) and N400 (an event-related brain potential component). Paliperidone Palmitate 28-40 brain derived neurotrophic factor Homo sapiens 161-194 30246715-1 2018 Background: Risperidone and paliperidone have been the mainstay treatment for schizophrenia and their potential role in neuroprotection could be associated with brain-derived neurotrophic factor (BDNF) and N400 (an event-related brain potential component). Paliperidone Palmitate 28-40 brain derived neurotrophic factor Homo sapiens 196-200 30246715-3 2018 However, few studies have been conducted on the mechanism of risperidone and paliperidone on BDNF and N400. Paliperidone Palmitate 77-89 brain derived neurotrophic factor Homo sapiens 93-97 30246715-4 2018 This study aimed to compare the effects of risperidone and paliperidone on BDNF and the N400 component of the event-related brain potential in patients with first-episode schizophrenia. Paliperidone Palmitate 59-71 brain derived neurotrophic factor Homo sapiens 75-79 30246715-12 2018 A negative correlation between the reduction rate of the PANSS score and the increase in serum BDNF level after the treatment was found in the paliperidone group but not in the risperidone group. Paliperidone Palmitate 143-155 brain derived neurotrophic factor Homo sapiens 95-99 30246715-13 2018 Conclusions: Both risperidone and paliperidone could increase the serum BDNF levels in patients with first-episode schizophrenia and improve their cognitive function (N400 latency and amplitude), but their antipsychotic mechanisms might differ. Paliperidone Palmitate 34-46 brain derived neurotrophic factor Homo sapiens 72-76 30093744-8 2018 Results: The number of CYP2D6*4 alleles affected the plasma levels of risperidone, 9-hydroxyrisperidone at 6 weeks of treatment but not at 12 weeks. Paliperidone Palmitate 83-103 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 23-29 30449206-9 2018 Any clinician considering switching patients to PP1M: 1) should switch from oral risperidone to PP1M rather than from oral paliperidone to PP1M, and 2) become proficient in paliperidone TDM to use during switches. Paliperidone Palmitate 173-185 neuropeptide Y receptor Y6 (pseudogene) Homo sapiens 139-150 30542502-0 2018 Paliperidone, a relatively novel atypical antipsychotic drug, is a substrate for breast cancer resistance protein. Paliperidone Palmitate 0-12 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 81-113 30214207-0 2018 Aripiprazole combination for reversal of paliperidone-induced increase in prolactin level. Paliperidone Palmitate 41-53 prolactin Homo sapiens 74-83 30214207-3 2018 Herein, we followed up a patient with elevated prolactin caused by paliperidone and found that the prolactin level was decreased after the administration of a combination with a low-dose aripiprazole. Paliperidone Palmitate 67-79 prolactin Homo sapiens 47-56 30214207-3 2018 Herein, we followed up a patient with elevated prolactin caused by paliperidone and found that the prolactin level was decreased after the administration of a combination with a low-dose aripiprazole. Paliperidone Palmitate 67-79 prolactin Homo sapiens 99-108 29914302-1 2018 AIM: The role of sex on the association of plasma prolactin levels with risperidone (R) and 9-hydroxyrisperidone (9-OHR) concentrations is investigated. Paliperidone Palmitate 92-112 prolactin Homo sapiens 50-59 29776316-3 2018 Paliperidone clearance was calculated from: 1) steady-state studies using concentration/dose (C/D) ratios, and 2) single-dose studies describing 24-h area under the curve calculations. Paliperidone Palmitate 0-12 complement C2 Homo sapiens 94-112 29802039-12 2018 Risperidone, haloperidol, paliperidone and olanzapine were associated with prolactin increase. Paliperidone Palmitate 26-38 prolactin Homo sapiens 75-84 28946784-0 2017 Associations of fatty acids with cognition, psychopathology, and brain-derived neurotrophic factor levels in patients with first-episode schizophrenia and related disorders treated with paliperidone extended release. Paliperidone Palmitate 186-198 brain derived neurotrophic factor Homo sapiens 65-98 29443543-3 2018 ABCB11199A recombinant cells had more sensitivity to olanzapine (2.2-fold, p < 0.01), aripiprazole (1.8-fold, p < 0.01), amisulpride (2.3-fold, p < 0.01), and risperidone (3.1-fold, p < 0.01) than ABCB1wt cells, while the resistance to paliperidone in both recombinant cell models was similar. Paliperidone Palmitate 248-260 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 29314615-0 2018 Serum prolactin levels might become a useful marker for switching strategy to paliperidone palmitate in male schizophrenia patient. Paliperidone Palmitate 78-100 prolactin Homo sapiens 6-15 28454922-0 2018 Paliperidone palmitate once-monthly maintains improvement in functioning domains of the Personal and Social Performance scale compared with placebo in subjects with schizoaffective disorder. Paliperidone Palmitate 0-22 BPI fold containing family A member 2 Homo sapiens 88-119 28454922-1 2018 OBJECTIVE: Evaluate the effect of paliperidone palmitate once-monthly (PP1M) injectable on the specific functioning domains of the Personal and Social Performance (PSP) scale in patients with schizoaffective disorder (SCA) participating in a long-term study. Paliperidone Palmitate 34-56 BPI fold containing family A member 2 Homo sapiens 131-162 28454922-1 2018 OBJECTIVE: Evaluate the effect of paliperidone palmitate once-monthly (PP1M) injectable on the specific functioning domains of the Personal and Social Performance (PSP) scale in patients with schizoaffective disorder (SCA) participating in a long-term study. Paliperidone Palmitate 34-56 BPI fold containing family A member 2 Homo sapiens 164-167 29040230-9 2017 CONCLUSIONS: The data show a 4-fold interindividual difference in dose-adjusted serum concentrations within the 10-90 percentile range and illustrate the significant effects of age and p-glycoprotein induction on the pharmacokinetics of paliperidone. Paliperidone Palmitate 237-249 ATP binding cassette subfamily B member 1 Homo sapiens 185-199 29226628-4 2017 Using interspecies scaling approaches, human D2 receptor occupancy and plasma prolactin concentrations were predicted for a range of clinical paliperidone and remoxipride doses. Paliperidone Palmitate 142-154 prolactin Homo sapiens 78-87 29226628-6 2017 The pool model could predict D2 receptor occupancy and prolactin response in humans following single doses of paliperidone and remoxipride. Paliperidone Palmitate 110-122 prolactin Homo sapiens 55-64 28272498-6 2017 We confirmed that the brain disposition of risperidone and 9-hydroxy risperidone is strongly influenced by P-gp, as P-gp knockout mice displayed greater brain concentrations of these drugs than wild-type mice. Paliperidone Palmitate 59-80 phosphoglycolate phosphatase Mus musculus 107-111 29048190-9 2017 Paliperidone was associated with a greater use of anticholinergic medications (p = .002), increased body weight (p < .001), and higher serum prolactin level (p < .001) compared with a placebo. Paliperidone Palmitate 0-12 prolactin Homo sapiens 144-153 28272498-6 2017 We confirmed that the brain disposition of risperidone and 9-hydroxy risperidone is strongly influenced by P-gp, as P-gp knockout mice displayed greater brain concentrations of these drugs than wild-type mice. Paliperidone Palmitate 59-80 phosphoglycolate phosphatase Mus musculus 116-120 28660406-0 2017 Evaluation of Potentially Prolactin-Related Adverse Events and Sexual Maturation in Adolescents with Schizophrenia Treated with Paliperidone Extended-Release (ER) for 2 Years: A Post Hoc Analysis of an Open-Label Multicenter Study. Paliperidone Palmitate 128-140 prolactin Homo sapiens 26-35 28660406-3 2017 OBJECTIVE: This study assessed potentially prolactin-related treatment-emergent adverse events (PPRL-TEAEs) and sexual maturation during long-term treatment of adolescents with paliperidone extended-release (ER). Paliperidone Palmitate 177-189 prolactin Homo sapiens 43-52 26987678-7 2017 Results In the PFC of rats exposed to acute stress, paliperidone increased CB1 receptor (CB1R) expression. Paliperidone Palmitate 52-64 cannabinoid receptor 1 Rattus norvegicus 75-78 26987678-8 2017 Furthermore, paliperidone increased the expression of the eCB synthesis enzymes N-acylphosphatidylethanolamine- hydrolysing phospholipase D and DAGLalpha, and blocked the stress-induced increased expression of the degrading enzyme fatty acid amide hydrolase. Paliperidone Palmitate 13-25 diacylglycerol lipase, alpha Rattus norvegicus 144-153 26987678-9 2017 In chronic conditions, paliperidone prevented the chronic stress-induced down-regulation of CB1R, normalised DAGLalpha expression and reverted stress-induced down-regulation of the 2-AG degrading enzyme monoacylglycerol lipase. Paliperidone Palmitate 23-35 diacylglycerol lipase, alpha Rattus norvegicus 109-118 26987678-9 2017 In chronic conditions, paliperidone prevented the chronic stress-induced down-regulation of CB1R, normalised DAGLalpha expression and reverted stress-induced down-regulation of the 2-AG degrading enzyme monoacylglycerol lipase. Paliperidone Palmitate 23-35 monoglyceride lipase Rattus norvegicus 203-226 26987678-11 2017 Acute stress decreased DAGLalpha expression, an effect prevented by paliperidone. Paliperidone Palmitate 68-80 diacylglycerol lipase, alpha Rattus norvegicus 23-32 26987678-12 2017 Contrarily, chronic stress increased DAGLalpha and this effect was potentiated by paliperidone. Paliperidone Palmitate 82-94 diacylglycerol lipase, alpha Rattus norvegicus 37-46 28265686-0 2017 Inhibition of cloned hERG potassium channels by risperidone and paliperidone. Paliperidone Palmitate 64-76 ETS transcription factor ERG Homo sapiens 21-25 28133766-5 2017 RESULTS: CYP2D6 poor and intermediate metabolizers had lower formation rates of 9-hydroxy-risperidone (94% and 76% lower, respectively) compared to the extensive CYP2D6 metabolizers. Paliperidone Palmitate 80-101 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 9-15 28265686-2 2017 We used a patch-clamp study to investigate the effects of paliperidone on hERG potassium channels expressed in HEK cells. Paliperidone Palmitate 58-70 ETS transcription factor ERG Homo sapiens 74-78 28265686-3 2017 Western blot analyses were used to study the effects of risperidone and paliperidone on hERG and hERG 3.1 isoform channel trafficking. Paliperidone Palmitate 72-84 ETS transcription factor ERG Homo sapiens 88-92 28265686-3 2017 Western blot analyses were used to study the effects of risperidone and paliperidone on hERG and hERG 3.1 isoform channel trafficking. Paliperidone Palmitate 72-84 ETS transcription factor ERG Homo sapiens 97-103 28265686-4 2017 Risperidone and paliperidone inhibited the hERG tail currents in a concentration-dependent manner with IC50 values of 0.16 and 0.57 muM, respectively. Paliperidone Palmitate 16-28 ETS transcription factor ERG Homo sapiens 43-47 28265686-5 2017 The block of hERG currents by paliperidone was voltage-dependent, increasing over a range of voltages for channel activation. Paliperidone Palmitate 30-42 ETS transcription factor ERG Homo sapiens 13-17 28265686-6 2017 A fast application of paliperidone inhibited the hERG current elicited by a 5-s depolarizing pulse to +60 mV to fully inactivate the hERG currents, suggesting an inactivated state block. Paliperidone Palmitate 22-34 ETS transcription factor ERG Homo sapiens 49-53 28265686-6 2017 A fast application of paliperidone inhibited the hERG current elicited by a 5-s depolarizing pulse to +60 mV to fully inactivate the hERG currents, suggesting an inactivated state block. Paliperidone Palmitate 22-34 ETS transcription factor ERG Homo sapiens 133-137 28265686-7 2017 A fast application of paliperidone during repolarization reversibly inhibited the hERG tail currents in a concentration-dependent manner with a IC50 value of 1.26 muM. Paliperidone Palmitate 22-34 ETS transcription factor ERG Homo sapiens 82-86 28265686-8 2017 Kinetic analysis of paliperidone interaction with the open state of the hERG channels showed that the rate constants of association (k +1) and dissociation (k -1) for paliperidone were 0.45 muM-1 s-1 and 1.07 s-1, respectively. Paliperidone Palmitate 20-32 ETS transcription factor ERG Homo sapiens 72-76 28265686-8 2017 Kinetic analysis of paliperidone interaction with the open state of the hERG channels showed that the rate constants of association (k +1) and dissociation (k -1) for paliperidone were 0.45 muM-1 s-1 and 1.07 s-1, respectively. Paliperidone Palmitate 20-32 PWWP domain containing 3A, DNA repair factor Homo sapiens 190-205 28265686-8 2017 Kinetic analysis of paliperidone interaction with the open state of the hERG channels showed that the rate constants of association (k +1) and dissociation (k -1) for paliperidone were 0.45 muM-1 s-1 and 1.07 s-1, respectively. Paliperidone Palmitate 167-179 ETS transcription factor ERG Homo sapiens 72-76 28265686-8 2017 Kinetic analysis of paliperidone interaction with the open state of the hERG channels showed that the rate constants of association (k +1) and dissociation (k -1) for paliperidone were 0.45 muM-1 s-1 and 1.07 s-1, respectively. Paliperidone Palmitate 167-179 PWWP domain containing 3A, DNA repair factor Homo sapiens 190-205 28265686-9 2017 Paliperidone shifted the steady-state inactivation curve of the hERG currents in a hyperpolarizing direction and also produced a use-dependent block. Paliperidone Palmitate 0-12 ETS transcription factor ERG Homo sapiens 64-68 28265686-11 2017 Our results indicated that paliperidone inhibited the hERG current by preferentially interacting with the open and inactivated states of the channel, but not by disruption of hERG channel protein trafficking. Paliperidone Palmitate 27-39 ETS transcription factor ERG Homo sapiens 54-58 27846195-9 2017 CONCLUSION: Genetic variations in the ADCK1 gene may differentially predict paliperidone efficacy in schizophrenic patients. Paliperidone Palmitate 76-88 aarF domain containing kinase 1 Homo sapiens 38-43 28520384-2 2012 Risperidone is metabolized to the active metabolite 9-hydroxyrisperidone by the enzyme CYP2D6 and to a lesser extent by CYP3A4. Paliperidone Palmitate 52-72 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 87-93 28039001-8 2017 Chronic paliperidone blocked this neuroinflammatory response possibly by the synergic activation and preservation of endogenous antioxidant/anti-inflammatory mechanisms such as NRF2 and PPARgamma pathways, respectively. Paliperidone Palmitate 8-20 nuclear factor, erythroid derived 2, like 2 Mus musculus 177-181 28039001-8 2017 Chronic paliperidone blocked this neuroinflammatory response possibly by the synergic activation and preservation of endogenous antioxidant/anti-inflammatory mechanisms such as NRF2 and PPARgamma pathways, respectively. Paliperidone Palmitate 8-20 peroxisome proliferator activated receptor gamma Mus musculus 186-195 27738718-0 2017 Erratum to: Genotype and co-medication dependent CYP2D6 metabolic activity: effects on serum concentrations of aripiprazole, haloperidol, risperidone, paliperidone and zuclopenthixol. Paliperidone Palmitate 151-163 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 28264565-0 2017 Dual Modulation of Human P-Glycoprotein and ABCG2 with Prodrug Dimers of the Atypical Antipsychotic Agent Paliperidone in a Model of the Blood-Brain Barrier. Paliperidone Palmitate 106-118 ATP binding cassette subfamily B member 1 Homo sapiens 25-39 28264565-0 2017 Dual Modulation of Human P-Glycoprotein and ABCG2 with Prodrug Dimers of the Atypical Antipsychotic Agent Paliperidone in a Model of the Blood-Brain Barrier. Paliperidone Palmitate 106-118 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 44-49 26780783-0 2017 Impact of CYP2D6 Polymorphism on Steady-State Plasma Levels of Risperidone and 9-Hydroxyrisperidone in Thai Children and Adolescents with Autism Spectrum Disorder. Paliperidone Palmitate 79-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 10-16 26780783-8 2017 Additionally, the plasma concentration of risperidone/9-OH risperidone ratio in patients with a CYP2D6 activity score of 0.5 were significantly higher than those with a CYP2D6 activity score of 2 (p = 0.04). Paliperidone Palmitate 54-70 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 96-102 26780783-11 2017 The findings indicate that CYP2D6 polymorphisms affect the plasma concentrations of risperidone and the risperidone/9-hydroxyrisperidone ratio. Paliperidone Palmitate 116-136 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 27-33 27836941-0 2017 Target-Site Investigation for the Plasma Prolactin Response: Mechanism-Based Pharmacokinetic-Pharmacodynamic Analysis of Risperidone and Paliperidone in the Rat. Paliperidone Palmitate 137-149 prolactin Rattus norvegicus 41-50 27836941-1 2017 To understand the drivers in the biological system response to dopamine D2 receptor antagonists, a mechanistic semiphysiologically based (PB) pharmacokinetic-pharmacodymanic (PKPD) model was developed to describe prolactin responses to risperidone (RIS) and its active metabolite paliperidone (PAL). Paliperidone Palmitate 280-292 prolactin Rattus norvegicus 213-222 27836941-1 2017 To understand the drivers in the biological system response to dopamine D2 receptor antagonists, a mechanistic semiphysiologically based (PB) pharmacokinetic-pharmacodymanic (PKPD) model was developed to describe prolactin responses to risperidone (RIS) and its active metabolite paliperidone (PAL). Paliperidone Palmitate 294-297 prolactin Rattus norvegicus 213-222 27145399-1 2016 The aim of this study was to investigate the impact of ageing on serum concentrations of risperidone and 9-hydroxyrisperidone in patients with known CYP2D6 genotype. Paliperidone Palmitate 105-125 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 149-155 27456824-0 2016 Association of ABCB1 Gene Polymorphisms with Efficacy and Adverse Reaction to Risperidone or Paliperidone in Han Chinese Schizophrenic Patients. Paliperidone Palmitate 93-105 ATP binding cassette subfamily B member 1 Homo sapiens 15-20 27942231-5 2016 Several studies suggested that CYP2D6 polymorphisms were associated with plasma concentration of risperidone, 9-hydroxyrisperidone, and active moiety but did not impact on clinical outcomes. Paliperidone Palmitate 110-130 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 31-37 27825323-11 2016 In evidence gathered from randomized controlled trials, risperidone, olanzapine, and two doses of paliperidone (3-5 mg/day and 6-12 mg/day) were associated with increased prolactin levels compared to baseline. Paliperidone Palmitate 98-110 prolactin Homo sapiens 171-180 27233514-5 2016 In acute stress conditions, paliperidone enhanced NRF2 levels, possibly related to phosphoinositide 3-kinase upregulation and reduced kelch-Like ECH-associated protein 1 expression. Paliperidone Palmitate 28-40 NFE2 like bZIP transcription factor 2 Rattus norvegicus 50-54 27233514-5 2016 In acute stress conditions, paliperidone enhanced NRF2 levels, possibly related to phosphoinositide 3-kinase upregulation and reduced kelch-Like ECH-associated protein 1 expression. Paliperidone Palmitate 28-40 Kelch-like ECH-associated protein 1 Rattus norvegicus 134-169 27233514-6 2016 In chronic conditions, paliperidone tended to normalize NRF2 levels through a phosphoinositide 3-kinase related-mechanism, with no effects on kelch-Like ECH-associated protein 1. Paliperidone Palmitate 23-35 NFE2 like bZIP transcription factor 2 Rattus norvegicus 56-60 27233514-8 2016 However, paliperidone increased transforming growth factor-beta and interleukin-10 in favor of an M2 microglia profile in acute stress conditions, which was also corroborated by paliperidone-induced increased levels of the M2 cellular markers arginase I and folate receptor 2. Paliperidone Palmitate 9-21 interleukin 10 Rattus norvegicus 68-82 26879343-10 2016 The results of this study showed that serum prolactin levels, especially in autistic individuals with hyperprolactinaemia during risperidone treatment, were significantly correlated with the level of 9-hydroxyrisperidone. Paliperidone Palmitate 200-220 prolactin Homo sapiens 44-53 27489380-5 2016 RESULTS: The administration of paliperidone ER resulted in significant improvement in the PANSS, SANS, CAI, and GAF scores (p<0.001) over time. Paliperidone Palmitate 31-43 USH1 protein network component sans Homo sapiens 97-101 27489380-5 2016 RESULTS: The administration of paliperidone ER resulted in significant improvement in the PANSS, SANS, CAI, and GAF scores (p<0.001) over time. Paliperidone Palmitate 31-43 fibroblast growth factor 9 Homo sapiens 112-115 26055227-0 2016 Paliperidone Protects SH-SY5Y Cells Against MK-801-Induced Neuronal Damage Through Inhibition of Ca(2+) Influx and Regulation of SIRT1/miR-134 Signal Pathway. Paliperidone Palmitate 0-12 sirtuin 1 Homo sapiens 129-134 26661162-0 2016 Regulation of P-glycoprotein expression in brain capillaries in Huntington"s disease and its impact on brain availability of antipsychotic agents risperidone and paliperidone. Paliperidone Palmitate 162-174 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 27352936-4 2016 In addition, the effects of Ris and its main metabolite, 9-hydroxyrisperidone (9-OHRis), on rat d-amino acid oxidase (DAO) activity were examined in vitro. Paliperidone Palmitate 57-77 D-amino-acid oxidase Rattus norvegicus 96-116 27352936-4 2016 In addition, the effects of Ris and its main metabolite, 9-hydroxyrisperidone (9-OHRis), on rat d-amino acid oxidase (DAO) activity were examined in vitro. Paliperidone Palmitate 57-77 D-amino-acid oxidase Rattus norvegicus 118-121 26879343-2 2016 Therefore, this study aimed to investigate the association between plasma drug concentrations of risperidone, 9-hydroxyrisperidone and serum prolactin level in Thai children and adolescents with autism spectrum disorder (ASD). Paliperidone Palmitate 110-130 prolactin Homo sapiens 141-150 26879343-7 2016 Serum prolactin level was significantly positively correlated with plasma 9-hydroxyrisperidone level (rs = 0.355, p < 0.001). Paliperidone Palmitate 74-94 prolactin Homo sapiens 6-15 26879343-9 2016 By multivariate analysis, high prolactin level was correlated to high 9-hydroxyrisperidone level (p = 0.010). Paliperidone Palmitate 70-90 prolactin Homo sapiens 31-40 27800283-0 2016 Prolactin Levels After Switching to Paliperidone Palmitate in Patients with Schizophrenia. Paliperidone Palmitate 36-58 prolactin Homo sapiens 0-9 27800283-1 2016 Objective: The aim of this study was to investigate the tolerability and efficacy of paliperidone palmitate and its effect on the levels of prolactin in patients with schizophrenia. Paliperidone Palmitate 85-107 prolactin Homo sapiens 140-149 27800283-7 2016 As measurement of paliperidone concentrations is limited in routine practice, a fluctuation range of prolactin levels may be a useful marker for confirmation of safety maintenance treatment with long-acting injectables in clinical settings. Paliperidone Palmitate 18-30 prolactin Homo sapiens 101-110 27257556-10 2016 In comparison, the brain/plasma concentration ratios of risperidone and 9-hydroxy risperidone were profoundly higher in P-gp knockout mice than WT mice. Paliperidone Palmitate 72-93 phosphoglycolate phosphatase Mus musculus 120-124 26055227-0 2016 Paliperidone Protects SH-SY5Y Cells Against MK-801-Induced Neuronal Damage Through Inhibition of Ca(2+) Influx and Regulation of SIRT1/miR-134 Signal Pathway. Paliperidone Palmitate 0-12 microRNA 134 Homo sapiens 135-142 26055227-7 2016 Neurotoxicity of 100 muM MK-801, which reduced the cell viability, was diminished by 100 muM paliperidone using MTT and LDH assays (both p < 0.05). Paliperidone Palmitate 93-105 latexin Homo sapiens 21-24 26055227-7 2016 Neurotoxicity of 100 muM MK-801, which reduced the cell viability, was diminished by 100 muM paliperidone using MTT and LDH assays (both p < 0.05). Paliperidone Palmitate 93-105 latexin Homo sapiens 89-92 26055227-10 2016 Furthermore, paliperidone significantly reversed MK-801 induced increase of SIRT1 and decrease of miR-134 expression (both p < 0.05). Paliperidone Palmitate 13-25 sirtuin 1 Homo sapiens 76-81 26055227-10 2016 Furthermore, paliperidone significantly reversed MK-801 induced increase of SIRT1 and decrease of miR-134 expression (both p < 0.05). Paliperidone Palmitate 13-25 microRNA 134 Homo sapiens 98-105 26055227-12 2016 Taken together, our results demonstrated that paliperidone could protect SH-SY5Y cells against MK-801 induced neurotoxicity via inhibition of Ca(2+) influx and regulation of SIRT1/miR-134 pathway, providing a promising and potential therapeutic target for schizophrenia. Paliperidone Palmitate 46-58 sirtuin 1 Homo sapiens 174-179 26055227-12 2016 Taken together, our results demonstrated that paliperidone could protect SH-SY5Y cells against MK-801 induced neurotoxicity via inhibition of Ca(2+) influx and regulation of SIRT1/miR-134 pathway, providing a promising and potential therapeutic target for schizophrenia. Paliperidone Palmitate 46-58 microRNA 134 Homo sapiens 180-187 25545018-4 2015 The basic aim of this study is to determine the effects of the newly marketed drug paliperidone on the activities of the enzymes adenosine deaminase (ADA), xanthine oxidase (XO), superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px) as well as on malondialdehyde (MDA) and nitric oxide (NO) levels in rat brain tissues. Paliperidone Palmitate 83-95 catalase Rattus norvegicus 207-215 26129906-12 2015 CONCLUSIONS: Genetic polymorphisms of CYP2D6 play an important role in risperidone, 9-hydroxyrisperidone and active moiety plasma concentration variability, which were associated with common side effects. Paliperidone Palmitate 84-104 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 38-44 26387027-4 2015 Pharmacokinetic parameters were derived from plasma concentrations of risperidone and its active metabolite, 9-hydroxyrisperidone (formed via CYP2D6 and CYP3A4), collected before and over 4 days after risperidone administration, and from steady-state plasma concentrations of armodafinil and its circulating metabolites, R-modafinil acid and modafinil sulfone. Paliperidone Palmitate 109-129 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 142-148 26424421-9 2015 RESULTS: The average ICER of paliperidone compared to placebo reached 28,935 EUR/QALY. Paliperidone Palmitate 29-41 cAMP responsive element modulator Homo sapiens 21-25 26424421-11 2015 CONCLUSIONS: Treatment of SAD with paliperidone results in acceptable ICER and high probability of being cost-effective compared to placebo. Paliperidone Palmitate 35-47 cAMP responsive element modulator Homo sapiens 70-74 25545018-11 2015 RESULTS: Our results demonstrated that paliperidone significantly decreased the activities of ADA (P = 0.015), XO (P = 0.0001), and CAT (P = 0.004) while insignificantly increasing the activity of SOD (P = 0.49), MDA (P = 0.71), and NO (P = 0.26) levels in rat brain tissues. Paliperidone Palmitate 39-51 catalase Rattus norvegicus 132-135 25545018-12 2015 In addition, paliperidone insignificantly decreased the activity of GSH-Px (P = 0.30) compared to the control group in rat brain tissues. Paliperidone Palmitate 13-25 glutathione peroxidase 1 Rattus norvegicus 68-74 26944100-7 2016 The plasma concentration of risperidone and risperidone/9-hydroxyrisperidone ratio in the patients were significant differences among the CYP2D6 predicted phenotype group (P = 0.001 and P < 0.0001 respectively). Paliperidone Palmitate 56-76 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 138-144 26944100-8 2016 Moreover, the plasma concentration of risperidone and risperidone/9-hydroxyrisperidone ratio in the patients with CYP2D6 activity score 0.5 were significantly higher than those with the CYP2D6 activity score 2.0 (P = 0.004 and P = 0.002 respectively). Paliperidone Palmitate 66-86 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 114-120 26514968-0 2016 Genotype and co-medication dependent CYP2D6 metabolic activity: effects on serum concentrations of aripiprazole, haloperidol, risperidone, paliperidone and zuclopenthixol. Paliperidone Palmitate 139-151 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 37-43 26514968-10 2016 It was demonstrated that CYP2D6 polymorphisms affect the serum concentrations of aripiprazole (n = 18), haloperidol (n = 11), risperidone (n = 20), and zuclopenthixol (n = 6), while no influence was seen on the paliperidone serum concentrations (n = 31). Paliperidone Palmitate 211-223 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 25-31 26418700-6 2016 The sensitivity, specificity, positive predictive value, and negative predictive value (confidence interval) of a risperidone/9-hydroxyrisperidone ratio >1 to predict a CYP2D6 poor metabolizer genotype were 91% (76%-97%), 86% (83%-89%), 35% (26%-46%), and 99% (97%-100%), respectively. Paliperidone Palmitate 126-146 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 172-178 27478670-0 2016 Paliperidone Induced Hypoglycemia by Increasing Insulin Secretion. Paliperidone Palmitate 0-12 insulin Homo sapiens 48-55 27478670-4 2016 Paliperidone may induce hypoglycemia by increasing insulin secretion. Paliperidone Palmitate 0-12 insulin Homo sapiens 51-58 25545018-4 2015 The basic aim of this study is to determine the effects of the newly marketed drug paliperidone on the activities of the enzymes adenosine deaminase (ADA), xanthine oxidase (XO), superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px) as well as on malondialdehyde (MDA) and nitric oxide (NO) levels in rat brain tissues. Paliperidone Palmitate 83-95 catalase Rattus norvegicus 217-220 25545018-4 2015 The basic aim of this study is to determine the effects of the newly marketed drug paliperidone on the activities of the enzymes adenosine deaminase (ADA), xanthine oxidase (XO), superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px) as well as on malondialdehyde (MDA) and nitric oxide (NO) levels in rat brain tissues. Paliperidone Palmitate 83-95 glutathione peroxidase 1 Rattus norvegicus 251-257 25522409-7 2014 RESULTS: Paliperidone pre-treatment prevented TLR-4 activation and neuroinflammation in the prefrontal cortices of stressed rats. Paliperidone Palmitate 9-21 toll-like receptor 4 Rattus norvegicus 46-51 25714000-6 2015 RESULTS: We identified an SNP in ERBB4 that may contribute toward differential treatment response to paliperidone. Paliperidone Palmitate 101-113 erb-b2 receptor tyrosine kinase 4 Homo sapiens 33-38 25714000-10 2015 CONCLUSION: These preliminary findings suggest that genetic variation in the ERBB4 gene may differentially affect treatment response to paliperidone in individuals with schizophrenia. Paliperidone Palmitate 136-148 erb-b2 receptor tyrosine kinase 4 Homo sapiens 77-82 26449925-2 2015 We report about two patients who developed an up to threefold increase of dose-related serum concentrations of risperidone"s active moiety (risperidone plus 9-hydroxyrisperidone) during acute inflammation indicated by elevated C-reactive protein. Paliperidone Palmitate 157-177 C-reactive protein Homo sapiens 227-245 25522409-9 2014 In addition, paliperidone also prevented the activation of the endogenous activators of TLR-4 HSP70 and HGMB-1. Paliperidone Palmitate 13-25 toll-like receptor 4 Rattus norvegicus 88-93 25522409-10 2014 CONCLUSIONS: Our results showed a regulatory role of paliperidone on brain TLR-4, which could explain the therapeutic benefits of its use for the treatment of psychotic diseases beyond its effects on dopamine and serotonin neurotransmission. Paliperidone Palmitate 53-65 toll-like receptor 4 Rattus norvegicus 75-80 24677189-8 2014 Although the highest rates of HPRL are consistently reported in association with amisulpride, risperidone and paliperidone, while aripiprazole and quetiapine have the most favorable profile with respect to this outcome, all SGAs can induce PRL elevations, especially at the beginning of treatment, and have the potential to cause new-onset HPRL. Paliperidone Palmitate 110-122 prolactin Homo sapiens 31-34 24589909-5 2014 P-gp removes both RIS and its metabolite 9-OH-RIS from cardiac tissue. Paliperidone Palmitate 41-49 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 24962437-0 2014 Paliperidone protects SK-N-SH cells against glutamate toxicity via Akt1/GSK3beta signaling pathway. Paliperidone Palmitate 0-12 AKT serine/threonine kinase 1 Homo sapiens 67-71 24962437-0 2014 Paliperidone protects SK-N-SH cells against glutamate toxicity via Akt1/GSK3beta signaling pathway. Paliperidone Palmitate 0-12 glycogen synthase kinase 3 beta Homo sapiens 72-80 24962437-9 2014 In addition, paliperidone also effectively reversed glutamate-induced decreases of gene expression and phosphorylation of Akt1 and GSK3beta (both p<0.05). Paliperidone Palmitate 13-25 AKT serine/threonine kinase 1 Homo sapiens 122-126 24962437-9 2014 In addition, paliperidone also effectively reversed glutamate-induced decreases of gene expression and phosphorylation of Akt1 and GSK3beta (both p<0.05). Paliperidone Palmitate 13-25 glycogen synthase kinase 3 beta Homo sapiens 131-139 24962437-10 2014 Our results demonstrated that paliperidone could effectively protect SK-N-SH cells from glutamate-induced damages via Akt1/GSK3beta signaling pathway. Paliperidone Palmitate 30-42 AKT serine/threonine kinase 1 Homo sapiens 118-122 24962437-10 2014 Our results demonstrated that paliperidone could effectively protect SK-N-SH cells from glutamate-induced damages via Akt1/GSK3beta signaling pathway. Paliperidone Palmitate 30-42 glycogen synthase kinase 3 beta Homo sapiens 123-131 24677189-11 2014 However, antipsychotics having a high potential for PRL elevation (amisulpride, risperidone and paliperidone) can have a profound impact on PRL levels even at relatively low doses, while PRL levels with antipsychotics having a minimal effect on PRL, in most cases, can remain unchanged (quetiapine) or reduce (aripiprazole) over all dosages. Paliperidone Palmitate 96-108 prolactin Homo sapiens 52-55 24677189-11 2014 However, antipsychotics having a high potential for PRL elevation (amisulpride, risperidone and paliperidone) can have a profound impact on PRL levels even at relatively low doses, while PRL levels with antipsychotics having a minimal effect on PRL, in most cases, can remain unchanged (quetiapine) or reduce (aripiprazole) over all dosages. Paliperidone Palmitate 96-108 prolactin Homo sapiens 140-143 24677189-11 2014 However, antipsychotics having a high potential for PRL elevation (amisulpride, risperidone and paliperidone) can have a profound impact on PRL levels even at relatively low doses, while PRL levels with antipsychotics having a minimal effect on PRL, in most cases, can remain unchanged (quetiapine) or reduce (aripiprazole) over all dosages. Paliperidone Palmitate 96-108 prolactin Homo sapiens 140-143 24677189-11 2014 However, antipsychotics having a high potential for PRL elevation (amisulpride, risperidone and paliperidone) can have a profound impact on PRL levels even at relatively low doses, while PRL levels with antipsychotics having a minimal effect on PRL, in most cases, can remain unchanged (quetiapine) or reduce (aripiprazole) over all dosages. Paliperidone Palmitate 96-108 prolactin Homo sapiens 140-143 23851570-5 2013 RESULTS: Prolactin levels were associated positively and significantly with risperidone levels (P=0.05), 9-hydroxyrisperidone levels (P<=0.0001), and with the oral risperidone dose in milligrams per kilogram (P<=0.0001). Paliperidone Palmitate 105-125 prolactin Homo sapiens 9-18 24586772-10 2014 A mediation analysis showed that both prolactin and benzodiazepine treatment act as mediators of the relationship between risperidone/paliperidone treatment and speed of processing. Paliperidone Palmitate 134-146 prolactin Homo sapiens 38-47 23826915-5 2013 Interestingly, for 5-HT2A -mediated recruitment of beta-arrestin, 5-HT2A -mediated sensitization of ERK, and dopamine D2 -mediated sensitization of adenylyl cyclase signalling, both paliperidone and risperidone behaved as agonists. Paliperidone Palmitate 182-194 5-hydroxytryptamine receptor 2A Homo sapiens 21-25 23609388-0 2013 Impact of the ABCB1 gene polymorphism on plasma 9-hydroxyrisperidone and active moiety levels in Japanese patients with schizophrenia. Paliperidone Palmitate 48-68 ATP binding cassette subfamily B member 1 Homo sapiens 14-19 23583326-0 2013 Paliperidone protects prefrontal cortical neurons from damages caused by MK-801 via Akt1/GSK3beta signaling pathway. Paliperidone Palmitate 0-12 thymoma viral proto-oncogene 1 Mus musculus 84-88 23583326-0 2013 Paliperidone protects prefrontal cortical neurons from damages caused by MK-801 via Akt1/GSK3beta signaling pathway. Paliperidone Palmitate 0-12 glycogen synthase kinase 3 beta Mus musculus 89-97 23583326-7 2013 Moreover, paliperidone could significantly retard MK-801-mediated inhibition of neurite outgrowth (p<0.01) and reverse MK-801-induced decreases of gene expression and phosphorylation of Akt1 and GSK3beta (both p<0.01). Paliperidone Palmitate 10-22 thymoma viral proto-oncogene 1 Mus musculus 189-193 23583326-7 2013 Moreover, paliperidone could significantly retard MK-801-mediated inhibition of neurite outgrowth (p<0.01) and reverse MK-801-induced decreases of gene expression and phosphorylation of Akt1 and GSK3beta (both p<0.01). Paliperidone Palmitate 10-22 glycogen synthase kinase 3 beta Mus musculus 198-206 23583326-9 2013 Taking together, our results demonstrated that paliperidone could protect prefrontal cortical neurons from MK-801-induced damages via Akt1/GSK3beta signaling pathway. Paliperidone Palmitate 47-59 thymoma viral proto-oncogene 1 Mus musculus 134-138 23583326-9 2013 Taking together, our results demonstrated that paliperidone could protect prefrontal cortical neurons from MK-801-induced damages via Akt1/GSK3beta signaling pathway. Paliperidone Palmitate 47-59 glycogen synthase kinase 3 beta Mus musculus 139-147 23609388-9 2013 The ABCB1 3435C>T genetic polymorphism may predict plasma 9-OH-RIS and total active moiety levels. Paliperidone Palmitate 61-69 ATP binding cassette subfamily B member 1 Homo sapiens 4-9 22623266-0 2012 Population pharmacokinetic analysis of risperidone and 9-hydroxyrisperidone with genetic polymorphisms of CYP2D6 and ABCB1. Paliperidone Palmitate 55-75 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 106-112 23503445-7 2013 RESULTS: Treatment with those antipsychotics believed associated with a higher risk for MetS (ie, AAPs: olanzapine, quetiapine, risperidone, paliperidone, clozapine) was found to be associated with significantly greater TNF-alpha (F 1,88 = 11.2, P = 0.001, mean difference of 1.7 +- 0.51) and a higher likelihood of MetS (F 1,88 = 4.5, P = 0.036) than in those not receiving treatment with an AAP. Paliperidone Palmitate 141-153 tumor necrosis factor Homo sapiens 220-229 23232756-0 2013 Changes in prolactin levels and sexual function in young psychotic patients after switching from long-acting injectable risperidone to paliperidone palmitate. Paliperidone Palmitate 135-157 prolactin Homo sapiens 11-20 22947594-0 2012 An analysis of potentially prolactin-related adverse events and abnormal prolactin values in randomized clinical trials with paliperidone palmitate. Paliperidone Palmitate 125-147 prolactin Homo sapiens 27-36 22947594-1 2012 BACKGROUND: Paliperidone palmitate has been associated with serum prolactin elevations in some patients. Paliperidone Palmitate 12-34 prolactin Homo sapiens 66-75 22947594-13 2012 CONCLUSIONS: Clinicians should periodically assess patients on paliperidone palmitate for any PPR-AEs and carefully assess the benefits and risks when managing these effects. Paliperidone Palmitate 63-85 PPR1 Homo sapiens 94-97 23205514-10 2013 The repeated exposures of silymarin, compared to single administration of silymarin, increased oral bioavailability and affected the pharmacokinetics of risperidone and 9-hydroxyrisperidone, by inhibiting P-gp. Paliperidone Palmitate 169-189 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 205-209 22691713-6 2012 Affinity of blonanserin, risperidone, and 9-hydroxyrisperidone for P-gp was evaluated by in vitro transcellular transport across LLC-PK1, human MDR1 cDNA-transfected LLC-PK1 (LLC-MDR1), and mouse Mdr1a cDNA-transfected LLC-PK1 (LLC-Mdr1a). Paliperidone Palmitate 42-62 phosphoglycolate phosphatase Homo sapiens 67-71 22691713-6 2012 Affinity of blonanserin, risperidone, and 9-hydroxyrisperidone for P-gp was evaluated by in vitro transcellular transport across LLC-PK1, human MDR1 cDNA-transfected LLC-PK1 (LLC-MDR1), and mouse Mdr1a cDNA-transfected LLC-PK1 (LLC-Mdr1a). Paliperidone Palmitate 42-62 ATP binding cassette subfamily B member 1 Homo sapiens 144-148 22929407-0 2012 Population pharmacokinetic modeling of risperidone and 9-hydroxyrisperidone to estimate CYP2D6 subpopulations in children and adolescents. Paliperidone Palmitate 55-75 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 88-94 22929407-5 2012 RESULTS: A 1-compartment mixture model described risperidone and (+-)-9-hydroxyrisperidone clearances for 3 CYP2D6 metabolizer subpopulations: extensive, intermediate, and poor. Paliperidone Palmitate 65-90 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 108-114 22967779-4 2012 Dopamine D2 receptor occupancy levels at trough were estimated from plasma concentrations of risperidone plus 9-hydroxyrisperidone immediately before the intramuscular injection of risperidone LAI, using a 1-site binding model derived from our previous positron emission tomography data. Paliperidone Palmitate 110-130 dopamine receptor D2 Homo sapiens 0-20 22623266-0 2012 Population pharmacokinetic analysis of risperidone and 9-hydroxyrisperidone with genetic polymorphisms of CYP2D6 and ABCB1. Paliperidone Palmitate 55-75 ATP binding cassette subfamily B member 1 Homo sapiens 117-122 22623266-1 2012 This study estimated the population pharmacokinetics of risperidone and its active metabolite, 9-hydroxyrisperidone, according to genetic polymorphisms in the metabolizing enzyme (CYP2D6) and transporter (ABCB1) genes in healthy subjects. Paliperidone Palmitate 95-115 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 180-186 22623266-1 2012 This study estimated the population pharmacokinetics of risperidone and its active metabolite, 9-hydroxyrisperidone, according to genetic polymorphisms in the metabolizing enzyme (CYP2D6) and transporter (ABCB1) genes in healthy subjects. Paliperidone Palmitate 95-115 ATP binding cassette subfamily B member 1 Homo sapiens 205-210 22623266-10 2012 The population pharmacokinetic model of risperidone and 9-hydroxyrisperidone including the genetic polymorphisms of CYP2D6*10 and ABCB1 3435C>T as covariates was successfully constructed. Paliperidone Palmitate 56-76 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 116-122 22623266-10 2012 The population pharmacokinetic model of risperidone and 9-hydroxyrisperidone including the genetic polymorphisms of CYP2D6*10 and ABCB1 3435C>T as covariates was successfully constructed. Paliperidone Palmitate 56-76 ATP binding cassette subfamily B member 1 Homo sapiens 130-135 22623266-11 2012 The estimated contribution of genetic polymorphisms in CYP2D6*10 and ABCB1 3435C>T to population pharmacokinetics of risperidone and 9-hydroxyrisperidone suggests the interplay of CYP2D6 and ABCB1 on the pharmacokinetics of risperidone and 9-hydroxyrisperidone according to genetic polymorphisms. Paliperidone Palmitate 136-156 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 55-61 22623266-11 2012 The estimated contribution of genetic polymorphisms in CYP2D6*10 and ABCB1 3435C>T to population pharmacokinetics of risperidone and 9-hydroxyrisperidone suggests the interplay of CYP2D6 and ABCB1 on the pharmacokinetics of risperidone and 9-hydroxyrisperidone according to genetic polymorphisms. Paliperidone Palmitate 136-156 ATP binding cassette subfamily B member 1 Homo sapiens 69-74 22623266-11 2012 The estimated contribution of genetic polymorphisms in CYP2D6*10 and ABCB1 3435C>T to population pharmacokinetics of risperidone and 9-hydroxyrisperidone suggests the interplay of CYP2D6 and ABCB1 on the pharmacokinetics of risperidone and 9-hydroxyrisperidone according to genetic polymorphisms. Paliperidone Palmitate 136-156 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 183-189 22623266-11 2012 The estimated contribution of genetic polymorphisms in CYP2D6*10 and ABCB1 3435C>T to population pharmacokinetics of risperidone and 9-hydroxyrisperidone suggests the interplay of CYP2D6 and ABCB1 on the pharmacokinetics of risperidone and 9-hydroxyrisperidone according to genetic polymorphisms. Paliperidone Palmitate 136-156 ATP binding cassette subfamily B member 1 Homo sapiens 194-199 22623266-11 2012 The estimated contribution of genetic polymorphisms in CYP2D6*10 and ABCB1 3435C>T to population pharmacokinetics of risperidone and 9-hydroxyrisperidone suggests the interplay of CYP2D6 and ABCB1 on the pharmacokinetics of risperidone and 9-hydroxyrisperidone according to genetic polymorphisms. Paliperidone Palmitate 243-263 ATP binding cassette subfamily B member 1 Homo sapiens 69-74 22623266-11 2012 The estimated contribution of genetic polymorphisms in CYP2D6*10 and ABCB1 3435C>T to population pharmacokinetics of risperidone and 9-hydroxyrisperidone suggests the interplay of CYP2D6 and ABCB1 on the pharmacokinetics of risperidone and 9-hydroxyrisperidone according to genetic polymorphisms. Paliperidone Palmitate 243-263 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 183-189 21518375-2 2012 It is mainly metabolized by human cytochrome P450 CYP2D6 and partly by CYP3A4 to 9-hydroxyrisperidone. Paliperidone Palmitate 81-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 22544010-0 2012 Different impacts of aquaporin 4 and MAOA allele variation among olanzapine, risperidone, and paliperidone in schizophrenia. Paliperidone Palmitate 94-106 monoamine oxidase A Homo sapiens 37-41 21878360-10 2012 In cells treated with dopamine in combination with antipsychotics, only paliperidone (10 muM) induced a slight improvement in cell viability. Paliperidone Palmitate 72-84 latexin Homo sapiens 89-92 22225965-2 2012 We explored symptomatic remission rate in patients treated with flexibly dosed paliperidone ER by 8 items of Positive and Negative Syndrome Scale (PANSS) and change of Personal and Social Performance (PSP) scale. Paliperidone Palmitate 79-91 BPI fold containing family A member 2 Homo sapiens 168-199 22225965-15 2012 CONCLUSIONS: Although the short-term nature of this study may limit the potential for assessing improvements in function, it is noteworthy that in the present short-term study significant improvements in patient personal and social functioning with paliperidone ER treatment were observed, as assessed by PSP scale. Paliperidone Palmitate 249-261 BPI fold containing family A member 2 Homo sapiens 305-308 21220416-5 2011 BDNF mRNA expression was significantly decreased by lithium in the CA1/2 cell fields and increased by paliperidone in the CA1/2, CA3, and dentate gyrus. Paliperidone Palmitate 102-114 brain-derived neurotrophic factor Rattus norvegicus 0-4 22332706-10 2012 For patients receiving 156 mg paliperidone palmitate, the annual incremental cost was $1216 per patient (ICER = $191 per day of relapse averted). Paliperidone Palmitate 30-52 cAMP responsive element modulator Homo sapiens 105-109 22332706-11 2012 Inclusion of generic risperidone (market share 18.6%) also resulted in net incremental cost for paliperidone palmitate ($120; ICER = $13). Paliperidone Palmitate 96-118 cAMP responsive element modulator Homo sapiens 126-130 21394035-4 2011 METHODS: (1) Patch-clamp experiments: Human ether-a-go-go-related gene (HERG)- or KCNQ1 + KCNE1-transfected cells were exposed to 0.1-100 mumol/L paliperidone (N = 39 cells, total) to assess the drug effect on HERG and KCNQ1 + KCNE1 currents. Paliperidone Palmitate 146-158 potassium voltage-gated channel subfamily E regulatory subunit 1 Homo sapiens 90-95 21394035-7 2011 RESULTS: (1) The estimated concentration at which 50% of the maximal inhibitory effect is observed (IC(50)) for paliperidone on HERG current was 0.5276 mumol/L. Paliperidone Palmitate 112-124 potassium voltage-gated channel subfamily H member 2 Homo sapiens 128-132 21394035-11 2011 CONCLUSIONS: Paliperidone prolongs the QT interval by blocking HERG current at clinically relevant concentrations and is potentially unsafe. Paliperidone Palmitate 13-25 potassium voltage-gated channel subfamily H member 2 Homo sapiens 63-67 27738355-2 2011 METHODS: In this 3-arm, double-blind, placebo- and active-controlled, parallel-group study, paliperidone ER 1.5 mg was assessed to determine the lowest efficacious dose in patients (N = 201) with acute schizophrenia. Paliperidone Palmitate 92-104 MIER1 transcriptional regulator Homo sapiens 105-109 27738355-8 2011 The most frequently reported treatment emergent adverse events (>=10%) were: placebo group-headache (15.6%) and psychotic disorder (14.1%); paliperidone ER 1.5 mg group-insomnia (13.6%); and paliperidone ER 6 mg group-headache (11.4%), insomnia (10%), and tremor (10%). Paliperidone Palmitate 143-155 MIER1 transcriptional regulator Homo sapiens 156-160 27738355-12 2011 Paliperidone ER 1.5 mg was generally tolerable with a safety profile comparable to placebo. Paliperidone Palmitate 0-12 MIER1 transcriptional regulator Homo sapiens 13-17 22713195-3 2011 Conventional antipsychotics and some of the atypical antipsychotics, such as risperidone, paliperidone, amisulpride and zotepine, are frequently associated with the raise in prolactin plasma levels. Paliperidone Palmitate 90-102 prolactin Homo sapiens 174-183 21523348-0 2011 Neuroprotection of paliperidone on SH-SY5Y cells against beta-amyloid peptide(25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death. Paliperidone Palmitate 19-31 amyloid beta precursor protein Homo sapiens 57-77 21523348-7 2011 In contrast, paliperidone works finely at low concentrations (10 and 50 muM) against Abeta(25-35) and MPP(+) and solely protected SH-SY5Y from hydrogen peroxide. Paliperidone Palmitate 13-25 latexin Homo sapiens 72-75 21523348-8 2011 At 100 muM, paliperidone completely diminished cell reduction induced by different stressors, regardless of their dosages. Paliperidone Palmitate 12-24 latexin Homo sapiens 7-10 21449914-3 2011 KEY RESULTS: Significant differences were observed between the ABCB1 3435C>T genotypes for the pharmacokinetic parameters (peak serum concentration) of risperidone and the active moiety (risperidone and its main metabolite, 9-hydroxyrisperidone). Paliperidone Palmitate 227-247 ATP binding cassette subfamily B member 1 Homo sapiens 63-68 21458237-4 2011 Only risperidone and its metabolite paliperidone significantly and selectively up-regulated liver delta-6 desaturase (Fads2) mRNA expression, and robustly increased plasma indices of n-3 and n-6 fatty acid biosynthesis. Paliperidone Palmitate 36-48 fatty acid desaturase 2 Rattus norvegicus 98-116 21458237-4 2011 Only risperidone and its metabolite paliperidone significantly and selectively up-regulated liver delta-6 desaturase (Fads2) mRNA expression, and robustly increased plasma indices of n-3 and n-6 fatty acid biosynthesis. Paliperidone Palmitate 36-48 fatty acid desaturase 2 Rattus norvegicus 118-123 21458237-5 2011 In risperidone- and paliperidone-treated rats, plasma indices of n-3 and n-6 fatty acid biosynthesis were all positively correlated with liver Fads2 mRNA expression, but not Fads1, Elovl2, or Elovl5 mRNA expression. Paliperidone Palmitate 20-32 fatty acid desaturase 2 Rattus norvegicus 143-148 21458237-5 2011 In risperidone- and paliperidone-treated rats, plasma indices of n-3 and n-6 fatty acid biosynthesis were all positively correlated with liver Fads2 mRNA expression, but not Fads1, Elovl2, or Elovl5 mRNA expression. Paliperidone Palmitate 20-32 fatty acid desaturase 1 Rattus norvegicus 174-179 21458237-5 2011 In risperidone- and paliperidone-treated rats, plasma indices of n-3 and n-6 fatty acid biosynthesis were all positively correlated with liver Fads2 mRNA expression, but not Fads1, Elovl2, or Elovl5 mRNA expression. Paliperidone Palmitate 20-32 ELOVL fatty acid elongase 2 Rattus norvegicus 181-187 21458237-5 2011 In risperidone- and paliperidone-treated rats, plasma indices of n-3 and n-6 fatty acid biosynthesis were all positively correlated with liver Fads2 mRNA expression, but not Fads1, Elovl2, or Elovl5 mRNA expression. Paliperidone Palmitate 20-32 ELOVL fatty acid elongase 5 Rattus norvegicus 192-198 21458237-8 2011 These in vivo data demonstrate that augmentation of PUFA biosynthesis is not common to all antipsychotic medications, and that risperidone and paliperidone uniquely increase delta-6 desaturase (Fads2) mRNA expression and most robustly increase PUFA biosynthesis and peripheral membrane composition. Paliperidone Palmitate 143-155 fatty acid desaturase 2 Rattus norvegicus 174-192 21458237-8 2011 These in vivo data demonstrate that augmentation of PUFA biosynthesis is not common to all antipsychotic medications, and that risperidone and paliperidone uniquely increase delta-6 desaturase (Fads2) mRNA expression and most robustly increase PUFA biosynthesis and peripheral membrane composition. Paliperidone Palmitate 143-155 fatty acid desaturase 2 Rattus norvegicus 194-199 20706126-8 2010 Reported events most likely related to paliperidone [largest attributable risks (AR)] were extra-pyramidal symptoms (AR=10), reduction in acute psychosis (AR=8), any treatment emergent adverse event (AR=6), tachycardia (AR=4), and weight gain (AR=4). Paliperidone Palmitate 39-51 androgen receptor Homo sapiens 155-159 22969177-1 2011 BACKGROUND: Paliperidone is an active metabolite of risperidone and actss through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone Palmitate 12-24 5-hydroxytryptamine receptor 2A Homo sapiens 150-165 19825908-0 2010 A comparison of serum prolactin concentrations after administration of paliperidone extended-release and risperidone tablets in patients with schizophrenia. Paliperidone Palmitate 71-83 prolactin Homo sapiens 22-31 20621147-3 2010 The present study evaluated the gender differences in the relationship between plasma levels of RIS or 9-OH-RIS and PRL. Paliperidone Palmitate 103-111 prolactin Homo sapiens 116-119 20621147-8 2010 In the female patients, there was a significant positive correlation between the plasma 9-OH-RIS levels and PRL levels (rs=0.456, p=0.049). Paliperidone Palmitate 88-96 prolactin Homo sapiens 108-111 20621147-11 2010 CONCLUSION: 9-OH-RIS is considered to play a more important role in PRL elevation than RIS, and a gender difference exists in the effect of 9-OH-RIS on PRL level. Paliperidone Palmitate 12-20 prolactin Homo sapiens 68-71 20621147-11 2010 CONCLUSION: 9-OH-RIS is considered to play a more important role in PRL elevation than RIS, and a gender difference exists in the effect of 9-OH-RIS on PRL level. Paliperidone Palmitate 140-148 prolactin Homo sapiens 152-155 20962362-0 2010 [9-hydroxy-risperidone (9OHRIS) prevents stress-induced beta-actin overexpression in rat hippocampus]. Paliperidone Palmitate 1-22 actin, beta Rattus norvegicus 56-66 19825908-1 2010 Increases in serum prolactin concentrations after administration of risperidone have been attributed, by some, to the availability of paliperidone in plasma. Paliperidone Palmitate 134-146 prolactin Homo sapiens 19-28 19825908-2 2010 This double-blind, randomized, parallel-group study in patients with schizophrenia compared serum prolactin concentrations following the administration of paliperidone extended-release and risperidone immediate-release tablets. Paliperidone Palmitate 155-167 prolactin Homo sapiens 98-107 19825908-5 2010 Mean serum prolactin concentrations increased on day 1 (C(max): 71.8 ng/ml and 89.7 ng/ml reached at 6.5 hours and 2.6 hours for paliperidone extended-release and risperidone immediate-release, respectively). Paliperidone Palmitate 129-141 prolactin Homo sapiens 11-20 19825908-7 2010 These results indicate that paliperidone extended-release 12 mg and risperidone immediate-release 4 mg, administered over a period of 6 days, lead to similar elevations in serum prolactin concentrations. Paliperidone Palmitate 28-40 prolactin Homo sapiens 178-187 21387786-2 2010 The therapeutic action of RIS depends not only on the parent compound but also its major active metabolite, 9-hydroxyrisperidone (9-OH-RIS), and the pharmacokinetics is modified by the genetic polymorphism of CYP2D6, the main site o RIS metabolism. Paliperidone Palmitate 108-128 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 209-215 21387786-2 2010 The therapeutic action of RIS depends not only on the parent compound but also its major active metabolite, 9-hydroxyrisperidone (9-OH-RIS), and the pharmacokinetics is modified by the genetic polymorphism of CYP2D6, the main site o RIS metabolism. Paliperidone Palmitate 130-138 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 209-215 18708991-0 2008 ABCB1 polymorphisms influence steady-state plasma levels of 9-hydroxyrisperidone and risperidone active moiety. Paliperidone Palmitate 60-80 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 19910717-0 2009 Impact of CYP2D6 genotype on steady-state serum concentrations of risperidone and 9-hydroxyrisperidone in patients using long-acting injectable risperidone. Paliperidone Palmitate 82-102 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 10-16 19910717-2 2009 The present study is the first to investigate the impact of CYP2D6 genotype on serum concentrations of risperidone and 9-hydroxyrisperidone in patients using injectable long-acting risperidone. Paliperidone Palmitate 119-139 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 60-66 19387994-1 2009 OBJECTIVE: Risperidone is converted to 9-hydroxyrisperidone by CYP2D6. Paliperidone Palmitate 39-59 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 63-69 19440082-0 2009 Effects of CYP2D6 and CYP3A5 genotypes on the plasma concentrations of risperidone and 9-hydroxyrisperidone in Korean schizophrenic patients. Paliperidone Palmitate 87-107 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 22-28 19440082-8 2009 CYP3A5 nonexpressors exhibited higher plasma concentrations of both RIS and 9-OH-RIS than its expressors. Paliperidone Palmitate 76-84 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 19440082-9 2009 In the case of 9-OH-RIS, CYP3A5 nonexpressors exhibited significantly higher concentrations than CYP3A5 expressors (5.42 vs 3.51 ng/mL per milligram, P = 0.022). Paliperidone Palmitate 15-23 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 25-31 19440082-11 2009 In conclusion, both CYP2D6 and CYP3A5 genotypes affected plasma levels of RIS and 9-OH-RIS, whereas the active moiety levels were influenced only by the CYP3A5 genotype but not by the CYP2D6 genotype. Paliperidone Palmitate 82-90 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 20-26 19440082-11 2009 In conclusion, both CYP2D6 and CYP3A5 genotypes affected plasma levels of RIS and 9-OH-RIS, whereas the active moiety levels were influenced only by the CYP3A5 genotype but not by the CYP2D6 genotype. Paliperidone Palmitate 82-90 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 31-37 19116265-4 2009 The C(CSF)s of eight of the nine compounds were within 3-fold of their corresponding C(m); 9-hydroxyrisperidone showed a C(CSF) 5-fold of its C(m). Paliperidone Palmitate 91-111 colony stimulating factor 2 Rattus norvegicus 123-126 19113797-3 2009 First-generation antipsychotics pose the greatest risk of causing this adverse effect; however, second-generation antipsychotics, particularly risperidone and paliperidone, also often increase prolactin secretion. Paliperidone Palmitate 159-171 prolactin Homo sapiens 193-202 18708991-1 2008 Risperidone is metabolized to its active metabolite, 9-hydroxyrisperidone, mainly by the cytochrome P450 enzymes CYP2D6 and 3A4. Paliperidone Palmitate 53-73 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 113-119 18708991-3 2008 Both risperidone and 9-hydroxyrisperidone are substrates of P-glycoprotein (P-gp), a transport protein involved in drug absorption, distribution, and elimination. Paliperidone Palmitate 21-41 ATP binding cassette subfamily B member 1 Homo sapiens 60-74 18708991-3 2008 Both risperidone and 9-hydroxyrisperidone are substrates of P-glycoprotein (P-gp), a transport protein involved in drug absorption, distribution, and elimination. Paliperidone Palmitate 21-41 ATP binding cassette subfamily B member 1 Homo sapiens 76-80 18375569-3 2008 In addition, paliperidone is associated with substantial increases in serum prolactin that may be associated with sexual dysfunction, although sexual functioning outcomes were not reported. Paliperidone Palmitate 13-25 prolactin Homo sapiens 76-85 18425951-12 2008 Adverse effect data were not well reported but paliperidone does seem to produce a greater incidence of tachycardia than placebo (n=1638, 5 RCTs, RR1.88 CI 1.28 to 2.76, NNH 21 CI 11 to 90) and a consistent, significant elevation in serum prolactin was found for both men (n=413, 3 RCTs, WMD 27.68 CI 23.66 to 31.69) and women (n=252, 3 RCTs, WMD 87.39 CI 74.27 to 100.51). Paliperidone Palmitate 47-59 ribonucleotide reductase catalytic subunit M1 Homo sapiens 146-149 18164477-2 2008 The antipsychotic drug risperidone and its active metabolite 9-hydroxyrisperidone (paliperidone) are substrates of P-gp. Paliperidone Palmitate 61-81 phosphoglycolate phosphatase Mus musculus 115-119 18164477-2 2008 The antipsychotic drug risperidone and its active metabolite 9-hydroxyrisperidone (paliperidone) are substrates of P-gp. Paliperidone Palmitate 83-95 phosphoglycolate phosphatase Mus musculus 115-119 18058087-0 2008 Dose-finding study of paliperidone ER based on striatal and extrastriatal dopamine D2 receptor occupancy in patients with schizophrenia. Paliperidone Palmitate 22-34 dopamine receptor D2 Homo sapiens 74-94 18058087-3 2008 OBJECTIVES: In this study, we measured striatal and extrastriatal dopamine D2 receptor occupancy during paliperidone ER treatment in patients with schizophrenia using positron emission tomography (PET) to compare regional occupancy and to estimate the optimal dose. Paliperidone Palmitate 104-116 dopamine receptor D2 Homo sapiens 66-86 18708991-4 2008 The aim of the present study was to evaluate the influence of polymorphisms in genes encoding CYP3A5 and P-gp (ABCB1) on the steady-state plasma levels of risperidone, 9-hydroxyrisperidone, and the active moiety, taking CYP2D6 genotype status into account. Paliperidone Palmitate 168-188 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 94-100 18708991-4 2008 The aim of the present study was to evaluate the influence of polymorphisms in genes encoding CYP3A5 and P-gp (ABCB1) on the steady-state plasma levels of risperidone, 9-hydroxyrisperidone, and the active moiety, taking CYP2D6 genotype status into account. Paliperidone Palmitate 168-188 ATP binding cassette subfamily B member 1 Homo sapiens 105-109 18708991-9 2008 The CYP2D6 genotype in these 46 patients was again associated with risperidone C/D (P = 0.001) but not with 9-hydroxyrisperidone C/D or active moiety C/D, as previously shown by our group in 37 of these patients. Paliperidone Palmitate 108-128 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-10 18708991-10 2008 Patients homozygous for the ABCB1 3435T/2677T/1236T haplotype had significantly lower C/Ds of 9-hydroxyrisperidone (P = 0.026) and active moiety (P = 0.028) than patients carrying other ABCB1 genotypes. Paliperidone Palmitate 94-114 ATP binding cassette subfamily B member 1 Homo sapiens 28-33 18708991-10 2008 Patients homozygous for the ABCB1 3435T/2677T/1236T haplotype had significantly lower C/Ds of 9-hydroxyrisperidone (P = 0.026) and active moiety (P = 0.028) than patients carrying other ABCB1 genotypes. Paliperidone Palmitate 94-114 ATP binding cassette subfamily B member 1 Homo sapiens 186-191 18708991-11 2008 In conclusion, our results confirmed the significant effect of CYP2D6 genotype on the steady-state plasma levels of risperidone and showed that ABCB1 polymorphisms have a moderate effect on those of 9-hydroxyrisperidone and the active moiety. Paliperidone Palmitate 199-219 ATP binding cassette subfamily B member 1 Homo sapiens 144-149 18728628-3 2008 CYP2D6 catalyzes the conversion of risperidone to the active metabolite 9-OH-risperidone. Paliperidone Palmitate 72-88 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 18728628-4 2008 The question whether CYP2D6 activity is important for the level of the "active moiety" (ie, the sum of risperidone and 9-OH-risperidone) is controversial. Paliperidone Palmitate 119-135 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 21-27 18728628-5 2008 Concentration-to-dose (C:D) ratios of risperidone and 9-OH-risperidone in 218 patients were associated with the number of concomitantly used substrates or inhibitors of CYP2D6. Paliperidone Palmitate 54-70 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 169-175 18325493-6 2008 We found the order of dopamine D2 receptor occupancy required to suppress conditioned avoidance response behaviour according to EC50 measurements to be sertindole (+dehydrosertindole)=dehydrosertindole=paliperidone (the metabolite of risperidone)=haloperidol=olanzapine>risperidone>>clozapine. Paliperidone Palmitate 202-214 dopamine receptor D2 Homo sapiens 22-42 18058087-6 2008 The relationship between the dose or plasma concentration of paliperidone and dopamine D2 receptor occupancy was calculated. Paliperidone Palmitate 61-73 dopamine receptor D2 Homo sapiens 78-98 18053652-5 2008 RESULTS: Compared with pretreatment values, prolactin levels at endpoint were significantly increased (p<0.00001) and correlated with risperidone doses (r=0.58, N=16, p<0.02), and plasma levels of risperidone (r=0.60, N=16, p<0.02) and 9-hydroxyrisperidone (r=0.54, N=16, p=0.03). Paliperidone Palmitate 245-265 prolactin Homo sapiens 44-53 18477617-8 2008 Of those atypicals that are associated with prolactin elevation, the main causative factor appears to be a higher peripheral-to-central dopamine receptor potency of either the parent drug or its active metabolite (e.g. risperidone, 9-hydroxy-risperidone and amisulpride). Paliperidone Palmitate 232-253 prolactin Homo sapiens 44-53 18058087-10 2008 CONCLUSIONS: The data from this study suggest that paliperidone ER at 6-9 mg provides an estimated level of dopamine D2 receptor occupancy between 70-80% and that the magnitude of dopamine D2 receptor occupancy is similar between the striatum and temporal cortex. Paliperidone Palmitate 51-63 dopamine receptor D2 Homo sapiens 108-128 17962372-4 2008 One drug and its metabolite, risperidone and 9-hydroxyrisperidone, of the 32 CNS compounds, and 6 of the 7 non-CNS drugs were determined to have positive efflux using ratio of ratios in MDR1-MDCK versus MDCK transwell assays. Paliperidone Palmitate 45-65 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 186-190 18053652-6 2008 CONCLUSIONS: These data suggest that risperidone"s effect on prolactin release is dose-dependent in adolescents and is linked to both plasma risperidone and 9-hydroxyrisperidone concentrations. Paliperidone Palmitate 157-177 prolactin Homo sapiens 61-70 18543120-4 2008 Furthermore, the brain entry of risperidone and 9-hydroxyrisperidone has been shown to be greatly limited by P-gp (Int J Neuropsychopharmacol 7:415-419, 2004). Paliperidone Palmitate 48-68 ATP binding cassette subfamily B member 1 Homo sapiens 109-113 17094165-5 2006 Morning serum samples for prolactin were analyzed and investigated in relation to the serum concentrations of risperidone and 9-hydroxyrisperidone. Paliperidone Palmitate 126-146 prolactin Homo sapiens 26-35 18004132-5 2007 The first-generation antipsychotics, as well as the second-generation antipsychotic risperidone and its active metabolite paliperidone, have been shown to cause marked and sustained elevations in prolactin levels, whereas others of the second-generation antipsychotics appear to have little or no effect on prolactin levels or may decrease prolactin. Paliperidone Palmitate 122-134 prolactin Homo sapiens 196-205 18004132-5 2007 The first-generation antipsychotics, as well as the second-generation antipsychotic risperidone and its active metabolite paliperidone, have been shown to cause marked and sustained elevations in prolactin levels, whereas others of the second-generation antipsychotics appear to have little or no effect on prolactin levels or may decrease prolactin. Paliperidone Palmitate 122-134 prolactin Homo sapiens 307-316 18004132-5 2007 The first-generation antipsychotics, as well as the second-generation antipsychotic risperidone and its active metabolite paliperidone, have been shown to cause marked and sustained elevations in prolactin levels, whereas others of the second-generation antipsychotics appear to have little or no effect on prolactin levels or may decrease prolactin. Paliperidone Palmitate 122-134 prolactin Homo sapiens 307-316 17715206-1 2007 The object of this study is to assess 1) the relationship between plasma antipsychotic drug concentration, serum prolactin levels and the clinical efficacy of risperidone, 2) the relationship between the CYP2D6 polymorphisms and metabolizing of risperidone and 3) the role of 9-hydroxyrisperidone in elevating prolactin levels. Paliperidone Palmitate 276-296 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 204-210 17541883-1 2007 Risperidone (R) is metabolized to 9-hydroxyrisperidone (9-OHR) by cytochrome P450 2D6 (CYP2D6). Paliperidone Palmitate 34-54 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 87-93 16936711-0 2007 Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Paliperidone Palmitate 16-28 ATP binding cassette subfamily B member 1 Homo sapiens 37-51 16936711-1 2007 Risperidone (RSP) and its major active metabolite, 9-hydroxy-risperidone (paliperidone, PALI), are substrates of the drug transporter P-glycoprotein (P-gp). Paliperidone Palmitate 51-72 ATP binding cassette subfamily B member 1 Homo sapiens 134-148 16936711-1 2007 Risperidone (RSP) and its major active metabolite, 9-hydroxy-risperidone (paliperidone, PALI), are substrates of the drug transporter P-glycoprotein (P-gp). Paliperidone Palmitate 51-72 ATP binding cassette subfamily B member 1 Homo sapiens 150-154 16936711-1 2007 Risperidone (RSP) and its major active metabolite, 9-hydroxy-risperidone (paliperidone, PALI), are substrates of the drug transporter P-glycoprotein (P-gp). Paliperidone Palmitate 74-86 ATP binding cassette subfamily B member 1 Homo sapiens 134-148 16936711-1 2007 Risperidone (RSP) and its major active metabolite, 9-hydroxy-risperidone (paliperidone, PALI), are substrates of the drug transporter P-glycoprotein (P-gp). Paliperidone Palmitate 74-86 ATP binding cassette subfamily B member 1 Homo sapiens 150-154 17094165-7 2006 Levels of prolactin were positively correlated to the 9-hydroxyrisperidone serum concentration (r(s) = 0.48, p = 0.03) and to the daily dose of risperidone (r(s) = 0.51, p = 0.03), but did not correlate to the risperidone serum concentration. Paliperidone Palmitate 54-74 prolactin Homo sapiens 10-19 17094165-8 2006 CONCLUSION: The present results suggest that 9-hydroxyrisperidone and not risperidone is the main contributor to the increased serum levels of prolactin observed in many risperidone-treated patients. Paliperidone Palmitate 45-65 prolactin Homo sapiens 143-152 16833023-8 2006 The CYP2D6*10 allele particularly was associated with higher serum concentrations of risperidone and the risperidone/9-OH-risperidone ratio compared with the CYP2D6*1 allele. Paliperidone Palmitate 117-133 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-10 16833023-10 2006 Furthermore, the pharmacokinetic parameters of risperidone and the risperidone/9-OH-risperidone ratio are highly dependent on the CYP2D6 genotypes. Paliperidone Palmitate 79-95 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 130-136 17054409-2 2006 The brain entry of risperidone and 9-OH-risperidone is greatly limited by P-glycoprotein, which implies that the functional polymorphisms of ABCB1 in humans may be a factor contributing to the variability in response to risperidone. Paliperidone Palmitate 35-51 ATP binding cassette subfamily B member 1 Homo sapiens 74-88 17054409-2 2006 The brain entry of risperidone and 9-OH-risperidone is greatly limited by P-glycoprotein, which implies that the functional polymorphisms of ABCB1 in humans may be a factor contributing to the variability in response to risperidone. Paliperidone Palmitate 35-51 ATP binding cassette subfamily B member 1 Homo sapiens 141-146