PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 31782100-0 2020 OSU-6162, a Sigma1R Ligand in Low Doses, Can Further Increase the Effects of Cocaine Self-Administration on Accumbal D2R Heteroreceptor Complexes. OSU 6162 0-8 sigma non-opioid intracellular receptor 1 Rattus norvegicus 12-19 31782100-2 2020 It therefore becomes of interest to test if the monoamine stabilizer (-) OSU-6162 (OSU-6162) with a nanomolar affinity for the Sigma1R can acutely modulate in low doses the effects of cocaine self-administration. OSU 6162 73-81 sigma non-opioid intracellular receptor 1 Rattus norvegicus 127-134 31782100-2 2020 It therefore becomes of interest to test if the monoamine stabilizer (-) OSU-6162 (OSU-6162) with a nanomolar affinity for the Sigma1R can acutely modulate in low doses the effects of cocaine self-administration. OSU 6162 83-91 sigma non-opioid intracellular receptor 1 Rattus norvegicus 127-134 31782100-5 2020 In contrast, in maintenance of cocaine self-administration, the proximity ligation assay performed on brains from rats pretreated with OSU-6162 showed highly significant increases in the density of the D2R-Sigma1R heteroreceptor complexes in the shell of the nucleus accumbens versus OSU-6162 induced increases in this region of yoked saline rats. OSU 6162 135-143 sigma non-opioid intracellular receptor 1 Rattus norvegicus 206-213 31782100-5 2020 In contrast, in maintenance of cocaine self-administration, the proximity ligation assay performed on brains from rats pretreated with OSU-6162 showed highly significant increases in the density of the D2R-Sigma1R heteroreceptor complexes in the shell of the nucleus accumbens versus OSU-6162 induced increases in this region of yoked saline rats. OSU 6162 284-292 sigma non-opioid intracellular receptor 1 Rattus norvegicus 206-213 31782100-6 2020 In cocaine self-administration, highly significant increases were also induced by OSU-6162 in the A2AR-D2R heteroreceptor complexes in the nucleus accumbens shell versus vehicle-treated rats. OSU 6162 82-90 adenosine A2a receptor Rattus norvegicus 98-102 31782100-7 2020 Furthermore, ex vivo, the A2AR agonist CGS21680 (100 nM) produced a marked and significant increase of the D2R Ki high values in the OSU-6162-treated versus vehicle-treated rats under maintenance of cocaine self-administration. OSU 6162 133-141 adenosine A2a receptor Rattus norvegicus 26-30 31782100-9 2020 The current results indicate that OSU-6162 via its high affinity for the Sigma1R may increase the number of accumbal shell D2R-Sigma1R and A2AR-D2R heteroreceptor complexes associated with further increases in the antagonistic A2AR-D2R interactions in cocaine self-administration. OSU 6162 34-42 sigma non-opioid intracellular receptor 1 Rattus norvegicus 73-80 31782100-9 2020 The current results indicate that OSU-6162 via its high affinity for the Sigma1R may increase the number of accumbal shell D2R-Sigma1R and A2AR-D2R heteroreceptor complexes associated with further increases in the antagonistic A2AR-D2R interactions in cocaine self-administration. OSU 6162 34-42 sigma non-opioid intracellular receptor 1 Rattus norvegicus 127-134 31782100-9 2020 The current results indicate that OSU-6162 via its high affinity for the Sigma1R may increase the number of accumbal shell D2R-Sigma1R and A2AR-D2R heteroreceptor complexes associated with further increases in the antagonistic A2AR-D2R interactions in cocaine self-administration. OSU 6162 34-42 adenosine A2a receptor Rattus norvegicus 139-143 31782100-9 2020 The current results indicate that OSU-6162 via its high affinity for the Sigma1R may increase the number of accumbal shell D2R-Sigma1R and A2AR-D2R heteroreceptor complexes associated with further increases in the antagonistic A2AR-D2R interactions in cocaine self-administration. OSU 6162 34-42 adenosine A2a receptor Rattus norvegicus 227-231 20804495-0 2010 Analysis of the actions of the novel dopamine receptor-directed compounds (S)-OSU6162 and ACR16 at the D2 dopamine receptor. OSU 6162 78-85 dopamine receptor D2 Homo sapiens 103-123 22560595-0 2012 The dopaminergic stabilizer, (-)-OSU6162, rescues striatal neurons with normal and expanded polyglutamine chains in huntingtin protein from exposure to free radicals and mitochondrial toxins. OSU 6162 29-40 huntingtin Mus musculus 116-126 22560595-5 2012 We investigated the effects of (-)-OSU6162 on huntingtin knocked-in striatal neurons in culture. OSU 6162 31-42 huntingtin Mus musculus 46-56 22560595-12 2012 (-)-OSU6162 increases the intracellular levels of BDNF and Bcl2/Bax and decreases those of p-ERK/ERK and CHIP in Q111 cells. OSU 6162 4-11 brain derived neurotrophic factor Mus musculus 50-54 22560595-12 2012 (-)-OSU6162 increases the intracellular levels of BDNF and Bcl2/Bax and decreases those of p-ERK/ERK and CHIP in Q111 cells. OSU 6162 4-11 B cell leukemia/lymphoma 2 Mus musculus 59-63 22560595-12 2012 (-)-OSU6162 increases the intracellular levels of BDNF and Bcl2/Bax and decreases those of p-ERK/ERK and CHIP in Q111 cells. OSU 6162 4-11 BCL2-associated X protein Mus musculus 64-67 22560595-12 2012 (-)-OSU6162 increases the intracellular levels of BDNF and Bcl2/Bax and decreases those of p-ERK/ERK and CHIP in Q111 cells. OSU 6162 4-11 eukaryotic translation initiation factor 2 alpha kinase 3 Mus musculus 91-96 22560595-12 2012 (-)-OSU6162 increases the intracellular levels of BDNF and Bcl2/Bax and decreases those of p-ERK/ERK and CHIP in Q111 cells. OSU 6162 4-11 mitogen-activated protein kinase 1 Mus musculus 93-96 21866391-1 2011 In vitro evidence that (-)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors. OSU 6162 23-34 5-hydroxytryptamine receptor 2A Rattus norvegicus 92-98 21866391-1 2011 In vitro evidence that (-)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors. OSU 6162 39-50 5-hydroxytryptamine receptor 2A Rattus norvegicus 92-98 21866391-6 2011 Both enantiomers of OSU6162 were medium intrinsic activity partial agonists at 5-HT2A receptors and low intrinsic activity partial agonists at D2 receptors. OSU 6162 20-27 5-hydroxytryptamine receptor 2A Rattus norvegicus 79-85 21866391-7 2011 (+)-OSU6162 had higher efficacy at 5-HT2A receptors, which correlated with its greater stimulatory activity in vivo, but (-)-OSU6162 had higher potency at D2 receptors, which correlated with its greater inhibitory activity in vivo. OSU 6162 0-11 5-hydroxytryptamine receptor 2A Rattus norvegicus 35-41 21874578-1 2011 In vivo evidence for partial agonist effects of (-)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors. OSU 6162 48-59 5-hydroxytryptamine (serotonin) receptor 2A Mus musculus 79-85 21874578-1 2011 In vivo evidence for partial agonist effects of (-)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors. OSU 6162 64-75 5-hydroxytryptamine (serotonin) receptor 2A Mus musculus 79-85 21874578-13 2011 Overall, these results indicate that the dual effects on behavior of (-)- and (+)-OSU6162 are mediated through D2 and 5-HT2A receptors, consistent with their in vitro functional selectivity profiles (see Burstein et al., accompanying paper). OSU 6162 78-89 5-hydroxytryptamine (serotonin) receptor 2A Mus musculus 118-124 21533991-0 2011 Effects of the dopamine stabilizers (S)-(-)-OSU6162 and ACR16 on prolactin secretion in drug-naive and monoamine-depleted rats. OSU 6162 36-51 prolactin Rattus norvegicus 65-74 21533991-6 2011 We find that OSU6162 and ACR16 both stimulate prolactin secretion in drug-naive rats with OSU6162 being considerably more potent and efficacious. OSU 6162 13-20 prolactin Rattus norvegicus 46-55 19919834-0 2010 The dopaminergic stabilizers pridopidine (ACR16) and (-)-OSU6162 display dopamine D(2) receptor antagonism and fast receptor dissociation properties. OSU 6162 53-64 dopamine receptor D2 Homo sapiens 73-95 19919834-5 2010 In contrast to the high-affinity typical antipsychotics haloperidol and raclopride, the dopaminergic stabilizers ACR16 and (-)-OSU6162 both displayed fast dopamine D(2) receptor dissociation properties, a feature that has previously been suggested as a contributing factor to antipsychotic atypicality and attributed mainly to low receptor affinity. OSU 6162 123-134 dopamine receptor D2 Homo sapiens 155-177 11312565-2 2001 We studied the effects of coadministration of (-)-OSU6162 with l-DOPA on the regulation of striatal preproenkephalin (PPE) and prodynorphin (PDyn) mRNA expression in the primate brain by in situ hybridization histochemistry. OSU 6162 46-57 proenkephalin-B Callithrix jacchus 141-145 12433806-6 2002 quinidine, a CYP2D6-specific inhibitor, inhibited (-)-OSU6162 N-depropylation, whereas other p450 enzyme-specific substrates/inhibitors did not significantly inhibit this activity; 3). OSU 6162 50-61 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 13-19 12433806-8 2002 In addition, the selectivity of (-)-OSU6162 to inhibit six human p450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2E1, CYP2D6 and CYP3A4) was evaluated using an in vitro inhibition screen. OSU 6162 32-43 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 65-69 12433806-8 2002 In addition, the selectivity of (-)-OSU6162 to inhibit six human p450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2E1, CYP2D6 and CYP3A4) was evaluated using an in vitro inhibition screen. OSU 6162 32-43 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 79-85 12433806-8 2002 In addition, the selectivity of (-)-OSU6162 to inhibit six human p450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2E1, CYP2D6 and CYP3A4) was evaluated using an in vitro inhibition screen. OSU 6162 32-43 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 87-93 12433806-8 2002 In addition, the selectivity of (-)-OSU6162 to inhibit six human p450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2E1, CYP2D6 and CYP3A4) was evaluated using an in vitro inhibition screen. OSU 6162 32-43 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 95-102 12433806-8 2002 In addition, the selectivity of (-)-OSU6162 to inhibit six human p450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2E1, CYP2D6 and CYP3A4) was evaluated using an in vitro inhibition screen. OSU 6162 32-43 cytochrome P450 family 2 subfamily E member 1 Homo sapiens 104-110 12433806-8 2002 In addition, the selectivity of (-)-OSU6162 to inhibit six human p450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2E1, CYP2D6 and CYP3A4) was evaluated using an in vitro inhibition screen. OSU 6162 32-43 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 112-118 12433806-8 2002 In addition, the selectivity of (-)-OSU6162 to inhibit six human p450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2E1, CYP2D6 and CYP3A4) was evaluated using an in vitro inhibition screen. OSU 6162 32-43 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 123-129 12433806-9 2002 Of the enzymes examined, only the activity of CYP2D6 was inhibited by coincubation with (-)-OSU6162. OSU 6162 88-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 46-52 12433806-10 2002 Thus, it is concluded that (-)-OSU6162 is metabolized by several p450 enzymes and that CYP2D6 accounts for the majority of the observed p450 N-depropylase activity in vitro. OSU 6162 27-38 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 65-69 12433806-10 2002 Thus, it is concluded that (-)-OSU6162 is metabolized by several p450 enzymes and that CYP2D6 accounts for the majority of the observed p450 N-depropylase activity in vitro. OSU 6162 27-38 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 87-93 12433806-10 2002 Thus, it is concluded that (-)-OSU6162 is metabolized by several p450 enzymes and that CYP2D6 accounts for the majority of the observed p450 N-depropylase activity in vitro. OSU 6162 27-38 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 136-140 17157291-3 2007 We found that (-)-OSU6162 had a dissociation constant of 35 nM at the functional high-affinity site of the dopamine D2 receptor, stimulated the incorporation of [35S]-GTP-gamma-S above 100 nM, and inhibited the incorporating action of 1 microM dopamine with an inhibitory dissociation constant, Ki, of 27 nM, all being properties of a dopamine partial agonist. OSU 6162 14-25 dopamine receptor D2 Homo sapiens 107-127 12433806-1 2002 (S,S)-3-[3-(Methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride [(-)-OSU6162] is a weak dopamine D2 receptor modulator that possesses potential for the treatment of levodopa (L-DOPA)-induced dyskinesias in patients with Parkinson"s disease. OSU 6162 69-80 dopamine receptor D2 Homo sapiens 92-112 12433806-3 2002 Kinetics evidence is presented that the N-depropylation of (-)-OSU6162 in human hepatic microsomes is mediated by multiple cytochrome p450 (p450) enzymes, in particular CYP2D6. OSU 6162 59-70 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 134-138 12433806-3 2002 Kinetics evidence is presented that the N-depropylation of (-)-OSU6162 in human hepatic microsomes is mediated by multiple cytochrome p450 (p450) enzymes, in particular CYP2D6. OSU 6162 59-70 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 140-144 12433806-3 2002 Kinetics evidence is presented that the N-depropylation of (-)-OSU6162 in human hepatic microsomes is mediated by multiple cytochrome p450 (p450) enzymes, in particular CYP2D6. OSU 6162 59-70 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 169-175 12433806-5 2002 incubations of (-)-OSU6162 (5 micro M) with hepatic microsomes from a panel of human donors showed that (-)-OSU6162 N-depropylase activity correlated well with CYP2D6-catalyzed dextromethorphan O-demethylase activity but not with other p450 enzyme-specific activities; 2). OSU 6162 15-26 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 160-166 12433806-5 2002 incubations of (-)-OSU6162 (5 micro M) with hepatic microsomes from a panel of human donors showed that (-)-OSU6162 N-depropylase activity correlated well with CYP2D6-catalyzed dextromethorphan O-demethylase activity but not with other p450 enzyme-specific activities; 2). OSU 6162 15-26 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 236-240 11166288-1 2001 (S)-(-)-3-(3-(methylsulfonyl)phenyl)-1-propylpiperidine ((-)-OSU6162) is a phenylpiperidine derivative which exhibits low affinity to the dopamine D2 receptor in vitro. OSU 6162 57-68 dopamine receptor D2 Homo sapiens 138-158