PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 25794333-3 2015 Methylone has been assumed to induce hyperthermic effects through inhibition of serotonin and/or dopamine transporters (SERT and DAT, respectively). methylone 0-9 solute carrier family 6 (neurotransmitter transporter, serotonin), member 4 Mus musculus 120-124 33609514-6 2021 It was also observed an enantioselectivity in the binding to P-glycoprotein (P-gp), another efflux protein, being the R-(-)-pentedrone and S-(-)-methylone the most transported enantiomeric compounds. methylone 139-154 ATP binding cassette subfamily B member 1 Homo sapiens 61-75 33609514-6 2021 It was also observed an enantioselectivity in the binding to P-glycoprotein (P-gp), another efflux protein, being the R-(-)-pentedrone and S-(-)-methylone the most transported enantiomeric compounds. methylone 139-154 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 33609514-7 2021 These results were confirmed, in silico, by docking studies, revealing that R-(-)-pentedrone is the enantiomer with highest affinity to MRP1 and S-(-)-methylone and R-(-)-pentedrone are the enantiomers with highest affinity to P-gp. methylone 145-160 ATP binding cassette subfamily B member 1 Homo sapiens 227-231 33609514-8 2021 In conclusion, our data demonstrated that pentedrone and methylone present enantioselectivity in their cytotoxicity, which seems to involve, different oxidative reactivity as well as different affinity to the P-gp and MRP1 that together with GSH, play a protective role. methylone 57-66 ATP binding cassette subfamily B member 1 Homo sapiens 209-213 33609514-8 2021 In conclusion, our data demonstrated that pentedrone and methylone present enantioselectivity in their cytotoxicity, which seems to involve, different oxidative reactivity as well as different affinity to the P-gp and MRP1 that together with GSH, play a protective role. methylone 57-66 ATP binding cassette subfamily C member 1 Homo sapiens 218-222 31934604-9 2019 Tissue samples collected after treatment on the sixth week indicate that chronic exposure to methylone reduced UCP1 expression in SKM and BAT of the female rats. methylone 93-102 uncoupling protein 1 Rattus norvegicus 111-115 25794333-8 2015 Administration of the selective D1 receptor antagonist SCH 23390 and the D2 receptor antagonist raclopride reduced methylone-induced hyperthermia, but these drugs also had hypothermic effects in saline-treated mice, albeit to a smaller extent than the effects observed in methylone-treated mice. methylone 115-124 dopamine receptor D1 Mus musculus 32-43 25794333-8 2015 Administration of the selective D1 receptor antagonist SCH 23390 and the D2 receptor antagonist raclopride reduced methylone-induced hyperthermia, but these drugs also had hypothermic effects in saline-treated mice, albeit to a smaller extent than the effects observed in methylone-treated mice. methylone 115-124 dopamine receptor D2 Mus musculus 73-84 25794333-9 2015 In contradistinction to 3,4-methylenedioxymethamphetamine, which induces its toxicity through SERT and DAT, these data indicate that DAT, but not SERT, is strongly associated with the lethal toxicity produced by methylone, which did not seem to be dependent on the hyperthermic effects of methylone. methylone 212-221 solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 Mus musculus 133-136 25794333-3 2015 Methylone has been assumed to induce hyperthermic effects through inhibition of serotonin and/or dopamine transporters (SERT and DAT, respectively). methylone 0-9 solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 Mus musculus 129-132 25794333-9 2015 In contradistinction to 3,4-methylenedioxymethamphetamine, which induces its toxicity through SERT and DAT, these data indicate that DAT, but not SERT, is strongly associated with the lethal toxicity produced by methylone, which did not seem to be dependent on the hyperthermic effects of methylone. methylone 289-298 solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 Mus musculus 133-136 25794333-10 2015 DAT is therefore a strong candidate molecule for interventions aimed at preventing acute neurotoxic and lethal effects of methylone. methylone 122-131 solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 Mus musculus 0-3 25794333-7 2015 By contrast, only a slight diminution in the hyperthermic effects of methylone was observed in DAT KO mice, whereas a slight enhancement of these effects was observed in SERT KO mice. methylone 69-78 solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 Mus musculus 95-98 25626880-15 2015 Methylone (METHY) and mephedrone (MEPH; b), like METH, are substrates for the DAT but release DA from cytoplasmic pools selectively. methylone 0-9 solute carrier family 6 member 3 Homo sapiens 78-81 25626880-15 2015 Methylone (METHY) and mephedrone (MEPH; b), like METH, are substrates for the DAT but release DA from cytoplasmic pools selectively. methylone 11-16 solute carrier family 6 member 3 Homo sapiens 78-81 23099177-7 2013 Methylone had little effect on behavior or neurotransmitter levels in mice but produced a widespread depletion of 5-HT and 5-HTT levels in rats. methylone 0-9 huntingtin Mus musculus 125-128 23545806-7 2013 Additionally, a time-dependent loss of CYP2D6 activity was observed when the enzyme was preincubated with methylone, reaching a maximum rate of inactivation at high methylone concentrations, indicating that methylone is a mechanism-based inhibitor of CYP2D6. methylone 106-115 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 39-45 23545806-7 2013 Additionally, a time-dependent loss of CYP2D6 activity was observed when the enzyme was preincubated with methylone, reaching a maximum rate of inactivation at high methylone concentrations, indicating that methylone is a mechanism-based inhibitor of CYP2D6. methylone 106-115 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 251-257 23545806-7 2013 Additionally, a time-dependent loss of CYP2D6 activity was observed when the enzyme was preincubated with methylone, reaching a maximum rate of inactivation at high methylone concentrations, indicating that methylone is a mechanism-based inhibitor of CYP2D6. methylone 165-174 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 39-45 23545806-7 2013 Additionally, a time-dependent loss of CYP2D6 activity was observed when the enzyme was preincubated with methylone, reaching a maximum rate of inactivation at high methylone concentrations, indicating that methylone is a mechanism-based inhibitor of CYP2D6. methylone 165-174 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 251-257 23545806-3 2013 Using in vitro studies, CYP2D6 was determined to be the primary enzyme that metabolizes methylone, with minor contributions from CYP1A2, CYP2B6, and CYP2C19. methylone 88-97 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 24-30