Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptors

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dc.contributor.authorAcuña-Castillo, C
dc.contributor.authorVillalobos, C
dc.contributor.authorMoya, PR
dc.contributor.authorSáez, P
dc.contributor.authorCassels, BK
dc.contributor.authorHuidobro-Toro, J
dc.date.accessioned2025-01-21T01:30:25Z
dc.date.available2025-01-21T01:30:25Z
dc.date.issued2002
dc.description.abstract1 The pharmacological profile of a series of (+/-)-2,5-dimethoxy-4-(X)-phenylisopropylamines (X = I, Br, NO2, CH3, or H) and corresponding phenylethylamines, was determined in Xenopus laevis oocytes injected with cRNA coding for rat 5-HT2A or 5-HT2C receptors. The efficacy and relative potency of these drugs were determined and compared to classical 5-HT2 receptor agonists and antagonists.
dc.description.abstract2 The rank order of agonist potency at the 5-HT2A receptor was: alpha-methyl-5-HT = 5-HT > m- CPP>MK-212: at the 5-HT2C receptor the order was: 5-HT>alpha-methyl-5-HT>MK-212>m-CPP. All these compounds were full agonists at the 5-HT2C receptor, but alpha-methyl-5-HT and m-CPP showed lower efficacy at the 5-HT2A receptor.
dc.description.abstract3 4-(4-Fluorobenzoyl)-1-(4-phenylbutyl)piperidine (4F 4PP) was 200 times more potent as a 5-HT2A antagonist than at 5-HT2C receptors. Conversely, RS 102221 was 100 times more potent as a 5-HT2C antagonist, confirming their relative receptor selectivities.
dc.description.abstract4 The phenylisopropylamines were partial agonists at the 5-HT2A receptor, with I-max relative to 5-HT in the 22+/-7 to 58+/-15% range; the corresponding phenylethylamines had lower or undetectable efficacies. All these drugs had higher efficacies at 5-HT2C receptors; DOI was a full 5-HT2C agonist. 2C-I and the other phenylethylamines examined showed relative efficacies at the 5-HT2C receptor ranging from 44+/-10% to 76+/-16%. 1; 2C-N was a 5-HT2 receptor antagonist; the mechanism was competitive at the
dc.description.abstract5-HT2A, but noncompetitive at the 5-HT2C receptor. The antagonism was time-dependent at the 5-HT2C receptor but independent of pre-incubation time at the 5-HT2A receptor subtype. 6 The alpha-methyl group determines the efficacy of these phenylalkylamines at the 5-HT2A and 5-HT2C receptors.
dc.fuente.origenWOS
dc.identifier.issn0007-1188
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/96745
dc.identifier.wosidWOS:000176334200005
dc.issue.numero4
dc.language.isoen
dc.pagina.final519
dc.pagina.inicio510
dc.revistaBritish journal of pharmacology
dc.rightsacceso restringido
dc.subjecthallucinogenesis
dc.subjecthallucinogenic phenylalkylamines
dc.subject5-HT2A/2C receptors agonists/antagonists
dc.subject5-HT2 receptor subtype-selective
dc.subject5-HT2 partial agonist
dc.subjectphenylisopropylamines
dc.subjectphenylethylamines
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleDifferences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptors
dc.typeartículo
dc.volumen136
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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