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Titolo:
CHARACTERIZATION OF A CLONED HUMAN 5-HT1A RECEPTOR CELL-LINE USING [S-35] GTP-GAMMA-S BINDING
Autore:
STANTON JA; BEER MS;
Indirizzi:
MERCK SHARP & DOHME LTD,NEUROSCI RES CTR,TERLINGS PK,EASTWICK RD HARLOW CM20 2QR ESSEX ENGLAND MERCK SHARP & DOHME LTD,NEUROSCI RES CTR HARLOW CM20 2QR ESSEX ENGLAND
Titolo Testata:
European journal of pharmacology
fascicolo: 2-3, volume: 320, anno: 1997,
pagine: 267 - 275
SICI:
0014-2999(1997)320:2-3<267:COACH5>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
DORSAL RAPHE NEURONS; GAMMA-S BINDING; PARTIAL AGONISTS; PHARMACOLOGICAL CHARACTERIZATION; HUMAN 5-HT1A-RECEPTORS; ADENYLATE-CYCLASE; SEROTONIN 5-HT1A; ANTAGONIST; HIPPOCAMPAL; MEMBRANES;
Keywords:
[S-35] GTP-GAMMA-S BINDING ASSAY; 5-HT1A RECEPTOR, HUMAN; RECEPTOR RESERVE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
32
Recensione:
Indirizzi per estratti:
Citazione:
J.A. Stanton e M.S. Beer, "CHARACTERIZATION OF A CLONED HUMAN 5-HT1A RECEPTOR CELL-LINE USING [S-35] GTP-GAMMA-S BINDING", European journal of pharmacology, 320(2-3), 1997, pp. 267-275

Abstract

Compound potencies and efficacies depend upon receptor reserve and hence estimating this parameter in assay systems allows for a more meaningful interpretation of the data generated. This study describes a method whereby the degree of receptor reserve, with respect to 5-hydroxytryptamine (5-HT), was determined for a HeLa cell line expressing the human 5-HT1A receptor using the agonist-induced [S-35]guanosine 5'[gamma-thio]triphosphate ([S-35]GTP gamma S) binding assay, followed by a comparison of the potencies and relative efficacies of several compounds. Following irreversible antagonism with benextramine 5-HT yielded a pK(A) of 7.3, compared with a pK(obs) of 8.4 from saturation analysis,indicating the presence of high and low affinity state receptors. A 20% receptor occupancy elicited a half-maximal functional response consistent with the presence of receptor reserve. 5-HT, 5-carboxamidotryptamine (5-CT), 8-hydoxy-dipropylamino-tetralin (8-OH-DPAT), 5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1 H-indole (RU24969), buspirone, gepirone, mesulergine and sumatriptan were equally efficacious. ethoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine (NAN 190) displayed reduced relative efficacy and methiothepin inverse agonism.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/04/20 alle ore 03:14:41