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Titolo:
CHARACTERIZATION OF THE 5-HYDROXYTRYPTAMINE RECEPTOR-TYPE INVOLVED ININHIBITION OF SPONTANEOUS ACTIVITY OF HUMAN ISOLATED COLONIC CIRCULARMUSCLE
Autore:
TAM FSF; HILLIER K; BUNCE KT;
Indirizzi:
UNIV SOUTHAMPTON,FAC MED,CLIN PHARMACOL GRP SOUTHAMPTON SO9 3TU HANTSENGLAND UNIV SOUTHAMPTON,FAC MED,CLIN PHARMACOL GRP SOUTHAMPTON SO9 3TU HANTSENGLAND GLAXO GRP RES LTD,DEPT GASTROINTESTINAL PHARMACOL WARE HERTS ENGLAND
Titolo Testata:
British Journal of Pharmacology
fascicolo: 1, volume: 113, anno: 1994,
pagine: 143 - 150
SICI:
0007-1188(1994)113:1<143:COT5RI>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
CENTRAL NERVOUS-SYSTEM; ADENYLATE-CYCLASE; 5-HT RECEPTOR; PHARMACOLOGICAL CHARACTERIZATION; BENZAMIDE DERIVATIVES; SMOOTH-MUSCLE; PIG; RELAXATION; IDENTIFICATION; CONTRACTIONS;
Keywords:
5-HYDROXYTRYPTAMINE; HUMAN COLON; 5-HT4-LIKE RECEPTORS; PROKINETIC BENZAMIDES; TROPISETRON;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
35
Recensione:
Indirizzi per estratti:
Citazione:
F.S.F. Tam et al., "CHARACTERIZATION OF THE 5-HYDROXYTRYPTAMINE RECEPTOR-TYPE INVOLVED ININHIBITION OF SPONTANEOUS ACTIVITY OF HUMAN ISOLATED COLONIC CIRCULARMUSCLE", British Journal of Pharmacology, 113(1), 1994, pp. 143-150

Abstract

1 Experiments were carried out to characterize pharmacologically the 5-hydroxytryptamine (5-HT) receptor types which mediate inhibition of spontaneous contractions of the entertaining circular muscle in human isolated colon. 2 5-HT caused a reproducible concentration-dependent inhibition of spontaneous contractions of the circular muscle of human colon in vitro with a mean EC(50) value of 0.2 mu M and 95% confidencelimits of 0.1-0.5 mu M. NO evidence for a contractile action of 5-HT was found. Tetrodotoxin (TTX, 1.5 mu M) caused a rightward shift of the concentration-response curve of 5-HT with a concentration-ratio of 2.9. 3 The inhibitory response to 5-HT was mimicked by several indoles with the rank order of potency 5-HT > 5-methoxytryptamine = alpha-methyl-5-HT > 5-carboxamidotryptamine >> 2-methyl-5-HT. 5-Hydroxyindalpinewas inactive. 4 The substituted benzamides were agonists with the following rank order of potency, 5-HT > renzapride > zacopride > metoclopramide > cisapride. 5 The inhibitory responses to 5-HT were not inhibited by methysergide (10 mu M) or methiothepin (1 mu M), which are antagonists selective for 5-HT1-like and 5-HT2 receptors, nor by ondansetron (10 mu M) which is an antagonist at 5-HT3 receptors. 6 The inhibitory responses induced by 5-HT and 5-methoxytryptamine were competitively antagonized by a weak 5-HT4 receptor antagonist, tropisetron, with pK(B) values of approximately 6. Tropisetron had no significant effect on the inhibitory response curve produced by isoprenaline (0.01-100 muM). 7 The pharmacological profile of the 5-HT-evoked relaxations of human colon circular muscle are consistent with activation of a 5-HT4-like receptor.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/09/20 alle ore 10:50:05