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Titolo:
DIFFERENCES IN RESPONSE TO 5-HT4 RECEPTOR AGONISTS AND ANTAGONISTS OFTHE 5-HT4-LIKE RECEPTOR IN HUMAN COLON CIRCULAR SMOOTH-MUSCLE
Autore:
TAM FSF; HILLIER K; BUNCE KT; GROSSMAN C;
Indirizzi:
UNIV SOUTHAMPTON,FAC MED,CLIN PHARMACOL GRP SOUTHAMPTON SO16 7PX HANTS ENGLAND GLAXO GRP RES & DEV WARE HERTS ENGLAND
Titolo Testata:
British Journal of Pharmacology
fascicolo: 1, volume: 115, anno: 1995,
pagine: 172 - 176
SICI:
0007-1188(1995)115:1<172:DIRT5R>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG ILEUM; TUNICA MUSCULARIS MUCOSAE; CENTRAL NERVOUS-SYSTEM; BENZIMIDAZOLONE DERIVATIVES; ADENYLATE-CYCLASE; RAT ESOPHAGUS; RIGHT ATRIUM; 5-HYDROXYTRYPTAMINE; CONTRACTIONS; SDZ-205-557;
Keywords:
DAU 6285; GR 113808; 5-HT4-LIKE RECEPTORS; HUMAN COLON; SDZ 205-557; BENZIMIDAZOLES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
30
Recensione:
Indirizzi per estratti:
Citazione:
F.S.F. Tam et al., "DIFFERENCES IN RESPONSE TO 5-HT4 RECEPTOR AGONISTS AND ANTAGONISTS OFTHE 5-HT4-LIKE RECEPTOR IN HUMAN COLON CIRCULAR SMOOTH-MUSCLE", British Journal of Pharmacology, 115(1), 1995, pp. 172-176

Abstract

1 In isolated circular smooth muscle strips of human colon 5-hydroxytryptamine (5-HT) produced a concentration-related inhibition of spontaneous motility. 2 The azabicycloalkyl benzimidazolones, BIMU 8 and BIMU 1, which have 5-HT4 receptor stimulant properties, inhibited motility with EC(50) values of 0.76 mu M and 3.19 mu M respectively and theirE(max) values were not significantly different from 5-HT (EC(50), 0.13 mu M). 3 The 5-HT4 receptor antagonist, DAU 6285 (1-10 mu M), displaced the 5-HT concentration-response curve to the right in a parallel concentration-dependent manner without depressing the maximum. The Schild plot was linear and the slope did not differ significantly from unity giving a pA(2) value of 6.32. 4 The high affinity selective 5-HT4 receptor antagonist, GR 113808, at a concentration of 3 nM displaced the 5-HT concentration-response curve in a parallel manner giving an apparent pK(B) estimate of 8.9 +/- 0.24. However, higher concentrations of 10-100 nM GR 113808 did not result in a further significant displacement of the 5-HT concentration-response curve and there was no suppression of E(max). 5 GR 113808 (10 nM) also caused a parallel displacement of the concentration-response curve to the 5-HT4 receptor agonist, 5-methoxytryptamine (5-MeOT) giving apparent pK(B) values ranging from 8.3-9.3. 6 GR 113808 (3-100 nM) failed to displace 5-HT or 5-MeOT concentration-response curves in tissue strips from 3 patients out of a total of 10 patients studied in whom the response to 5-HT and 5-MeOT wasnormal. 7 The 5-HT4 receptor antagonist, SDZ 205-557 (0.3-10 mu M), had no significant effect on 5-HT-induced inhibition of spontaneous motility. 8 The present results are discussed in the light of variabilityof response to GR 113808 and SDZ 205-557 in other tissues. 9 Overall,our data indicate that human colon circular smooth muscle can be regarded as a site in which 5-HT4-like receptors are present but it is as yet unclear whether these results are also an indication of receptor variation.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/09/20 alle ore 10:42:01