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Titolo:
5-HT(3) RECEPTOR ANTAGONISM BY ANPIRTOLINE, A MIXED 5-HT(1) RECEPTOR AGONIST 5-HT(3) RECEPTOR ANTAGONIST
Autore:
GOTHERT M; HAMON M; BARANN M; BONISCH H; GOZLAN H; LAGUZZI R; METZENAUER P; NICKEL B; SZELENYI I;
Indirizzi:
UNIV BONN,INST PHARMACOL TOXICOL,REUTERSTR 2B D-53113 BONN GERMANY UNIV PARIS 06,INSERM,U288 F-75634 PARIS 13 FRANCE ASTA MEDICA AG,DEPT PHARMACOL D-60001 FRANKFURT GERMANY
Titolo Testata:
British Journal of Pharmacology
fascicolo: 2, volume: 114, anno: 1995,
pagine: 269 - 274
SICI:
0007-1188(1995)114:2<269:5RABAA>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
C-14 GUANIDINIUM; CEREBRAL-CORTEX; SMALL-INTESTINE; CANCER THERAPY; GUINEA-PIG; EMESIS; 5-HYDROXYTRYPTAMINE; CISPLATIN; RELEASE; CHANNEL;
Keywords:
ANPIRTOLINE; 5-HYDROXYTRYPTAMINE RECEPTORS; ANTIEMETIC EFFECT; DOMESTIC PIG; 5-HT3 RECEPTORS; [C-14] GUANIDINIUM INFLUX;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
35
Recensione:
Indirizzi per estratti:
Citazione:
M. Gothert et al., "5-HT(3) RECEPTOR ANTAGONISM BY ANPIRTOLINE, A MIXED 5-HT(1) RECEPTOR AGONIST 5-HT(3) RECEPTOR ANTAGONIST", British Journal of Pharmacology, 114(2), 1995, pp. 269-274

Abstract

1 The aim of this study was to provide evidence that anpirtoline, which is an agonist at 5-HT1B and 5-HT1D receptors and also displays submicromolar affinity for 5-HT1A recognition sites, in addition, acts as an antagonist at 5-HT3 receptors. 2 In radioligand binding studies on rat brain cortical membranes, anpirtoline inhibited specific binding of [H-3]-(S)-zacopride to 5-HT3 receptor recognition sites (pK(i): 7.53). 3 In NlE-115 neuroblastoma cells in which [C-14]-guanidinium was used as a tool to measure cation influx through the 5-HT3 receptor channel, the 5-HT-induced influx was concentration-dependently inhibited byanpirtoline. In this respect, anpirtoline mimicked other 5-HT3 receptor antagonists; the rank order of potency was ondansetron> anpirtoline> metoclopramide. 4 The concentration-response curve for 5-HT as a stimulator of [C-14]-guanidinium influx was shifted to the right by anpirtoline (apparent pA(2): 7.78), 5 In urethane-anaesthetized rats, anpirtoline inhibited (at lower potency than zacopride and tropisetron) the5-HT- or phenylbiguanide-induced bradycardia (Bezold-Jarisch reflex),but did not induce this reflex by itself. 6 Intravenous infusion of cisplatin in the domestic pig caused a consistent emetic response whichwas antagonized by anpirtoline. 7 It is concluded that anpirtoline, which was previously characterized as a 5-HT1 receptor agonist also proved to be a 5-HT3 receptor antagonist in several experimental models and, hence, exhibits a unique pattern of properties at different 5-HT receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/09/20 alle ore 05:07:26