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Titolo:
The interaction of antidepressant drugs with enteric 5-HT7 receptors
Autore:
Lucchelli, A; Santagostino-Barbone, MG; DAgostino, G; Masoero, E; Tonini, M;
Indirizzi:
Univ Pavia, Sch Pharm, Dept Expt & Appl Pharmacol, I-27100 Pavia, Italy Univ Pavia Pavia Italy I-27100 pt & Appl Pharmacol, I-27100 Pavia, Italy Univ Pavia, Dept Interal Med & Therapeut, Div Expt & Clin Pharmacol, I-27100 Pavia, Italy Univ Pavia Pavia Italy I-27100 pt & Clin Pharmacol, I-27100 Pavia, Italy
Titolo Testata:
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
fascicolo: 3, volume: 362, anno: 2000,
pagine: 284 - 289
SICI:
0028-1298(200009)362:3<284:TIOADW>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
SEROTONIN RECEPTOR; MOLECULAR-CLONING; MEDIATING RELAXATION; RAT HYPOTHALAMUS; SMOOTH-MUSCLE; BRAIN; EXPRESSION; JEJUNUM; SUBTYPE; ILEUM;
Keywords:
5-HT7 receptors; antidepressant drugs; amitriptyline; mianserin; maprotiline; imipramine; fluoxetine; flibanserin; guinea-pig ileum;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
25
Recensione:
Indirizzi per estratti:
Indirizzo: Lucchelli, A Univ Pavia, Sch Pharm, Dept Expt & Appl Pharmacol, Viale Taramelli 14, I-27100 Pavia, Italy Univ Pavia Viale Taramelli 14 Pavia Italy I-27100 via, Italy
Citazione:
A. Lucchelli et al., "The interaction of antidepressant drugs with enteric 5-HT7 receptors", N-S ARCH PH, 362(3), 2000, pp. 284-289

Abstract

In this study the functional interaction of the antidepressant drugs amitriptyline, mianserin, maprotiline, imipramine, fluoxetine and the putative antidepressant drug flibanserin has been studied on 5-HT7-mediated responsesto 5-carboxamidotryptamine (5-CT) in the guineapig ileum.5-CT induced a concentration-dependent inhibition of the contractile response to substance P (100 nM). Except for fluoxetine and flibanserin, all theantidepressants antagonized by different degrees the 5-CT inhibitory response with the following rank affinity order: mianserin > maprotiline greaterthan or equal to imipramine > amitriptyline. Mianserin was the only antidepressant to show a profile of competitive antagonism at 5-HT7 receptors in a tenfold range of concentrations (0.1-1 mu M), with an affinity (pA(2)) value of 8.1+/-0.6. The antagonism of the other antidepressants was not concentration-dependent (amitriptyline) or was associated with slight or moderate reduction of the maximal. 5-CT response (imipramine or maprotiline). The apparent affinity (pK(B)) values were: amitriptyline, 7.0+/-0.2; maprotiline, 7.3+/-0.6; imipramine, 7.2+/-0.4. Our results show that various antidepressant drugs belonging to different chemical classes behave as antagonists at enteric 5-HT7 receptors through competitive or allosteric mechanisms. This evidence extends our previous findings demonstrating the interaction of antidepressants with other 5-HT receptors, namely 5-HT3 and 5-HT4 receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 02:20:10