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Titolo:
BLOCKADE OF NICOTINIC RECEPTOR-MEDIATED RELEASE OF DOPAMINE FROM STRIATAL SYNAPTOSOMES BY CHLORISONDAMINE AND OTHER NICOTINIC ANTAGONISTS ADMINISTERED IN-VITRO
Autore:
ELBIZRI H; CLARKE PBS;
Indirizzi:
MCGILL UNIV,DEPT PHARMACOL & THERAPEUT,3655 DRUMMOND ST MONTREAL H3G 1Y6 PQ CANADA MCGILL UNIV,DEPT PHARMACOL & THERAPEUT MONTREAL H3G 1Y6 PQ CANADA
Titolo Testata:
British Journal of Pharmacology
fascicolo: 2, volume: 111, anno: 1994,
pagine: 406 - 413
SICI:
0007-1188(1994)111:2<406:BONRRO>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
H-3 DOPAMINE; RAT-BRAIN; BINDING-SITES; ACETYLCHOLINE; SYSTEM; DRUGS; MODULATION; SUBUNITS; AVERSION; SLICES;
Keywords:
NICOTINE; ACETYLCHOLINE; CYTISINE; DMPP; CHLORISONDAMINE; MECAMYLAMINE; DIHYDRO-BETA-ERYTHROIDINE; NICOTINIC RECEPTORS; CALCIUM DEPENDENCE; SURMOUNTABLE ANTAGONISM;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
55
Recensione:
Indirizzi per estratti:
Citazione:
H. Elbizri e P.B.S. Clarke, "BLOCKADE OF NICOTINIC RECEPTOR-MEDIATED RELEASE OF DOPAMINE FROM STRIATAL SYNAPTOSOMES BY CHLORISONDAMINE AND OTHER NICOTINIC ANTAGONISTS ADMINISTERED IN-VITRO", British Journal of Pharmacology, 111(2), 1994, pp. 406-413

Abstract

1 Central nicotinic receptor function examined in vitro, by measuringnicotine-induced [H-3]-dopamine release from rat striatal synaptosomes. 2 The agonists (-)-nicotine, acetylcholine, 1,1 -dimethyl-4-phenylpiperazinium (DMPP) and cytisine (10(-7)-10(-4) M) all increased [H-3]-dopamine release in a concentration-dependent manner. Cytisine did notproduce a full agonist response, compared to the other agonists. 3 The actions of nicotine, acetylcholine and cytisine were largely dependent on external Ca2+. In contrast, DMPP (10(-5) and 10(-4) M) evoked a marked release of [3(H)]-dopamine even in the absence of Ca2+. Nevertheless, in the presence of external Ca2+, responses to DMPP were completely blocked by the nicotinic antagonists chlorisondamine and mecamylamine (5 x 10(5) M); in the absence of external Ca2+, blockade was onlypartial. 4 Chlorisondamine, mecamylamine and dihydro-beta-erythroidine (10(-8)-10(-4) M) produced a concentration-dependent block of responses to nicotine (10(-6) M). Approximate IC50 values were 1.6, 0.3 and 0.2 x 10(-6), respectively. Chlorisondamine and mecamylamine blocked responses to nicotine (10(-7)-10(-4) M) insurmountably, whereas dihydro-beta-erythroidine behaved in a surmountable fashion. 5 The occurrenceof use-dependent block was tested by briefly pre-exposing the synaptosomes to nicotine during superfusion with antagonist, and determining the response to a subsequent nicotine application. Consistent with a possible channel blocking action, brief pre-exposure to agonist increased the antagonist potency of chlorisondamine (approximately 25 fold). No significant use-dependent block was detected with dihydro-beta-erythroidine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/07/20 alle ore 22:00:17