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Titolo:
INHIBITION OF NEUROTRANSMITTER RELEASE FROM ENTERIC NERVE-ENDINGS BY L)-PHENETHYLAMINO]-5'-N-ETHYLCARBOXAMIDO-ADENOSINE (CGS-21680) AND RELATED ADENOSINE-ANALOGS - LACK OF SIMPLE COMPETITION BY ANTAGONISTS
Autore:
BROAD RM; COOK MA;
Indirizzi:
UNIV WESTERN ONTARIO,DEPT PHARMACOL & TOXICOL LONDON N6A 5C1 ONTARIO CANADA UNIV WESTERN ONTARIO,DEPT PHARMACOL & TOXICOL LONDON N6A 5C1 ONTARIO CANADA
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 2, volume: 266, anno: 1993,
pagine: 634 - 641
SICI:
0022-3565(1993)266:2<634:IONRFE>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG ILEUM; RECEPTOR AGONIST; ACETYLCHOLINE-RELEASE; MYENTERIC PLEXUS; RAT; ADENOSINE-A1-RECEPTORS; NUCLEOSIDES; NUCLEOTIDES; TRIAZOLOQUINAZOLINE; THEOPHYLLINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
37
Recensione:
Indirizzi per estratti:
Citazione:
R.M. Broad e M.A. Cook, "INHIBITION OF NEUROTRANSMITTER RELEASE FROM ENTERIC NERVE-ENDINGS BY L)-PHENETHYLAMINO]-5'-N-ETHYLCARBOXAMIDO-ADENOSINE (CGS-21680) AND RELATED ADENOSINE-ANALOGS - LACK OF SIMPLE COMPETITION BY ANTAGONISTS", The Journal of pharmacology and experimental therapeutics, 266(2), 1993, pp. 634-641

Abstract

Adenosine receptors on enteric nerves mediate inhibitory responses toadenosine and its analogs and contribute to the overall excitability of enteric nerves. In characterizing these receptors, the response of the electrically stimulated guinea pig ileum longitudinal muscle-myenteric plexus preparation to receptor-selective analogs of adenosine wasinvestigated and the antagonism of such activity by selective antagonists quantitated. The A1-selective agonist N6-cyclopentyladenosine, the nonselective agonist 5'-N-ethylcarboxamidoadenosine and the 2-substituted uronamides, yl)-phenethylaminol-5'-N-ethylcarboxamidoadenosine and orophenyl)-ethoxy]-5'-N-ethylcarboxamidoadenosine, both relatively A2-selective agonists, inhibited field-stimulated responses of the ileum with the potency rank order: N6-cyclopentyladenosine > 5'-N-ethylcarboxamidoadenosine much greater than yl)-phenethylamino]-5'-N-ethylcarboxamidoadenosine almost-equal-to orophenyl)-ethoxy]-5'-N-ethylcarboxamidoadenosine. Antagonism of these responses by receptor-selective antagonists was quantitated using the Schild technique and, for 1,3-dipropyl-8-cyclopentylxanthine, the A1-selective antagonist, demonstrated simple competitive interaction with the responses to N-cyclopentyladenosine yielding a linear Schild isobole with unit slope. In contrast, responses to the uronamides could not be antagonized in a simple competitive manner. The potency order of the selective agonists is compatiblewith the presence on enteric nerve endings of an Al receptor but doesnot support the presence of the A2 subtype. Moreover, these data demonstrate that the putatively A2-selective adenosine analogs yl)-phenethylamino]-5'-N-ethylcarboxamidoadenosine and uorophenyl)-ethoxy]-5'-N-ethylcarboxamidoadenosine interact with 1,3-dipropyl-8-cyclopentylxanthine at enteric nerve adenosine receptors in a manner which is not compatible with simple competitive interactions. These studies demonstratethat analogs of adenosine possessing the 5'-uronamide substituent behave as full agonists at the enteric neural adenosine A1 receptor but suggest that they act in a distinct way compared to the nonuronamide A1-selective agonists.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 02:00:32