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Titolo:
Role of peptidase and cyclooxygenase inhibitors in the guinea-pig bronchial response to the synthetic endothelin ETB agonist IRL 1620 and antagonist BQ-788
Autore:
Lazzeri, N; Nieri, P; Lenzi, P; Ratti, C; Breschi, MC;
Indirizzi:
Univ Pisa, Dept Psychiat Neurobiol Pharmacol & Biotechnol, I-56126 Pisa, Italy Univ Pisa Pisa Italy I-56126 Pharmacol & Biotechnol, I-56126 Pisa, Italy Univ Pisa, Dept Human Morphol & Appl Biol, I-56126 Pisa, Italy Univ Pisa Pisa Italy I-56126 an Morphol & Appl Biol, I-56126 Pisa, Italy
Titolo Testata:
JOURNAL OF AUTONOMIC PHARMACOLOGY
fascicolo: 4, volume: 19, anno: 1999,
pagine: 201 - 207
SICI:
0144-1795(199908)19:4<201:ROPACI>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
ET(B) RECEPTORS; SMOOTH-MUSCLE; IRL-1620; SUBTYPES; ILEUM; CONTRACTIONS; PD-145065; AIRWAYS; POTENT; ET(A);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
23
Recensione:
Indirizzi per estratti:
Indirizzo: Breschi, MC Univ Pisa, Dept Psychiat Neurobiol Pharmacol & Biotechnol, ViaBonanno 6, I-56126 Pisa, Italy Univ Pisa Via Bonanno 6 Pisa Italy I-56126-56126 Pisa, Italy
Citazione:
N. Lazzeri et al., "Role of peptidase and cyclooxygenase inhibitors in the guinea-pig bronchial response to the synthetic endothelin ETB agonist IRL 1620 and antagonist BQ-788", J AUT PHARM, 19(4), 1999, pp. 201-207

Abstract

1 In isolated guinea-pig bronchial preparations the selective endothelin ETB agonist, IRL 1620 caused a concentration-dependent contraction. The pD(2) value (7.16 +/- 0.09, n = 6) was significantly increased in the presence of peptidase inhibitors (thiorfan 1 mu M, captopril 1 mu M, bestatin 1 mu M) (pD(2) = 7.75 +/- 0.09, n = 6). Indomethacin (5 mu M) did not appear to influence the ETB-agonist pD(2) value (6.92 + 0.11, n = 6) but potentiated its maximal response significantly (67.23 +/- 4.81% vs. 53.37 +/- 4.80%).2 The concentration-response curve for the contractile response to IRL 1620 (pD(2) = 7.83 +/- 0.01, (n) under bar = 16); was reproducible, although not completely, since the second curve to this selective ETB agonist was shifted significantly to the right (pD(2) = 7.34 +/- 0.09, n = 16) and a decrease in the maximal response was observed (20.0 +/- 2.0%).3 BQ 788, a selective antagonist for ETB receptors, employed in concentrations ranging from 1.5 to 150 nM, caused a dose-dependent shift to the rightof the concentration-response curve to IRL 1620, with a pIC(50) value of 8.11 +/- 0.03; this action was not influenced by adding enzyme inhibitors (pIC(50) = 8.17 +/- 0.29).4 Our data show that IRL 1620 undergoes a hydrolytic metabolism in guinea-pig bronchial preparations, which could influence the calculation of the pD(2). Pretreatment of the tissue with peptidase inhibitors and indomethacin is consequently significant in the evaluation of IRL 1620 activity, while it does not influence the action of the antagonist, BQ 788.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/07/20 alle ore 04:51:35