The tachykinin NK1 receptor antagonist, RP67580, inhibits the bradykinin-induced rise in intracellular Ca2+ concentration in bovine pulmonary artery endothelial cells

European Journal of Pharmacology
J F Westra-De VliegerF P Nijkamp

Abstract

The bradykinin-induced rise in intracellular Ca2+ concentration ([Ca2+]i) and the bradykinin receptor involved in this response were characterized in bovine pulmonary artery endothelial cells. It was found that bradykinin induces an intracellular biphasic Ca2+ response, consisting of a transient peak followed by an elevated plateau phase. Both bradykinin and the bradykinin B1 receptor agonist, des-Arg9-bradykinin, induced a concentration-dependent increase in [Ca2+]i, but the bradykinin-induced rise was much greater. Moreover, the bradykinin-induced [Ca2+]i rise could be inhibited by the bradykinin B2 receptor antagonists, D-Arg0[Hyp3, Thi(5,8), D-Phe7]bradykinin and Hoe 140 (D-Arg[Hyp3, Thi5, D-Tic7, Oic8]bradykinin), but not by the bradykinin B1 receptor antagonist, des-Arg9-[Leu8]bradykinin. From these results it can be concluded that a bradykinin B2 receptor is involved in this response. Furthermore, we found that the tachykinin NK1 receptor antagonist, RP67580 ([imino 1 (methoxy-2-phenyl)-2 ethyl]-2 diphenyl 7,7 perhydroisoindolone-4 (3aR, 7aR)), and its negative enantiomer, RP68651 (2-[1-imino 2-(2 methoxy phenyl) ethyl] 7,7 diphenyl 4-perhydroisoindolone (3aS-7aS)), could inhibit the bradykinin-induced [Ca2+]i response, ...Continue Reading

References

Nov 1, 1992·Trends in Pharmacological Sciences·P A Revest, N J Abbott
Jan 1, 1992·Annual Review of Pharmacology and Toxicology·S G Farmer, R M Burch
Apr 1, 1992·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·F E Curry
Nov 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·C GarretP M Laduron
Oct 1, 1989·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·D J AdamsC Van Breemen
Oct 1, 1987·The American Journal of Physiology·R Morgan-BoydA Hassid
Mar 1, 1994·Trends in Pharmacological Sciences·C FasolatoT Pozzan
Mar 15, 1994·European Journal of Pharmacology·A Lombet, M Spedding
Aug 1, 1993·Canadian Journal of Physiology and Pharmacology·D RegoliN E Rhaleb
Mar 1, 1993·Pflügers Archiv : European journal of physiology·M GerickeB Nilius

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