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Hoe 140 a new potentand long actingbradykinin‐antagonist: in vitro studies Franz J. HockKlaus WirthUdo Albus1991 год

Hoe 140 a new potent and long acting bradykinin‐antagonist: in vitro studies
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Аннотация: Hoe 140 ( d ‐Arg‐[Hyp 3 , Thi 5 , d ‐Tic 7 , Oic 8 ]bradykinin) is a new bradykinin (BK)‐antagonist. It was tested in several in vitro assays and compared with d ‐Arg‐[Hyp 2 , Thi 5,8 , d ‐Phe 7 ]BK. In receptor binding studies in guinea‐pig ileum preparations, Hoe 140 showed an IC 50 of 1.07 × 10 −9 mol l −1 and a K I value of 7.98 × 10 −10 mol l −1 . In isolated organ preparations Hoe 140 and d ‐Arg‐[Hyp 2 , Thi 5,8 , d ‐Phe 7 ]BK inhibited bradykinin‐induced contractions concentration dependently, with IC 50 ‐values in the guinea‐pig ileum preparation of 1.1 × 10 −8 mol l −1 and 3 × 10 −5 mol l −1 , respectively. pA 2 values in this tissue were 8.42 and 6.18, respectively. In the rat uterus preparation the IC 50 value was 4.9 × 10 −9 mol l −1 for Hoe 140. d ‐Arg‐[Hyp 2 , Thi 5,8 , d ‐Phe 7 ]BK showed an IC 50 of 4.0 × 10 −6 mol l −1 . The IC 50 values in the guinea‐pig isolated pulmonary artery were 5.4 × 10 −9 mol l −1 and 6.4 × 10 −6 mol l −1 , respectively. In the rabbit aorta no inhibitory effects on Des‐Arg 9 ‐BK induced contractions were observed. In cultured bovine endothelial cells, Hoe 140 antagonized (IC 50 = 10 −8 mol l −1 ) bradykinin‐induced endothelium‐derived relaxing factor (EDRF) release and the bradykinin‐induced increase in cytosolic free calcium (IC 50 = 10 −9 mol l −1 ). Hoe 140 (10 −7 mol l −1 ) totally suppressed the bradykinin‐induced (10 −8 to 10 −4 mol l −1 ) prostacyclin (PGI 2 ) release from cultured endothelial cells of bovine aorta. d ‐Arg‐[Hyp 2 , Thi 5,8 , d ‐Phe 7 ]BK (10 −7 mol l −1 ) showed a weaker antagonism. Taken together these results show that Hoe 140 is a highly potent bradykinin antagonist. It was two to three orders of magnitude more potent than d ‐Arg‐[Hyp 2 , Thi 5,8 , d ‐Phe 7 ]BK.
Год издания: 1991
Авторы: Franz J. Hock, Klaus Wirth, Udo Albus, Wolfgang Linz, H.J. Gerhards, Gabriele Wiemer, St. Henke, Gerhard Breipohl, Wilfried Α. König, Jochen Knolle, Bernward A. Schölkens
Издательство: Wiley
Источник: British Journal of Pharmacology
Ключевые слова: Coagulation, Bradykinin, Polyphosphates, and Angioedema, Nitric Oxide and Endothelin Effects, Cell Adhesion Molecules Research
Другие ссылки: British Journal of Pharmacology (PDF)
British Journal of Pharmacology (HTML)
Europe PMC (PubMed Central) (PDF)
Europe PMC (PubMed Central) (HTML)
PubMed Central (HTML)