HOE 140, a new highly potent and long-acting bradykinin antagonist in conscious rats. |
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| Authors: | G Bao F Qadri B Stauss H Stauss P Gohlke T Unger |
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| Affiliation: | Department of Pharmacology, University of Heidelberg, F.R.G. |
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| Abstract: | The inhibitory effects of the new bradykinin antagonist HOE 140 (D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg) on depressor responses to exogenous bradykinin were investigated in conscious rats and compared with those of the bradykinin antagonist B4146 (D-Arg-Hyp-Pro-Gly-Thi-Ser-D-Pro-Thi-Arg). HOE 140 showed a 250-700-fold higher potency in vivo and a much longer biological half-life than B4146. Plasma catecholamines were not increased after application of HOE 140, indicating that this compound did not interfere with catecholamine release. HOE 140 proved to be a highly potent, specific and long-acting bradykinin B2-receptor antagonist. |
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