HOE 140, a new highly potent and long-acting bradykinin antagonist in conscious rats.

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.

journal_name

Eur J Pharmacol

authors

Bao G,Qadri F,Stauss B,Stauss H,Gohlke P,Unger T

doi

10.1016/0014-2999(91)90684-i

subject

Has Abstract

pub_date

1991-07-23 00:00:00

pages

179-82

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(91)90684-I

journal_volume

200

pub_type

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