HOE 140, a new highly potent and long-acting bradykinin antagonist in conscious rats.
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.
Bao
G
G
Department of Pharmacology, University of Heidelberg, F.R.G.
Qadri
F
F
Stauss
B
B
Stauss
H
H
Gohlke
P
P
Unger
T
T
D000595:Amino Acid Sequence; D000818:Animals; D001920:Bradykinin / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors* / Q000493:pharmacokinetics / Q000494:pharmacology; D002395:Catecholamines / Q000097:blood; D005463:Fluoroacetates; D006207:Half-Life; D008297:Male; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
D002395:Catecholamines; D005463:Fluoroacetates; D009842:Oligopeptides; C050396:B 4146; C065679:icatibant; D001920:Bradykinin