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.

• Authors: G Bao, F Qadri, B Stauss, H Stauss, P Gohlke, T Unger
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 200 Issue 1 Pg. 179-82 (Jul 23 1991) ISSN: 0014-2999 [Print] Netherlands
• PMID: 1769370 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Catecholamines
• Fluoroacetates
• Oligopeptides
• B 4146
• icatibant
• Bradykinin

Topics

• Amino Acid Sequence
• Animals
• Bradykinin (administration & dosage, analogs & derivatives, antagonists & inhibitors, pharmacokinetics, pharmacology)
• Catecholamines (blood)
• Fluoroacetates
• Half-Life
• Male
• Molecular Sequence Data
• Oligopeptides (pharmacokinetics, pharmacology)
• Rats
• Rats, Inbred Strains