A novel bradykinin antagonist with improved properties.
Acylation of the N-terminus of [D-Arg0, Hyp3, Thi5,8, D-Phe7] bradykinin with 1-adamantanecarboxylic acid results in an analogue with enhanced potency of at least 33-fold. The new antagonist has potential as a pharmacological tool in the investigation of the role of endogenous bradykinin in cardiovascular regulation.
Department of Medicine, Thorndike Memorial Laboratory, Boston City Hospital, Massachusetts.
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Lammek
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Wang
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Gavras
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Gavras
D000218:Adamantane / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000595:Amino Acid Sequence; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001920:Bradykinin / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors* / Q000138:chemical synthesis / Q000494:pharmacology; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D008969:Molecular Sequence Data; D051381:Rats; D011919:Rats, Inbred Strains
C074544:bradykinin, 1-adamantanecarboxylic acid-Arg(0)-Hyp(3)-Thi(5,8)-Phe(7)-; D000218:Adamantane; D001920:Bradykinin