Bradykinin antagonists do not require a D-aromatic amino acid residue at position 7.
More than 200 new analogs of bradykinin have been synthesized and assayed. Analogs containing a D-aliphatic amino acid residue at position 7 and an L-aliphatic residue at position 8 are very potent antagonists of BK action on classical systems. Thus the "conventional wisdom" that a D-aromatic amino acid residue is required at sequence position 7 of BK antagonists must be modified.
Vavrek
R J
RJ
Department of Biochemistry, University of Colorado School of Medicine, Denver 80262.
Gera
L
L
Stewart
J M
JM
D000595:Amino Acid Sequence; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001920:Bradykinin / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors* / Q000737:chemistry; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008969:Molecular Sequence Data; D051381:Rats; D013329:Structure-Activity Relationship; D014599:Uterus / Q000187:drug effects
D001920:Bradykinin