Effect of bradykinin analogues on the B1 receptor of rat ileum.
The longitudinal muscle of isolated rat ileum is a sensitive bioassay suitable for testing compounds with antagonistic effects on the B(1) receptor. Bradykinin analogues with replacement of proline by alkyl-substituted phenylalanine at position 7 are effective on this receptor as entire molecules and have a stronger antagonistic effect than on the B(2) receptor. A corresponding desArg(9)-compound has a specific effect on the B(1) receptor and a very high antagonistic potency. [LNMPhe(2)]bradykinin as a compound without any replacement at position 7 or 8 shows antagonistic activity as well.
Vietinghoff
Gabriele
G
Centre of Pharmacology and Toxicology, Medical Faculty, University of Rostock, Schillingallee 70, D-18055 Rostock, Germany. gabriele.vietinghoff@med.uni-rostock.de
Hilscher
Enzo
E
Paegelow
Inge
I
Reissmann
Siegmund
S
D000818:Animals; D001920:Bradykinin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D065169:Bradykinin B1 Receptor Antagonists; D005260:Female; D007082:Ileum / Q000187:drug effects* / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology; D051381:Rats; D017208:Rats, Wistar; D043783:Receptor, Bradykinin B1 / Q000378:metabolism
D065169:Bradykinin B1 Receptor Antagonists; D043783:Receptor, Bradykinin B1; D001920:Bradykinin