Effect of bradykinin analogues on the B1 receptor of rat ileum
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Gabriele Vietinghoff1, Enzo Hilscher, Inge Paegelow
1Centre of Pharmacology and Toxicology, Medical Faculty, University of Rostock, Schillingallee 70, D-18055 Rostock, Germany. gabriele.vietinghoff@med.uni-rostock.de
Abstract:
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.
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