bradykinin in rabbit aortae. Can. J. Physiol. Pharmacol. 55,[855][856][857][858][859][860][861][862][863][864][865][866][867] Rabbit aorta strips respond to bradykinin (BK) and to the C-terminal fragment of BK, the octapeptide 1-8 BK (Octa) with sustained contractions which are presumably due to the stimulation of specific receptors, because they remain unchanged in presence of phentolamine, methysergide, mepyramine, 8-Leu-AT,,, and indomethacin. Experimental dose-response curves of BK and Octa are very similar to the theoretical curves predicted by the mass-action law and show the classical hyperbolic shape; ratios of doses producing 16% and 84% of maximum effects are 1 :20 for Qcta and 1: 19 for BK. The relations of stinlulus and effect are linear, suggesting that the extents of the contractions are proportional to the number of receptors occupied by the agonists.Stnicture-activity studies performed with fragments and analogues of BK and with analogues of Qcta have shown that 8-Phe is essential for activation of the aortic receptor, and plays an important role for the affinity. The octapeptide 1-8 sequence is more favorable than the nonapeptide. because BK (pD2 = 6.40) is less potent than Octa (pDs = 7.19) and 9-Ala BK is a partial agonist.Antagonists for both Octa and BK have been found by replacing 8-Phe with aliphatic residues (Ala. Nle, Leu, Leu-OMe) in the octapeptide. Affinities of 8-Leu-Octa (PA, = 6.75) and 8-Leu-OMe-Qcta (PA? = 6-66) for the aortic receptors are fairly high and the antagonism appears to be of the competitive type because pA, -pAIo is close to 0.95 for both compounds.The inhibitory effect of these two compounds are specific for Qcta and BK. It is concluded that rabbit aortae contain a new type of receptor for BK, different from those found in the intestine and the uterus of several species. REC;OLI: D., BARABB, J. et PARK, W. K. 1977. Receptors for bradykinin in rabbit aortae. Can. J. Physiol. Pharniacol. 55. 855-867.Les bandelettes d'aorte de lapin rtpondent la bradykinine (BK) et au fragment Cterminal de la BK, l'octapeptide 1-8 BK (Octa) par des contractions soutenues qui sont apparemment dues B la stimulation de ricepteurs spkcifiques. En fait, ces contractions ne sont pas modifites par la phentolamine, la mithylsergide, la mCpyramine, la 8-Leu-AtII et l'indomtthacine. Les courbes dose-rCponse expkrimentales de la BK et de l'Octa sont tr&s semblables aux courbes thtoriques prtvues par la loi d'action de masse et on la forme hyperbolique classique; les rapports entre les doses produisant 16% et 84% de la contraction maximale correspondent A 1 :20 pour l'octa et 1 :9 pour la BK. Les relations stimuluseffet sont 1inCaires et ainsi suggerent que l'ttendue des contractions est proportionnelle au nombre relatif de rtcepteurs occup~s par les agonistes.Des ttudes de structure-activitt utilisant des fragments et analogues de la BK et des analogues de 1'Octa ont dCmontrt que la 8-Phe est essentielle pour l'activation du rtcepteur aortique et peut jouer un r61e important dans l'affiniti.. La ...