Regulatory Peptides, 45 (1993) 323-340 323 © 1993 Elsevier Science Publishers B.V. All rights reserved 0167-0115/93/$06.00 REGPEP 01378 Review Vasoactive peptides and characterization of their receptors D. Regoli, P. D'Orlrans-Juste, N. Rouissi and N.E. Rhaleb Department of Pharmacology, Medical School, Universit~de Sherbrooke, Sherbrooke (Canada) (Received 23 January 1993; revised version received 7 February 1993; accepted 9 February 1993) Key words: Vasoactive peptide; Receptor; Characterization; Pharmacology; Review Contents I. II. III. IV. V. References Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 323 Receptors for angiotensin . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 326 Receptors for kinins . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 329 Receptors for neurokinins . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 331 Receptors for endothelins . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 333 . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 336 I. Introduction A variety of peptides take part in the modulation of peripheral vascular tone, which is primarily con- trolled by the sympathetic nervous system. Table I gives an overview of the 15eptides and their receptors. Noteworthy is the fact that each vasoactive endog- enous agent has at least two binding and one or more Correspondence to: D. Regoli, Department of Pharmacology, Med- ical School, Universit6 de Sherbrooke, Sherbrooke, Qurbec, J1H 5N4, Canada. functional sites. Such a complexity is quite common in physiology. The content of the present review will be limited to analysis of receptors for angiotensins, bradykinin and related kinins, substance P and related neuro- kinins and endothelins. For all these peptides (see Table II), data obtained in pharmacological studies have been confirmed by the identification (with mo- lecular biology techniques) of receptor genes and messenger mRNAs, as well as by the discovery of specific and selective antagonists of peptide or non- peptide nature. Receptors for vasoactive peptides are found in dif-