Characterization of the peripheral action of neurokinins and neurokinin receptor selective agonists on the rat cardiovascular system.

Naunyn-Schmiedeberg's Archives of Pharmacology
R CoutureD Regoli

Abstract

The effects on mean arterial pressure (MAP) and heart rate (HR) of increasing doses (0.65-65 nmol/kg) of substance P (SP), neurokinin A (NKA), neurokinin B (NKB) and selective agonists for neurokinin receptors were measured after intravenous (i.v.) injection in urethane anaesthetized rats. Neurokinins (NKs) elicited a vasodepressor effect with the following rank order of potency: SP (100%) greater than NKB (17.5%) greater than NKA (10%). The two undecapeptide NK-1 selective agonists, [Pro9, Met(O2)11]SP (787%) and [Sar9, Met(O2)11]SP (697%), evoked a significantly (P less than 0.05) greater vasodepressor response than SP, while the potency of the octapeptide NK-1 selective agonist [beta-Ala4, Sar9, Met(O2)11]SP (4-11) (316%) was not significantly different from SP. Conversely, the NK-2 selective agonist NKA (4-10) (less than 2%) caused only a small effect. The vasodepressor effect elicited by [MePhe7]NKB (112%) and [beta-Asp4, MePhe7]NKB (4-10) (92%), two NK-3 selective agonists, were not significantly different from that of SP. Senktide (1,095%) is the most potent NK-3 agonist, and is significantly (P less than 0.01) more potent than SP. No cross-desensitization, of the vasodepressor response, was observed between NK-1 and NK-...Continue Reading

Citations

Nov 12, 1991·European Journal of Pharmacology·P D'Orléans-JusteD Regoli
Mar 17, 1992·European Journal of Pharmacology·A Décarie, R Couture
Feb 16, 1993·European Journal of Pharmacology·S Lindberg, J Dolata
Jun 11, 1993·Regulatory Peptides·D RegoliN E Rhaleb
May 31, 2002·Autonomic Neuroscience : Basic & Clinical·John D Tompkins, John C Hancock
May 21, 2016·Clinical and Experimental Pharmacology & Physiology·Katarzyna KaczyńskaMałgorzata Szereda-Przestaszewska
Feb 1, 1993·Journal of Autonomic Pharmacology·C A MaggiA Giachetti
Oct 26, 2000·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·R V SchoborgJ C Hancock

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