Effect of YM087, a potent nonpeptide vasopressin antagonist, on vasopressin-induced hyperplasia and hypertrophy of cultured vascular smooth-muscle cells

Journal of Cardiovascular Pharmacology
Atsuo TaharaA Tanaka

Abstract

We investigated the effects of YM087, a potent nonpeptide V1A and V2 vasopressin (AVP)-receptor antagonist, in binding and functional studies on rat vascular smooth-muscle cells (VSMCs). V1A AVP receptors on VSMCs were characterized by using the radioligand [3H]AVP. Specific binding of [3H]AVP was time dependent, reversible, and saturable. A single class of high-affinity binding sites with the expected V1A profile was identified. YM087 showed high affinity for V1A receptors with an inhibitory dissociation constant (Ki) value of 0.24 nM. In addition, YM087 potently and concentration-dependently inhibited AVP-induced increase in intracellular free calcium concentration and activation of mitogen-activated protein kinase. When added to growth-arrested VSMCs, AVP concentration-dependently induced hyperplasia and hypertrophy. YM087 prevented AVP-induced hyperplasia and hypertrophy of these cells in a concentration-dependent manner. YM087 had no agonistic activity in any biological assays used. These results suggest that YM087 displays high affinity for V1A receptors on VSMCs and high potency in inhibiting the AVP-induced physiological response. YM087 is a potent pharmacologic probe for investigating the physiologic and pathophysiolog...Continue Reading

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Citations

Aug 26, 2006·Pediatric Cardiology·Brady S Moffett, Anthony C Chang
Jul 6, 2002·European Journal of Pharmacology·Junko TsukadaAkihiro Tanaka
Mar 18, 2000·European Journal of Pharmacology·Y NakamuraK Kikuchi
Dec 19, 2008·Cardiology in Review·Gerard Oghlakian, Marc Klapholz
Jan 8, 2008·Clinical and Experimental Pharmacology & Physiology·Atsuo TaharaMasayuki Shibasaki
Jan 8, 2010·Drug Design, Development and Therapy·Jalal K GhaliHammam D Zmily
Jul 11, 2009·Expert Opinion on Investigational Drugs·Raphaël FavoryJean-Louis Vincent
Aug 17, 2010·Drug Discovery Today·Punniyakoti T VeeraveeduKenichi Watanabe
Dec 1, 2009·Journal of Cardiothoracic and Vascular Anesthesia·Natalie F Holt, Kenneth L Haspel
Jan 30, 2004·Fundamental & Clinical Pharmacology·Jörn O StreefkerkPieter A Van Zwieten
Jan 22, 2005·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Atsuo TaharaMasayuki Shibasaki
Dec 19, 2006·Journal of the American College of Cardiology·Emil M deGomaEuan A Ashley
Aug 7, 2010·Congestive Heart Failure·Mitchell H Rosner, Claudio Ronco
Jul 16, 2013·Clinical Pharmacology and Therapeutics·T G von LuederH Krum

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