Vascular alpha1-adrenoceptor subtype selectivity and alpha1-blocker-induced orthostatic hypotension

Japanese Journal of Pharmacology
H TakeGozoh Tsujimoto

Abstract

Newly developed alpha1-adrenoceptor antagonists including naftopidil are free from the "prazosin-like" side effect of orthostatic hypotension and associated symptoms. We investigated the mechanism for the differential effects of naftopidil and prazosin on the development of postural hypotension, with special attention on their selectivity for the alpha1-adrenoceptor subtype. We observed that head-up tilt caused a similar extent of drop in mean arterial pressure in control, naftopidil (1 mg/kg)- or prazosin (10 microg/kg)-treated rats; however, the tilt-induced postural hypotension was recovered within 2 min in the naftopidil-treated group, but not in the prazosin-treated group. Comparing an inhibitory effect on noradrenaline-induced contraction in the rat aorta and portal vein, we found that naftopidil was sixfold less potent in the portal vein, while prazosin showed similar potency in both tissues. Reverse transcription-polymerase chain reaction analysis showed that the expression of alpha1d-adrenoceptor mRNA predominated in the aorta, while that of alpha1b-adrenoceptor mRNA predominated in the portal vein. Using cloned rat alpha1-adrenoceptor subtypes, we found that naftopidil was selective for the alpha1d-subtype with approx...Continue Reading

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Citations

Jul 19, 2017·Pflügers Archiv : European journal of physiology·Toshio Kitazawa, Kazuyo Kitazawa
Oct 21, 2000·Hypertension·R E ShapiroD E Berkowitz
Mar 7, 2006·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Yoshitaka TomiyamaNobuo Shibata
Dec 12, 2012·Asian Journal of Andrology·Hui DingZhi-Ping Wang
Jan 24, 2002·The Journal of Pharmacology and Experimental Therapeutics·Arthur A HancockMichael Williams
Jul 31, 2020·International Journal of Molecular Sciences·Romane FlorentMonique N'Diaye
Mar 1, 2008·Current Protocols in Pharmacology·Philippe GuillaumePierre Lacroix

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