Renal dopamine-1 receptor coupling with gs and gq/11 proteins in spontaneously hypertensive rats. Hussain, Tahir, and Mustafa F. Lokhandwala. Institute for Cardiovascular Studies, College of Pharmacy, University of Houston, Houston, TX 77204-5511 USA
APStracts 3:0216F, 1996.
Dopamine-1 (DA1) receptor transduces its signal via adenylyl cyclase and phospholipase C in the renal proximal tubules which has been suggested to be defective at the level of receptor-G protein coupling in spontaneously hypertensive rats (SHR). We prepared basolateral membranes from Wistar Kyoto (WKY) rats and SHR to determine the coupling of DA1 receptor with G-proteins, especially Gq/11. Fenoldopam, a DA1 receptor agonist, produced a time and concentration-dependent stimulation in [35S]GTP[gamma]S binding in WKY rats. Fenoldopam-induced (10 [mu]M) stimulation was significantly inhibited by a DA1 receptor antagonist, SCH 23390. Specific antibodies against C-terminals of Gs[alpha] and Gq/11[alpha] produced 50-60% and 40-50% inhibition respectively, in fenoldopam stimulation of [35S]GTP[gamma]S binding. Western analysis of basolateral membranes with these antibodies revealed the presence of Gs[alpha] (45 kDa) and Gq/11[alpha] (42 kDa). Fenoldopam stimulation of [35S]GTP[gamma]S binding was significantly attenuated in SHR compared to WKY rats. Parathyroid hormone stimulation of [35S]GTP[gamma]S binding was similar in SHR and WKY rats whereas, stimulation by phenylephrine was significantly reduced in SHR. Densitometric quantification of 42 kDa band showed a reduced amount in SHR while the density of 45 kDa band was not significantly different compared to WKY rats. We provide the direct evidence showing the coupling of DA1 receptor with Gq/11[alpha] and Gs[alpha] and propose that in addition to a defect in the receptor-G-protein coupling, a reduced amount of Gq/11[alpha] observed in the hypertensive animals may also contribute to the diminished dopamine-induced inhibition of Na&,K&-ATPase in SHR.

Received 15 August 1996; accepted in final form 14 November 1996.
APS Manuscript Number F237-6.
Article publication pending Am. J. Physiol. (Renal Fluid Electrolyte
Physiology).
ISSN 1080-4757 Copyright 1996 The American Physiological Society.
Published in APStracts on 31 December 1996