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RS 100329 hydrochloride
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Sold with the permission of Roche Bioscience
Chemical Name:5-Methyl-3-[3-[3-[4-[2-(2,2,2,-trifluroethoxy)phenyl]-1
-piperazinyl]propyl]-2,4-(1H,3H)-pyrimidinedione
hydrochloride
Biological Activity:
Subtype selective α1A-adrenoceptor antagonist
(pKi = 9.6 for human cloned α1A receptors). Displays
126- and 50-fold selectivity over human α1B andα1D receptors respectively.
Active in vivo.
Shannon Kava et al (1998) α1L-Adrenoceptor mediation of smooth muscle contraction in rabbit
bladder neck: a model for lower urinary tract tissues of man. Br.J.Pharmacol. 123
1359. Williamset al (1999) In vitro α1-adrenoceptor
pharmacology of Ro 70-0004 and RS-100329, novel α1A-adrenoceptor selective antagonists.
Br.J.Pharmacol. 127 252. Conleyet al (2001) The
role of α1-adrenoceptors and 5-HT1A receptors in the control
of the micturition reflex in male anaesthetized rats. Br.J.Pharmacol. 133
61.
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