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The α1-adrenergic receptors are Gq protein-coupled receptors that play a key role in the modulation of sympathetic nervous system activity and are the site of action for therapeutic agents, such as antihypertensive drugs. A-61603 is a selective α1A-adrenergic receptor agonist that is at least 35-fold more potent at α1A receptor sites than at α1B or α1D.1 Activation of the α1A-adrenergic receptor by A-61603 has been reported to increase the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nM) much more potently than activation by phenylephrine (Item No. 17205; EC50 = 2.3 µM).2
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1. Synthesis and in vitro characterization of N-
2. Receptor subtype involved in α1-