119813-87-5

RS 15385-197 is a potent and selective alpha 2-adrenoceptor antagonist.

rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M2-adrenoceptor antagonist and α2-adrenoceptor antagonist. rel-Delequamine has a pKi of 9.45 for α2-adrenoceptors in the rat cortex. rel-Delequamine augments K+-evoked release of noradrenaline with an EC50 of 1 nM[1].

[1] Brown CM, et al. The pharmacology of RS-15385-197, a potent and selective alpha 2-adrenoceptor antagonist. Br J Pharmacol. 1993 Feb;108(2):516-25. DOI:10.1111/j.1476-5381.1993.tb12834.x
[2] Redfern WS, et al. Modulation of central noradrenergic function by RS-15385-197. Br J Pharmacol. 1993 Feb;108(2):526-33. DOI:10.1111/j.1476-5381.1993.tb12835.x