rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M 2 -adrenoceptor antagonist and α 2 -adrenoceptor antagonist. rel-Delequamine has a pK i of 9.45 for α 2 -adrenoceptors in the rat cortex. rel-Delequamine augments K + -evoked release of noradrenaline with an EC 50 of 1 nM.
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