Oct 1, 2013
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Journal
The Journal of Pharmacology and Experimental Therapeutics
Abstract
NSC23766, an Inhibitor of Rac1, Also Acts as a Muscarinic Antagonist NSC23766 [(N-[2-[[4-(diethylamino)-1-methylbutyl]amino]6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride] is a widely used inhibitor of Rac1 activation. It is noteworthy that NSC23766 also created a rightward shift of the positive inotropic response curve caused by the cholinergic agonist, carbachol. In contrast, an adenosine A1 receptorinduced positive inotropic response in neonatal rat hearts was not changed by NSC23766. To investigate its specificity toward the different mAChR types, the carbachol-induced elevation in intracellular Ca concentrations in HEK-293 cells expressing M1, M2 or M3 mAChRs was investigated. NSC23766 caused a concentration-dependent rightward shift of the carbachol concentration response curves at all mAChRs. Thus, NSC23766 is not only an inhibitor of Rac1 activation but also is a competitive antagonist at mAChRs within the same concentration range.