Article
Exploring the determinants of trace amine-associated receptor 1's functional selectivity for the stereoisomers of amphetamine and methamphetamine.
Journal of medicinal chemistry - 23 Jan 2014
Reese Edmund A, Norimatsu Yohei, Grandy Madeline S, Suchland Katherine L, Bunzow James R, Grandy David K
Abstract excerpt
Amphetamines are widely abused drugs that interfere with dopamine transport and storage. Recently, however, another mechanism of action was identified: stereoselective activation of the GαS protein-coupled trace amine-associated receptor 1 (TAAR1). To identify structural determinants of this stereoselectivity, we functionally evaluated six mutant receptors in vitro and then used homology modeling and dynamic...
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