Involvement of α4β2 and α3β4 nicotinic receptor subtypes in alcohol taking and seeking

Preclinical and clinical evidence has indicated that nicotinic acetylcholine receptors (nAChRs) are important pharmacological targets for treatment of alcoholism. However, it is unclear which specific nAChR subtypes serve as mediators of the rewarding effects of alcohol due, in part, to the lack of potent and selective ligands for the different possible combinations of the subunits that compose nAChRs. Using combinatorial mixture libraries, Assuage Pharmaceuticals, in collaboration with Torrey Pines Institute for Molecular Studies has discovered high affinity nAChR antagonists with exquisite selectivity for α4β2 nAChRs over α3β4 nAChRs.

Source: Alcohol - May 1, 2017 Category: Addiction Authors: Andrea Cippitelli, Jinhua Wu, Ginamarie Debevec, Christopher Armishaw, Greg S. Welmaker, Marc Giulianotti, Lawrence Toll Source Type: research