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Neurology

Addiction

Muscarinic acetylcholine receptor 5 (CHRM5; HM5)

In vitro studies identified HM5-selective antagonists that could help treat drug addiction. In mammalian cells expressing muscarinic acetylcholine receptors, a highly selective derivative of 1,2,5,6-tetrahydropyridine-3-carboxylic acid had 11-fold selectivity for HM5 over other muscarinic receptors. In striatal slices from wild-type rats, the compound inhibited dopamine release as effectively as genetic knockout of Hm5. Computational studies of the HM5 receptor identified the binding mode of the new compound. Next steps include testing the compound in animal models for drug abuse.

SciBX 6(9); doi:10.1038/scibx.2013.220
Published online March 7, 2013

Findings unpatented; unavailable for licensing

Zheng, G. et al. J. Med. Chem.; published online Feb. 4, 2013;
doi:10.1021/jm301774u
Contact: Guangrong Zheng, University of Arkansas for Medical Sciences,
Little Rock, Ark.
e-mail:

gzheng@uams.edu