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Bioorg Med Chem Lett. 2015 Nov 15;25(22):5032-5. doi: 10.1016/j.bmcl.2015.10.029. Epub 2015 Oct 19.

Muscarinic acetylcholine receptor binding affinities of pethidine analogs.

Author information

1
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, United States.
2
Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, United States.

Abstract

A series of pethidine analogs were synthesized and their affinities for the [(3)H]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs) were determined using M1, M3 or M5 human mAChRs expressed by Chinese hamster ovary (CHO) cell membranes. Compound 6b showed the highest binding affinities at M1, M3 and M5 mAChRs (Ki=0.67, 0.37, and 0.38 μM, respectively).

KEYWORDS:

Drug abuse; Muscarinic acetylcholine receptors; Pethidine; [(3)H]NMS binding affinity

PMID:
26494260
PMCID:
PMC4629469
DOI:
10.1016/j.bmcl.2015.10.029
[Indexed for MEDLINE]
Free PMC Article

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