Muscarinic acetylcholine receptor binding affinities of pethidine analogs.
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).
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, United States.
Na-Ra
NR
Lee
Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, United States.
Xuan
X
Zhang
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, United States.
Mahesh
M
Darna
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, United States.
Linda P
LP
Dwoskin
Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, United States.
Guangrong
G
Zheng
D000818:Animals; D016466:CHO Cells; D003412:Cricetulus; D005260:Female; D006801:Humans; D008024:Ligands; D008614:Meperidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000378:metabolism; D043643:Receptor, Muscarinic M1 / Q000378:metabolism*; D043587:Receptor, Muscarinic M3 / Q000378:metabolism*; D043642:Receptor, Muscarinic M5 / Q000378:metabolism*; D013329:Structure-Activity Relationship
D008024:Ligands; D043643:Receptor, Muscarinic M1; D043587:Receptor, Muscarinic M3; D043642:Receptor, Muscarinic M5; D008614:Meperidine
Drug abuse; Muscarinic acetylcholine receptors; Pethidine; [(3)H]NMS binding affinity