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).


Lee, Na-Ra; Zhang, Xuan; Darna, Mahesh; Dwoskin, Linda P; Zheng, Guangrong;

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