Muscarinic acetylcholine receptor binding affinities of pethidine analogs

作者：Lee Na Ra; Zhang Xuan; Darna Mahesh; Dwoskin Linda P; Zheng Guangrong^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(22): 5032-5035.

DOI：10.1016/j.bmcl.2015.10.029

• Pethidine
• Muscarinic acetylcholine receptors
• [H-3]NMS binding affinity
• Drug abuse

A series of pethidine analogs were synthesized and their affinities for the [H-3]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs) were determined using M-1, M-3 or M-5 human mAChRs expressed by Chinese hamster ovary (CHO) cell membranes. Compound 6b showed the highest binding affinities at M-1, M-3 and M-5 mAChRs (K-i = 0.67, 0.37, and 0.38 mu M, respectively).

• 出版日期2015-11-15