Muscarinic acetylcholine receptor binding affinities of pethidine analogs

[Display omitted] A series of pethidine analogs were synthesized and their affinities for the [3H]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 6...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-11, Vol.25 (22), p.5032-5035
Hauptverfasser:	Lee, Na-Ra, Zhang, Xuan, Darna, Mahesh, Dwoskin, Linda P., Zheng, Guangrong
Format:	Artikel
Sprache:	eng
Schlagworte:	[3H]NMS binding affinity Animals CHO Cells Cricetulus Drug abuse Female Humans Ligands Meperidine - analogs & derivatives Meperidine - chemical synthesis Meperidine - metabolism Muscarinic acetylcholine receptors Pethidine Receptor, Muscarinic M1 - metabolism Receptor, Muscarinic M3 - metabolism Receptor, Muscarinic M5 - metabolism Structure-Activity Relationship
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Zusammenfassung:	[Display omitted] A series of pethidine analogs were synthesized and their affinities for the [3H]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 0.38μM, respectively).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2015.10.029