Muscarinic acetylcholine receptor binding affinities of pethidine analogs

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

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • CHO Cells
  • Cricetulus
  • Female
  • Humans
  • Ligands
  • Meperidine / analogs & derivatives*
  • Meperidine / chemical synthesis*
  • Meperidine / metabolism
  • Receptor, Muscarinic M1 / metabolism*
  • Receptor, Muscarinic M3 / metabolism*
  • Receptor, Muscarinic M5 / metabolism*
  • Structure-Activity Relationship

Substances

  • Ligands
  • Receptor, Muscarinic M1
  • Receptor, Muscarinic M3
  • Receptor, Muscarinic M5
  • Meperidine