Muscarinic acetylcholine receptor binding affinities of pethidine analogs

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

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

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 0.38 μM, respectively).

Original languageEnglish
Pages (from-to)5032-5035
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number22
DOIs
StatePublished - Nov 15 2015

Bibliographical note

Funding Information:
This work was supported by funding from the National Institutes of Health ( DA030667 and UL1 TR000117 ).

Publisher Copyright:
© 2015 Elsevier Ltd. All rights reserved.

Keywords

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

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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