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).
|Number of pages||4|
|Journal||Bioorganic and Medicinal Chemistry Letters|
|State||Published - Nov 15 2015|
Bibliographical noteFunding Information:
This work was supported by funding from the National Institutes of Health ( DA030667 and UL1 TR000117 ).
© 2015 Elsevier Ltd. All rights reserved.
- Drug abuse
- Muscarinic acetylcholine receptors
- [H]NMS binding affinity
ASJC Scopus subject areas
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry