Muscarinic acetylcholine receptor binding affinities of pethidine analogs

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

doi:10.1016/j.bmcl.2015.10.029

Muscarinic acetylcholine receptor binding affinities of pethidine analogs

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

Research output: Contribution to journal › Article › peer-review

4 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 (K_i = 0.67, 0.37, and 0.38 μM, respectively).

Original language	English
Pages (from-to)	5032-5035
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2015.10.029
State	Published - Nov 15 2015

Bibliographical note

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

Funding

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

Funders	Funder number
National Institutes of Health (NIH)	DA030667
National Center for Advancing Translational Sciences (NCATS)	UL1TR000117

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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2015.10.029

Cite this

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title = "Muscarinic acetylcholine receptor binding affinities of pethidine analogs",

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).",

keywords = "Drug abuse, Muscarinic acetylcholine receptors, Pethidine, [H]NMS binding affinity",

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doi = "10.1016/j.bmcl.2015.10.029",

language = "English",

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T1 - Muscarinic acetylcholine receptor binding affinities of pethidine analogs

AU - Lee, Na Ra

AU - Zhang, Xuan

AU - Darna, Mahesh

AU - Dwoskin, Linda P.

AU - Zheng, Guangrong

PY - 2015/11/15

Y1 - 2015/11/15

N2 - 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).

AB - 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).

KW - Drug abuse

KW - Muscarinic acetylcholine receptors

KW - Pethidine

KW - [H]NMS binding affinity

UR - https://www.scopus.com/pages/publications/84945968249

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DO - 10.1016/j.bmcl.2015.10.029

M3 - Article

C2 - 26494260

AN - SCOPUS:84945968249

SN - 0960-894X

VL - 25

SP - 5032

EP - 5035

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 22

ER -

Muscarinic acetylcholine receptor binding affinities of pethidine analogs

Abstract

Bibliographical note

Funding

Keywords

ASJC Scopus subject areas

UN SDGs

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