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

Producción científica: Article › revisión exhaustiva

4 Citas (Scopus)

Resumen

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).

Idioma original	English
Páginas (desde-hasta)	5032-5035
Número de páginas	4
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	25
N.º	22
DOI	https://doi.org/10.1016/j.bmcl.2015.10.029
Estado	Published - nov 15 2015

Nota bibliográfica

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

Financiación

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

Financiadores	Número del financiador
National Institutes of Health (NIH)	DA030667
National Center for Advancing Translational Sciences (NCATS)	UL1TR000117

ASJC Scopus subject areas

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

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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",

author = "Lee, \{Na Ra\} and Xuan Zhang and Mahesh Darna and Dwoskin, \{Linda P.\} and Guangrong Zheng",

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

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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

UR - https://www.scopus.com/pages/publications/84945968249#tab=citedBy

U2 - 10.1016/j.bmcl.2015.10.029

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

Resumen

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Financiación

ASJC Scopus subject areas

ODS de las Naciones Unidas

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