p-fluoro-hexahydro-sila-difenidol exhibits poor selectivity between m3 and m1 muscarinic receptors

Yuqing Meng; Jingru Hu; Esam E. El-Fakahany

doi:10.3109/09687689009025848

p-fluoro-hexahydro-sila-difenidol exhibits poor selectivity between m₃ and m₁ muscarinic receptors

Yuqing Meng, Jingru Hu, Esam E. El-Fakahany

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

2 Scopus citations

Abstract

We investigated the potential ability of p-fluoro-hexahydro-sila-difenidol (p-F-HHSiD) to discriminate between M₁ and M₃ muscarinic receptor subtypes using Chinese hamster ovary cells stably transfected with the genes encoding the two receptors. Both radioligand binding and functional assays were utilized for this purpose. In contrast to initial reports of a 14-fold selectivity of this antagonist for M₃ versus M₁ receptors, we have detected a qualitatively similar selectivity that was markedly smaller in magnitude.

Original language	English (US)
Pages (from-to)	293-300
Number of pages	8
Journal	Molecular Membrane Biology
Volume	9
Issue number	4
DOIs	https://doi.org/10.3109/09687689009025848
State	Published - 1990
Externally published	Yes

Bibliographical note

Funding Information:
This work was supported in part by a grant NS-25743 from the National Institutes of Health and contract DAAL-03-88K-0078 from the U. S. Army Research Office.

Keywords

CHO cells
Muscarinic receptors
P-F-hexahydro-sila-difenidol
Receptor subtypes

Access

10.3109/09687689009025848

OpenUrl availability

Full text

Cite this

@article{bad9111ac0fc4003b4eeface62311f9f,

title = "p-fluoro-hexahydro-sila-difenidol exhibits poor selectivity between m3 and m1 muscarinic receptors",

abstract = "We investigated the potential ability of p-fluoro-hexahydro-sila-difenidol (p-F-HHSiD) to discriminate between M1 and M3 muscarinic receptor subtypes using Chinese hamster ovary cells stably transfected with the genes encoding the two receptors. Both radioligand binding and functional assays were utilized for this purpose. In contrast to initial reports of a 14-fold selectivity of this antagonist for M3 versus M1 receptors, we have detected a qualitatively similar selectivity that was markedly smaller in magnitude.",

keywords = "CHO cells, Muscarinic receptors, P-F-hexahydro-sila-difenidol, Receptor subtypes",

author = "Yuqing Meng and Jingru Hu and El-Fakahany, {Esam E.}",

note = "Funding Information: This work was supported in part by a grant NS-25743 from the National Institutes of Health and contract DAAL-03-88K-0078 from the U. S. Army Research Office.",

year = "1990",

doi = "10.3109/09687689009025848",

language = "English (US)",

volume = "9",

pages = "293--300",

journal = "Molecular Membrane Biology",

issn = "0968-7688",

publisher = "Informa Healthcare",

number = "4",

}

TY - JOUR

T1 - p-fluoro-hexahydro-sila-difenidol exhibits poor selectivity between m3 and m1 muscarinic receptors

AU - Meng, Yuqing

AU - Hu, Jingru

AU - El-Fakahany, Esam E.

N1 - Funding Information: This work was supported in part by a grant NS-25743 from the National Institutes of Health and contract DAAL-03-88K-0078 from the U. S. Army Research Office.

PY - 1990

Y1 - 1990

N2 - We investigated the potential ability of p-fluoro-hexahydro-sila-difenidol (p-F-HHSiD) to discriminate between M1 and M3 muscarinic receptor subtypes using Chinese hamster ovary cells stably transfected with the genes encoding the two receptors. Both radioligand binding and functional assays were utilized for this purpose. In contrast to initial reports of a 14-fold selectivity of this antagonist for M3 versus M1 receptors, we have detected a qualitatively similar selectivity that was markedly smaller in magnitude.

AB - We investigated the potential ability of p-fluoro-hexahydro-sila-difenidol (p-F-HHSiD) to discriminate between M1 and M3 muscarinic receptor subtypes using Chinese hamster ovary cells stably transfected with the genes encoding the two receptors. Both radioligand binding and functional assays were utilized for this purpose. In contrast to initial reports of a 14-fold selectivity of this antagonist for M3 versus M1 receptors, we have detected a qualitatively similar selectivity that was markedly smaller in magnitude.

KW - CHO cells

KW - Muscarinic receptors

KW - P-F-hexahydro-sila-difenidol

KW - Receptor subtypes

UR - http://www.scopus.com/inward/record.url?scp=0025495605&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0025495605&partnerID=8YFLogxK

U2 - 10.3109/09687689009025848

DO - 10.3109/09687689009025848

M3 - Article

C2 - 1967074

AN - SCOPUS:0025495605

SN - 0968-7688

VL - 9

SP - 293

EP - 300

JO - Molecular Membrane Biology

JF - Molecular Membrane Biology

IS - 4

ER -