Functional characterisation of human glycine receptors in a fluorescence-based high throughput screening assay

Anders A. Jensen

doi:10.1016/j.ejphar.2005.08.002

Functional characterisation of human glycine receptors in a fluorescence-based high throughput screening assay

13 Citationer (Scopus)

Abstract

The human glycine receptor subtypes alpha1beta and alpha2 have been expressed stably in HEK293 cells, and the functional characteristics of the receptors have been characterised in the FLIPR Membrane Potential Assay. The pharmacological properties obtained for nine standard ligands at the two receptors in this assay were found to be in good agreement with those from electrophysiology studies of the receptors expressed in Xenopus oocytes or mammalian cell lines. Hence, this high throughput screening assay will be of great use in future pharmacological studies of glycine receptors, particular in the search for novel compound structures acting at them.

Originalsprog	Engelsk
Tidsskrift	European Journal of Pharmacology
Vol/bind	521
Udgave nummer	1-3
Sider (fra-til)	39-42
Antal sider	4
ISSN	0014-2999
DOI	https://doi.org/10.1016/j.ejphar.2005.08.002
Status	Udgivet - 2005

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10.1016/j.ejphar.2005.08.002

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title = "Functional characterisation of human glycine receptors in a fluorescence-based high throughput screening assay",

abstract = "The human glycine receptor subtypes alpha1beta and alpha2 have been expressed stably in HEK293 cells, and the functional characteristics of the receptors have been characterised in the FLIPR Membrane Potential Assay. The pharmacological properties obtained for nine standard ligands at the two receptors in this assay were found to be in good agreement with those from electrophysiology studies of the receptors expressed in Xenopus oocytes or mammalian cell lines. Hence, this high throughput screening assay will be of great use in future pharmacological studies of glycine receptors, particular in the search for novel compound structures acting at them.",

keywords = "Androstanes, Azasteroids, Cell Line, Dose-Response Relationship, Drug, Fluorescence, Glycine, Glycine Agents, Humans, Membrane Potentials, Patch-Clamp Techniques, Picrotoxin, Receptors, Glycine, Strychnine, Taurine, Transfection, beta-Alanine",

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T1 - Functional characterisation of human glycine receptors in a fluorescence-based high throughput screening assay

AU - Jensen, Anders A.

PY - 2005

Y1 - 2005

N2 - The human glycine receptor subtypes alpha1beta and alpha2 have been expressed stably in HEK293 cells, and the functional characteristics of the receptors have been characterised in the FLIPR Membrane Potential Assay. The pharmacological properties obtained for nine standard ligands at the two receptors in this assay were found to be in good agreement with those from electrophysiology studies of the receptors expressed in Xenopus oocytes or mammalian cell lines. Hence, this high throughput screening assay will be of great use in future pharmacological studies of glycine receptors, particular in the search for novel compound structures acting at them.

AB - The human glycine receptor subtypes alpha1beta and alpha2 have been expressed stably in HEK293 cells, and the functional characteristics of the receptors have been characterised in the FLIPR Membrane Potential Assay. The pharmacological properties obtained for nine standard ligands at the two receptors in this assay were found to be in good agreement with those from electrophysiology studies of the receptors expressed in Xenopus oocytes or mammalian cell lines. Hence, this high throughput screening assay will be of great use in future pharmacological studies of glycine receptors, particular in the search for novel compound structures acting at them.

KW - Androstanes

KW - Azasteroids

KW - Cell Line

KW - Dose-Response Relationship, Drug

KW - Fluorescence

KW - Glycine

KW - Glycine Agents

KW - Humans

KW - Membrane Potentials

KW - Patch-Clamp Techniques

KW - Picrotoxin

KW - Receptors, Glycine

KW - Strychnine

KW - Taurine

KW - Transfection

KW - beta-Alanine

U2 - 10.1016/j.ejphar.2005.08.002

DO - 10.1016/j.ejphar.2005.08.002

M3 - Journal article

C2 - 16182281

SN - 0014-2999

VL - 521

SP - 39

EP - 42

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 1-3

ER -

Functional characterisation of human glycine receptors in a fluorescence-based high throughput screening assay

Abstract

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