3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity
Nicholas D. P. Cosford
1
,
Lida Tehrani
1
,
Jeffrey Roppe
1
,
Edwin Schweiger
1
,
Nicholas D Smith
1
,
Jeffrey Anderson
1
,
LINDA BRISTOW
1
,
Jesse Brodkin
1
,
Xiaohui Jiang
1
,
Ian McDonald
1
,
sara rao
1
,
Mark Washburn
1
,
Mark A. Varney
1
1
Merck Research Laboratories, MRLSDB2, 3535, General Atomics Court, San Diego, California 92121
|
Publication type: Journal Article
Publication date: 2002-12-12
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
12519057
Drug Discovery
Molecular Medicine
Abstract
2-Methyl-6-(phenylethynyl)pyridine (3), a potent noncompetitive mGlu5 receptor antagonist widely used to characterize the pharmacology of mGlu5 receptors, suffers from a number of shortcomings as a therapeutic agent, including off-target activity and poor aqueous solubility. Seeking to improve the properties of 3 led to the synthesis of compound 9, a highly selective mGlu5 receptor antagonist that is 5-fold more potent than 3 in the rat fear-potentiated startle model of anxiety.
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356
Total citations:
356
Citations from 2025:
5
(1.4%)
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MLA
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GOST
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Cosford N. D. P. et al. 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity // Journal of Medicinal Chemistry. 2002. Vol. 46. No. 2. pp. 204-206.
GOST all authors (up to 50)
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Cosford N. D. P., Tehrani L., Roppe J., Schweiger E., Smith N. D., Anderson J., BRISTOW L., Brodkin J., Jiang X., McDonald I., rao S., Washburn M., Varney M. A. 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity // Journal of Medicinal Chemistry. 2002. Vol. 46. No. 2. pp. 204-206.
Cite this
RIS
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TY - JOUR
DO - 10.1021/jm025570j
UR - https://doi.org/10.1021/jm025570j
TI - 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity
T2 - Journal of Medicinal Chemistry
AU - Cosford, Nicholas D. P.
AU - Tehrani, Lida
AU - Roppe, Jeffrey
AU - Schweiger, Edwin
AU - Smith, Nicholas D
AU - Anderson, Jeffrey
AU - BRISTOW, LINDA
AU - Brodkin, Jesse
AU - Jiang, Xiaohui
AU - McDonald, Ian
AU - rao, sara
AU - Washburn, Mark
AU - Varney, Mark A.
PY - 2002
DA - 2002/12/12
PB - American Chemical Society (ACS)
SP - 204-206
IS - 2
VL - 46
PMID - 12519057
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2002_Cosford,
author = {Nicholas D. P. Cosford and Lida Tehrani and Jeffrey Roppe and Edwin Schweiger and Nicholas D Smith and Jeffrey Anderson and LINDA BRISTOW and Jesse Brodkin and Xiaohui Jiang and Ian McDonald and sara rao and Mark Washburn and Mark A. Varney},
title = {3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity},
journal = {Journal of Medicinal Chemistry},
year = {2002},
volume = {46},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/jm025570j},
number = {2},
pages = {204--206},
doi = {10.1021/jm025570j}
}
Cite this
MLA
Copy
Cosford, Nicholas D. P., et al. “3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity.” Journal of Medicinal Chemistry, vol. 46, no. 2, Dec. 2002, pp. 204-206. https://doi.org/10.1021/jm025570j.