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J Med Chem. 2003 Jan 16;46(2):204-6.

3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.

Author information

1
Merck Research Laboratories, MRLSDB2, 3535, General Atomics Court, San Diego, California 92121, USA. nicholas_cosford@merck.com

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.

PMID:
12519057
DOI:
10.1021/jm025570j
[Indexed for MEDLINE]

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