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MPEP hydrochloride
Chemical Name:2-Methyl-6-(phenylethynyl)pyridine hydrochloride
Biological Activity:
Potent and highly selective
non-competitive antagonist at the mGlu5 receptor subtype (IC50
= 36 nM) and a positive allosteric modulator at mGlu4 receptors.
Centrally active following systemic administration in vivo. Reverses mechanical
hyperalgesia in the inflamed rat hind paw.
Boweset
al (1999) Anti-hyperalgesic effects of the novel metabotropic glutamate
receptor 5 antagonist, methylphenylethynylpyridine, in rat models of
inflammatory pain. Br.J.Pharmacol. 126 250P. Saltet al
(1999) Antagonism of the mGlu5 agonist 2-chloro-5-hydroxyphenylglycine by the
novel selective mGlu5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP) in
the thalamus. Br.J.Pharmacol. 127 1057. Gaspariniet al
(1999) 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and
systemically active mGlu5 receptor antagonist. Neuropharmacology 38
1493. Mathiesenet al (2003) Positive allosteric modulation of
the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP.
Br.J.Pharmacol. 138 1026.
