Glutamate release inhibiting properties of the novel mGlu(5) receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP): complementary in vitro and in vivo evidence.
We have previously demonstrated that neuronal release of the excitatory amino acid glutamate is facilitated by the selective activation of presynaptic Group I metabotropic autoreceptors. Here we report the release inhibiting actions of the novel mGlu(5) receptor-selective antagonist, 2-methyl-6-(phenylethynyl)-pyridine (MPEP), both in vitro and in vivo. These data provide compelling evidence for the presence of functional positive modulatory mGlu(5) subtype autoreceptors in the mammalian central nervous system.
Thomas
L S
LS
Department of Neuroinflammation, Imperial College School of Medicine, Charing Cross Hospital, Fulham Palace Road, London W6 8RF, UK.
Jane
D E
DE
Gasparini
F
F
Croucher
M J
MJ
D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects; D004558:Electric Stimulation; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology*; D018698:Glutamic Acid / Q000378:metabolism*; D005998:Glycine / Q000031:analogs & derivatives / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D017551:Microdialysis; D011725:Pyridines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D018092:Kainic Acid Receptors / Q000037:antagonists & inhibitors*; D012118:Resorcinols / Q000494:pharmacology
D018691:Excitatory Amino Acid Antagonists; D018698:Glutamic Acid; D005998:Glycine; D011725:Pyridines; D018092:Kainic Acid Receptors; D012118:Resorcinols; C079215:3,5-dihydroxyphenylglycine; C121465:6-methyl-2-(phenylethynyl)pyridine