3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl] -4-methylpyridine: A Highly Potent and Orally Bioavailable Metabotropic Glutamate Subtype 5 (mGlu5) Receptor Antagonist.

ChemInform ◽  
2005 ◽  
Vol 36 (14) ◽  
Author(s):  
Steve F. Poon ◽  
Brian W. Eastman ◽  
Deborah F. Chapman ◽  
Janice Chung ◽  
Merryl Cramer ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Metabotropic Glutamate ◽  
Mglu5 Receptor ◽  
Orally Bioavailable

2-{2-[3-(Pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl}pyridine: A Highly Potent, Orally Active, Metabotropic Glutamate Subtype 5 (mGlu5) Receptor Antagonist.

ChemInform ◽  
2005 ◽  
Vol 36 (14) ◽  
Author(s):  
Dehua Huang ◽  
Steve F. Poon ◽  
Deborah F. Chapman ◽  
Janice Chung ◽  
Merryl Cramer ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Metabotropic Glutamate ◽  
Mglu5 Receptor ◽  
Orally Active

2-{2-[3-(Pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl}pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist

2004 ◽  
Vol 14 (22) ◽  
pp. 5473-5476 ◽  
Author(s):  
Dehua Huang ◽  
Steve F. Poon ◽  
Deborah F. Chapman ◽  
Janice Chung ◽  
Merryl Cramer ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Metabotropic Glutamate ◽  
Mglu5 Receptor ◽  
Orally Active

scholarly journals Effects of the Positive Allosteric Modulator of Metabotropic Glutamate Receptor 5, VU-29, on Maintenance Association between Environmental Cues and Rewarding Properties of Ethanol in Rats

Biomolecules ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 793
Author(s):  
Marta Marszalek-Grabska ◽  
Kinga Gawel ◽  
Dariusz Matosiuk ◽  
Ewa Gibula-Tarlowska ◽  
Joanna Listos ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Home Cage ◽  
Metabotropic Glutamate Receptor ◽  
Drugs Of Abuse ◽  
Inhibitory Effect ◽  
Future Research ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Metabotropic Glutamate ◽  
Mglu5 Receptor

Metabotropic glutamate subtype 5 (mGlu5) receptors are implicated in various forms of synaptic plasticity, including drugs of abuse. In drug-addicted individuals, associative memories can drive relapse to drug use. The present study investigated the potential of the mGlu5 receptor positive allosteric modulator (PAM), VU-29 (30 mg/kg, i.p.), to inhibit the maintenance of a learned association between ethanol and environmental context by using conditioned place preference (CPP) in rats. The ethanol-CPP was established by the administration of ethanol (1.0 g/kg, i.p. ×10 days) using an unbiased procedure. Following ethanol conditioning, VU-29 was administered at various post-conditioning times (ethanol free state at the home cage) to ascertain if there was a temporal window during which VU-29 would be effective. Our experiments indicated that VU-29 did not affect the expression of ethanol-induced CPP when it was given over two post-conditioning days. However, the expression of ethanol-CPP was inhibited by 10-day home cage administration of VU-29, but not by first 2-day or last 2-day injection of VU-29 during the 10-day period. These findings reveal that VU-29 can inhibit the maintenance of ethanol-induced CPP, and that treatment duration contributes to this effect of VU-29. Furthermore, VU-29 effect was reversed by pretreatment with either MTEP (the mGlu5 receptor antagonist), or MK-801 (the N-methyl-D-aspartate-NMDA receptor antagonist). Thus, the inhibitory effect of VU-29 is dependent on the functional interaction between mGlu5 and NMDA receptors. Because a reduction in ethanol-associated cues can reduce relapse, mGlu5 receptor PAM would be useful for therapy of alcoholism. Future research is required to confirm the current findings.

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