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Alcohol Addiction- Metabotropic Glutamate Receptor Subtype 5 and its Ligands: How They All Come Together?
Jaya Kumar1, Zalina Ismail2, Nurul Hazwani Hatta3
1Department of Physiology, Faculty of Medicine, Universiti Kebangsaan Malaysia Medical Centre, 56000 Cheras, Kuala Lumpur, Malaysia.
Current Drug Targets
|May 13, 2017
Summary
Metabotropic glutamate receptor 5 (mGlu5) modulators show promise in reducing alcohol consumption and relapse behaviors. These agents target mGlu5 signaling pathways involved in alcohol
Area of Science:
- Neuroscience
- Pharmacology
- Addiction Research
Background:
- Metabotropic glutamate receptor subtype 5 (mGlu5) modulators have demonstrated efficacy in preclinical models for reducing alcohol-related behaviors.
- mGlu5 receptors are abundant in brain regions critical for emotion regulation, motivation, and drug administration.
- These receptors are postsynaptically located and linked to cell signaling and gene transcription pathways mediating alcohol-induced neuroplasticity.
Purpose of the Study:
- To review the effects of acute and chronic alcohol intake on mGlu5 signaling.
- To examine the impact of mGlu5 ligands on alcohol-related neurobehavioral changes in preclinical and clinical studies.
- To elucidate the underlying mechanisms of action for mGlu5-targeting drugs in alcohol use disorder.
Main Methods:
- Literature review of studies investigating mGlu5 modulators and alcohol-related effects.
- Analysis of preclinical and clinical data on mGlu5 ligands' efficacy.
- Exploration of the functional link between mGlu5 and Protein Kinase C epsilon (PKCε).
Main Results:
- mGlu5 modulators show potential in attenuating alcohol consumption, alcohol-seeking, and relapse-like behaviors.
- Negative allosteric modulators of mGlu5, such as MPEP and MTEP, exhibit therapeutic potential.
- A functional link between mGlu5 and PKCε is implicated in the therapeutic effects of mGlu5 modulators.
Conclusions:
- Pharmacological agents targeting mGlu5 represent a promising therapeutic strategy for alcohol use disorder.
- Further research into mGlu5 signaling pathways and their interaction with alcohol is warranted.
- mGlu5 modulators could offer novel treatment options for curbing inebriation and managing alcohol dependence.
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