Activation of a Receptor for Treating Alcoholism

Activation of a receptor with no known function in the brain reduces excessive alcohol use and the pain of withdrawal, according to preclinical research in male rats.

GPR139 is an orphan G protein-coupled receptor that is expressed mainly in the brain, with the highest expression in the medial habenula. The modulation of GPR139 receptor function has been hypothesized to be beneficial in the treatment of some mental disorders, but behavioral studies have not yet provided causal evidence of the role of GPR139 in brain dysfunction.

The scientists behind the study hypothesized that Because of the high expression of GPR139 in the habenula, a critical brain region in addiction, we can assume that GPR139 may play a role in alcohol dependence.

Experimenting with male rats, researchers found that activation of GPR139 reduced alcohol intake and restored pain sensitivity thresholds only in alcohol-dependent mice that showed compulsive-like alcohol consumption akin to problematic drinking in humans.

The results of the study provide robust preclinical evidence that GPR139 receptor activation reverses key addiction-like behaviors in dependent animals, suggesting that GPR139 may be a novel target for the treatment of alcohol use disorder.

Sources:

Jenni Kononoff, Marsida Kallupi, Adam Kimbrough, Dana Conlisk, Giordano de Guglielmo, Olivier George. Systemic and Intra-Habenular Activation of the Orphan G Protein-Coupled Receptor GPR139 Decreases Compulsive-like Alcohol Drinking and Hyperalgesia in Alcohol-Dependent Rats. eneuro, 2018; ENEURO.0153-18.2018 DOI: 10.1523/ENEURO.0153-18.2018

Society for Neuroscience. “New target for treating alcoholism: Activating GPR139 in rats reduced excessive alcohol use and pain of withdrawal.” ScienceDaily. ScienceDaily, 25 June 2018. <www.sciencedaily.com/releases/2018/06/180625130945.htm>.

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