Multi-Faceted Aspects ofGamma-Hydroxybutyric Acid: A Neurotransmitter, Therapeutic Agent and Drug of Abuse

Title: Multi-Faceted Aspects ofGamma-Hydroxybutyric Acid: A Neurotransmitter, Therapeutic Agent and Drug of Abuse

Volume: 8 Issue: 12

Author(s): M. Paola Castelli

Affiliation:

Keywords: GHB, GHB receptor, GABAB receptor, NCS-382

Abstract: Gamma hydroxybutyric acid (GHB), an endogenous constituent of the mammalian brain, acts as i) a neurotransmitter or neuromodulator, ii) a medicine used for the treatment of narcolepsy and alcoholism, and iii) a drug illicitly used for its psychotropic effects. GHB is thought to act as a specific GHB receptor agonist as well as a weak gammaaminobutyric acid type B (GABAB) receptor agonist. Here, I review the in vivo and in vitro pharmacological properties of GHB and its interaction with GHB and GABAB receptors. When exogenously administered, GHB is rapidly absorbed, crosses the blood-brain barrier, penetrates into the brain and exerts a number of pharmacological effects including anxiolysis, sedation/hypnosis and anesthesia. Due to its effects on the central nervous system, GHB has been used for the treatment of narcolepsy and as an anesthetic adjuvant. More recently, a role for GHB in the pharmacotherapy of alcohol dependence has been described. In this review, I also focus on the abuse liability and reinforcing properties of GHB in humans and laboratory animals.

Cite this article as:

Castelli Paola M., Multi-Faceted Aspects ofGamma-Hydroxybutyric Acid: A Neurotransmitter, Therapeutic Agent and Drug of Abuse, Mini-Reviews in Medicinal Chemistry 2008; 8 (12) . https://dx.doi.org/10.2174/138955708786141025