Multi-faceted aspects of gamma-hydroxybutyric acid: a neurotransmitter, therapeutic agent and drug of abuse.

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 gamma-aminobutyric acid type B (GABA(B)) receptor agonist. Here, I review the in vivo and in vitro pharmacological properties of GHB and its interaction with GHB and GABA(B) 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.

• Authors: M Paola Castelli
• Journal: Mini reviews in medicinal chemistry (Mini Rev Med Chem) Vol. 8 Issue 12 Pg. 1188-202 (Oct 2008) ISSN: 1389-5575 [Print] Netherlands
• PMID: 18855733 (Publication Type: Journal Article, Review)

Chemical References

• Hydroxybutyrates
• Ligands
• Neurotransmitter Agents
• 4-hydroxybutyric acid

Topics

• Alcoholism
• Anesthesia
• Animals
• Binding Sites
• Blood-Brain Barrier
• Brain (metabolism)
• Electrophysiology
• Haplorhini
• Humans
• Hydroxybutyrates (chemistry)
• Hypnosis
• Ligands
• Models, Chemical
• Neurotransmitter Agents (chemistry)
• Signal Transduction