Homotaurine

Medical use

Acamprosate (N-acetyl homotaurine) was approved by the FDA in 2004 to treat alcohol dependence.

Biochemical properties

In preclinical studies it had been found to bind to soluble amyloid beta and inhibit the formation of neurotoxic aggregates. Homotaurine has also shown anticonvulsant activities, reduction in skeletal muscle tonus, and hypothermic activity.

Homotaurine has been reported as a GABA antagonist, In vitro studies have found that homotaurine is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy, becoming an antagonist and displacing the full agonists GABA and baclofen at this receptor. In a study in rats, homotaurine reversed the catatonia induced by baclofen (the prototypical GABAB agonist), and was able to produce analgesia via the GABAB receptor, an effect that was abolished when CGP-35348, a GABAB receptor antagonist was applied.

In a human study homotaurine selectively and fully inhibits the formation of Aβ42 oligomers at the clinical dose, without evidence of vasogenic edema.

One study in rats showed that homotaurine suppressed ethanol-stimulated dopamine release, as well as ethanol intake and preference in rats in a way similar to the N-acetyl derivative of homotaurine, acamprosate.

References

References

1. "Homotaurine". [[Sigma-Aldrich]].
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14. (September 1987). "Baclofen induces catatonia in rats". Neuropharmacology.
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