cgp-36742 and Muscle-Spasticity

Although the presence of functional GABAB receptors in mammalian brain has been known for more than 20 years, there is still only one therapeutic agent in use, baclofen, which mediates its effects directly via this receptor. However, activation of this receptor can produce numerous effects that might be amenable to drug development. Evidence from preclinical studies also suggests that antagonism of the GABAB receptor produces beneficial clinical effects.

Topics: Animals; Baclofen; Brain; Clinical Trials as Topic; Cognition; Drug Evaluation, Preclinical; Epilepsy, Absence; GABA Agonists; GABA Antagonists; Humans; Muscle Spasticity; Organophosphorus Compounds; Pain; Receptors, GABA-B; Substance-Related Disorders