Analgesic, Anxiolytic, Antipsychotic/GABA Antagonists: Novel Selective GABA Autoreceptor Antagonists for the Treatment of a Variety of CNS Disorders

Summary

Novelty: The invention provides a method of treating or preventing pain and/or CNS disorders such as those requiring anxiolytic, hypnotic, muscle relaxant, anticonvulsant, antidepressant, antipsychotic and/or movement disorder therapy. It comprises administration of an effective amount of a compound having selective antagonist activity at GABA autoreceptors.

Biology: Antagonist activity at GABA autoreceptors is measured by blockade of agonist-induced inhibition of potassium-evoked GABA release from rat cortex in vitro and by antagonism of agonist-induced depolarisation of isolated rat vagus nerve.

Chemistry: Twenty-two compounds are exemplified by synthesis. 1,2,3,4-Tetrahydro-1-(2-thienyl)isoquinoline is typical of the claim.