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Serotonin 1a and serotonin-2 receptors are implicated in anxiety. Serazepine (CGS-15040A, (R, S)-1,3,4,16b-Tetrahydro-2-methyl-2H, 10H-indolo[2,1-c] Pyrazino-[1,2-a][1,4] benzodiazepine-16-carboxylic acid, methyl ester hydrochloride]) is a representative of a novel pentacyclic ring system containing a stabilized indole. In chemical assays it was a highly specific inhibitor of serotonin (5-HT2) binding, and it was active in preliminary preclinical assays of anxiolytic potential. This multicenter trial of CGS-15040A in patients with generalized anxiety disorder demonstrated clinical anxiolytic effects consistent with established preclinical effects. Doses greater than or equal to 10 mg reduced Hamilton Anxiety Scale scores. However, the dose -response relationship was nonlinear. Effects appeared primarily related to the psychic components of anxiety.
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Received in revised form: April 7, 1993
Received: June 20, 1992
© 1993 Published by Elsevier Inc.