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Abstract
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.
Keywords
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Article info
Publication history
Received in revised form:
April 7,
1993
Received:
June 20,
1992
Identification
Copyright
© 1993 Published by Elsevier Inc.
