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.
Serotonergic (5-HT2) mediation of anxiety-therapeutic effects of serazepine in generalized anxiety disorder. / Katz, R. J.; Landau, P. S.; Lott, M.; Bystritsky, A.; Diamond, B.; Hoehn-Saric, Rudolf; Rosenthal, M.; Weise, C.In: Biological Psychiatry, Vol. 34, No. 1-2, 1993, p. 41-44.
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