Serotonergic (5-HT2) mediation of anxiety-therapeutic effects of serazepine in generalized anxiety disorder

R. J. Katz; P. S. Landau; M. Lott; A. Bystritsky; B. Diamond; R. Hoehn-Saric; M. Rosenthal; C. Weise

doi:10.1016/0006-3223(93)90254-B

Serotonergic (5-HT₂) mediation of anxiety-therapeutic effects of serazepine in generalized anxiety disorder

R. J. Katz, P. S. Landau, M. Lott, A. Bystritsky, B. Diamond, R. Hoehn-Saric, M. Rosenthal, C. Weise

Research output: Contribution to journal › Article › peer-review

23 Scopus citations

Abstract

Serotonin 1_a 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.

Original language	English (US)
Pages (from-to)	41-44
Number of pages	4
Journal	Biological psychiatry
Volume	34
Issue number	1-2
DOIs	https://doi.org/10.1016/0006-3223(93)90254-B
State	Published - 1993
Externally published	Yes

Keywords

Anxiety CGS-15040
generalized anxiety disorder
serazepine
serotonin

ASJC Scopus subject areas

Biological Psychiatry

Access to Document

10.1016/0006-3223(93)90254-B

Cite this

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title = "Serotonergic (5-HT2) mediation of anxiety-therapeutic effects of serazepine in generalized anxiety disorder",

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 = "Anxiety CGS-15040, generalized anxiety disorder, serazepine, serotonin",

author = "Katz, {R. J.} and Landau, {P. S.} and M. Lott and A. Bystritsky and B. Diamond and R. Hoehn-Saric and M. Rosenthal and C. Weise",

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AU - Katz, R. J.

AU - Landau, P. S.

AU - Lott, M.

AU - Bystritsky, A.

AU - Diamond, B.

AU - Hoehn-Saric, R.

AU - Rosenthal, M.

AU - Weise, C.

PY - 1993

Y1 - 1993

N2 - 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.

AB - 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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