Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H21ClN6 |
Molecular Weight | 320.82 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=CN(CCCCN2CCN(CC2)C3=NC=CC=N3)N=C1
InChI
InChIKey=AHCPKWJUALHOPH-UHFFFAOYSA-N
InChI=1S/C15H21ClN6/c16-14-12-19-22(13-14)7-2-1-6-20-8-10-21(11-9-20)15-17-4-3-5-18-15/h3-5,12-13H,1-2,6-11H2
Molecular Formula | C15H21ClN6 |
Molecular Weight | 320.82 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Lesopitron is a non-benzodiazepine anxiolytic with pre- and post-synaptic 5-HT1A agonist activity. Its structure is similar to that of buspirone. Lesopitron has negligible effects on alpha-adrenergic and dopaminergic receptors [162653], and was more potent than structurally-related 5-HT1A agonists in rat social interaction and marmoset anxiety models. It also countered benzodiazepine withdrawal-induced anxiety in rodents. The acute toxicity of lesopitron is low and it does not potentiate the effects of alcohol or barbiturates. Long-term usage led to reductions in plasma glucose, triglycerides, phospholipids and cholesterol. The most common adverse events associated with lesopitron were somnolence, headache, pharyngitis, and dyspepsia.
Approval Year
PubMed
Title | Date | PubMed |
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Establishing the maximum tolerated dose of lesopitron in patients with generalized anxiety disorder: a bridging study. | 1996 Dec |
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Differential effects of haloperidol and two anxiolytic drugs, buspirone and lesopitron, on c-Fos expression in the rat striatum and nucleus accumbens. | 1996 Dec 2 |
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Absorption, distribution and excretion of [14C]-Lesopitron after single and repeated administration in rats and dogs. | 1997 Jan-Feb |
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The influence of 5-HT2 and 5-HT4 receptor antagonists to modify drug induced disinhibitory effects in the mouse light/dark test. | 1997 Nov |
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Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder. | 2000 Feb |
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Lesopitron (Esteve). | 2001 Feb |
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Effects of lesopitron on the central nervous system arising from its interaction with 5-HT1A receptors. | 2004 Oct |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8959472
50 mg two times a day
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 16:54:04 GMT 2023
by
admin
on
Sat Dec 16 16:54:04 GMT 2023
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Record UNII |
H1CGM4755H
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C47794
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m6771
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DTXSID40157587
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C80761
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60813
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Lesopitron
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C075568
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |