Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H21ClN6.2ClH |
| Molecular Weight | 393.742 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.ClC1=CN(CCCCN2CCN(CC2)C3=NC=CC=N3)N=C1
InChI
InChIKey=RGDLQJUAYQRGBC-UHFFFAOYSA-N
InChI=1S/C15H21ClN6.2ClH/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;2*1H
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| 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 |
|---|---|---|
| Establishing the maximum tolerated dose of lesopitron in patients with generalized anxiety disorder: a bridging study. | 1996 Dec |
|
| 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 |
|
| Absorption, distribution and excretion of [14C]-Lesopitron after single and repeated administration in rats and dogs. | 1997 Jan-Feb |
|
| The influence of 5-HT2 and 5-HT4 receptor antagonists to modify drug induced disinhibitory effects in the mouse light/dark test. | 1997 Nov |
|
| Prevention by 5-HT1A receptor agonists of restraint stress- and yohimbine-induced release of cholecystokinin in the frontal cortex of the freely moving rat. | 1999 Apr |
|
| Lesopitron (Esteve). | 2001 Feb |
|
| Effects of lesopitron on the central nervous system arising from its interaction with 5-HT1A receptors. | 2004 Oct |
Patents
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:14:33 GMT 2025
by
admin
on
Mon Mar 31 18:14:33 GMT 2025
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| Record UNII |
4T5L4T8473
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| Record Status |
Validated (UNII)
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| Record Version |
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132449-89-9
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DTXSID00157588
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m6771
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4T5L4T8473
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admin on Mon Mar 31 18:14:33 GMT 2025 , Edited by admin on Mon Mar 31 18:14:33 GMT 2025
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PARENT -> SALT/SOLVATE |
