Tìm theo
Lesopitron
Các tên gọi khác (1) :
  • Lesopitran
Thuốc Gốc
Small Molecule
CAS: 132449-46-8
CTHH: C15H21ClN6
PTK: 320.82
Lesopitron is an anxiolytic with pre- and post-synaptic 5-HT1A agonist activity, which is under development by Esteve.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H21ClN6
Phân tử khối
320.82
Monoisotopic mass
320.151622409
InChI
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
InChI Key
InChIKey=AHCPKWJUALHOPH-UHFFFAOYSA-N
IUPAC Name
2-{4-[4-(4-chloro-1H-pyrazol-1-yl)butyl]piperazin-1-yl}pyrimidine
Traditional IUPAC Name
lesopitron
SMILES
ClC1=CN(CCCCN2CCN(CC2)C2=NC=CC=N2)N=C1
Độ hòa tan
1.25e+00 g/l
logP
2.09
logS
-2.4
pKa (Strongest Basic)
7.75
PSA
50.08 Å2
Refractivity
100.45 m3·mol-1
Polarizability
34.97 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
5
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : In phase I trials in healthy volunteers, lesopitron was well tolerated in single doses up to 50 mg, and up to 45 mg/day in repeated doses. Lesopitron has negligible effects on alpha-adrenergic and dopaminergic receptors, 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.
Cơ Chế Tác Dụng : Lesopitron is an anxiolytic with pre- and post-synaptic 5-HT1A agonist activity, which is under development by Esteve. Lesopitron acts as a ligand for central serotonin 5-HT1A receptors. Lesopitron inhibits haloperidol-induced catalepsy that is the consequence of its action on 5-HT1A autoreceptors. The ability of lesopitron to induce 5-HT syndrome reflects post-synaptic 5-HT1A receptor activation and the reversion of 8-OHDPAT-induced 5-HT syndrome by lesopitron suggests a partial agonist effect on this receptor-type. Lesopitron induced a hypothermic effect due to the enhanced activation of post-synaptic 5-HT1A receptors. The agonist effect of lesopitron on 5-HT1A receptors and its marked hypothermic effect is an added value for this drug and a stimulus to the study of its possible neuroprotective action.
Dược Động Học :
▧ Absorption :
Rapidly absorbed in patients, having a time to maximum concentration (Tmax) ranging from 0.5 to 1 hour. The absolute bioavailability of lesopitron in rats was about 10%, suggesting an important first-pass effect.
▧ Metabolism :
Hepatic, the main metabolite being 5-hydroxylesopitron.
▧ Half Life :
1.1 to 5.6 hours
Độc Tính : The most commonly reported adverse events in all the panels in one study were headache, dizziness, and nausea [PMID: 8959472].
Chỉ Định : Intended for the treatment of anxiety disorders.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04970
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60813
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=14777028
ChemSpider
http://www.chemspider.com/Chemical-Structure.54801.html
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