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Namespace Prefixes

PrefixIRI
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n11http://linked.opendata.cz/resource/drugbank/drug/DB04970/identifier/chemspider/
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Statements

Subject Item
n2:DB04970
rdf:type
n3:Drug
n3:description
Lesopitron is an anxiolytic with pre- and post-synaptic 5-HT1A agonist activity, which is under development by Esteve.
n3:generalReferences
# Fisas MA, Farre A, Camarasa J, Escubedo E: Effects of lesopitron on the central nervous system arising from its interaction with 5-HT1A receptors. Pharmacology. 2004 Oct;72(2):57-67. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15331910 # Sramek JJ, Fresquet A, Marion-Landais G, Hourani J, Jhee SS, Martinez L, Jensen CM, Bolles K, Carrington AT, Cutler NR: Establishing the maximum tolerated dose of lesopitron in patients with generalized anxiety disorder: a bridging study. J Clin Psychopharmacol. 1996 Dec;16(6):454-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8959472 # Serafini MT, Puig S, Garcia-Encina G, Farran R, Garcia-Soret A, Moragon T, Martinez L: Absorption, distribution and excretion of [14C]-Lesopitron after single and repeated administration in rats and dogs. Methods Find Exp Clin Pharmacol. 1997 Jan-Feb;19(1):61-72. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9098842 # Micheli F: Lesopitron (Esteve). IDrugs. 2001 Feb;4(2):218-24. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16032484
n3:group
investigational
n3:halfLife
1.1 to 5.6 hours
n3:indication
Intended for the treatment of anxiety disorders.
owl:sameAs
n7:DB04970
dcterms:title
Lesopitron
adms:identifier
n9:DB04970 n10:60813 n11:54801 n12:14777028
n3:mechanismOfAction
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.
n3:synonym
Lesopitran
n3:toxicity
The most commonly reported adverse events in all the panels in one study were headache, dizziness, and nausea [PMID: 8959472].
n3:IUPAC-Name
n4:271B6193-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B6199-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B6198-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B6195-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B6196-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B6197-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B6191-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B618F-363D-11E5-9242-09173F13E4C5 n4:271B6192-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B6190-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n4:271B619F-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B61A0-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B619A-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B619B-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B619D-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B619C-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B619E-363D-11E5-9242-09173F13E4C5
n3: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.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
132449-46-8
n3:Bioavailability
n4:271B61A4-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B61A6-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B61A7-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B61A3-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B61A2-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B61A5-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B6194-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B61A1-363D-11E5-9242-09173F13E4C5