About: Lesopitron     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Lesopitron is an anxiolytic with pre- and post-synaptic 5-HT1A agonist activity, which is under development by Esteve. (en)
http://linked.open...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 (en)
http://linked.open...gy/drugbank/group
  • investigational (en)
http://linked.open...drugbank/halfLife
  • 1.1 to 5.6 hours (en)
http://linked.open...ugbank/indication
  • Intended for the treatment of anxiety disorders. (en)
sameAs
Title
  • Lesopitron (en)
adms:identifier
http://linked.open...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. (en)
http://linked.open.../drugbank/synonym
  • Lesopitran (en)
http://linked.open...drugbank/toxicity
  • The most commonly reported adverse events in all the panels in one study were headache, dizziness, and nausea [PMID: 8959472]. (en)
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
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http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/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. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 132449-46-8 (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
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http://linked.open...-strongest-basic-
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