<?xml version="1.0" encoding="UTF-8"?>
<compound>
  <id type="integer">2821</id>
  <title>T3D2779</title>
  <common-name>Loxapine</common-name>
  <description>Loxapine is only found in individuals that have used or taken this drug. It is an antipsychotic agent used in schizophrenia. Loxapine is a dopamine antagonist, and also a serotonin 5-HT2 blocker. The exact mode of action of Loxapine has not been established, however changes in the level of excitability of subcortical inhibitory areas have been observed in several animal species in association with such manifestations of tranquilization as calming effects and suppression of aggressive behavior.</description>
  <cas>1977-10-2</cas>
  <pubchem-id>3964</pubchem-id>
  <chemical-formula>C18H18ClN3O</chemical-formula>
  <weight>327.113840</weight>
  <appearance>White powder.</appearance>
  <melting-point>109-111°C</melting-point>
  <boiling-point nil="true"/>
  <density nil="true"/>
  <solubility>1.03e-01 g/L</solubility>
  <specific-gravity nil="true"/>
  <flash-point nil="true"/>
  <vapour-pressure nil="true"/>
  <route-of-exposure>Oral, Intramuscular.Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers.</route-of-exposure>
  <target nil="true"/>
  <mechanism-of-toxicity>Loxapine is a dopamine antagonist, and also a serotonin 5-HT2 blocker. The exact mode of action of Loxapine has not been established, however changes in the level of excitability of subcortical inhibitory areas have been observed in several animal species in association with such manifestations of tranquilization as calming effects and suppression of aggressive behavior.</mechanism-of-toxicity>
  <metabolism>HepaticRoute of Elimination: Metabolites are excreted in the urine in the form of conjugates and in the feces unconjugated.Half Life: Oral-4 hours</metabolism>
  <toxicity>LD&lt;sub&gt;50&lt;/sub&gt;=65 mg/kg (Orally in mice)</toxicity>
  <lethaldose nil="true"/>
  <carcinogenicity>No indication of carcinogenicity to humans (not listed by IARC).</carcinogenicity>
  <use-source>For the management of the manifestations of psychotic disorders such as schizophrenia</use-source>
  <min-risk-level nil="true"/>
  <health-effects nil="true"/>
  <symptoms>LD&lt;sub&gt;50&lt;/sub&gt;=65 mg/kg (Orally in mice)</symptoms>
  <treatment>The treatment of overdosage is essentially symptomatic and supportive. Early gastric lavage and extended dialysis might be expected to be beneficial. Centrally-acting emetics may have little effect because of the antiemetic action of loxapine. In addition, emesis should be avoided because of the possibility of aspiration of vomitus. Avoid analeptics, such as pentylenetetrazol, which may cause convulsions. Severe hypotension might be expected to respond to the administration of levarterenol or phenylephrine. Epinephrine should not be used since its use in a patient with partial adrenergic blockade may further lower the blood pressure. Severe extrapyramidal reactions should be treated with anticholinergic antiparkinson agents or diphenhydramine hydrochloride, and anticonvulsant therapy should be initiated as indicated. Additional measures include oxygen and intravenous fluids. (L1712)</treatment>
  <created-at type="dateTime">2009-07-21T20:26:49Z</created-at>
  <updated-at type="dateTime">2014-12-24T20:25:51Z</updated-at>
  <interacting-proteins nil="true"/>
  <wikipedia>Loxapine</wikipedia>
  <uniprot-id></uniprot-id>
  <kegg-compound-id>C07104</kegg-compound-id>
  <omim-id></omim-id>
  <chebi-id>50841</chebi-id>
  <biocyc-id></biocyc-id>
  <ctd-id nil="true"/>
  <stitch-id>Loxapine</stitch-id>
  <drugbank-id>DB00408</drugbank-id>
  <pdb-id></pdb-id>
  <actor-id nil="true"/>
  <organism nil="true"/>
  <export type="boolean">true</export>
  <metabolizing-proteins nil="true"/>
  <transporting-proteins nil="true"/>
  <moldb-smiles>CN1CCN(CC1)C1=NC2=CC=CC=C2OC2=C1C=C(Cl)C=C2</moldb-smiles>
  <moldb-formula>C18H18ClN3O</moldb-formula>
  <moldb-inchi>InChI=1S/C18H18ClN3O/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18/h2-7,12H,8-11H2,1H3</moldb-inchi>
  <moldb-inchikey>InChIKey=XJGVXQDUIWGIRW-UHFFFAOYSA-N</moldb-inchikey>
  <moldb-average-mass type="decimal">327.808</moldb-average-mass>
  <moldb-mono-mass type="decimal">327.11383992</moldb-mono-mass>
  <origin>Exogenous</origin>
  <state>Solid</state>
  <logp>3.6</logp>
  <hmdb-id>HMDB14552</hmdb-id>
  <chembl-id>CHEMBL831</chembl-id>
  <chemspider-id>3827</chemspider-id>
  <structure-image-file-name nil="true"/>
  <structure-image-content-type nil="true"/>
  <structure-image-file-size type="integer" nil="true"/>
  <structure-image-updated-at type="dateTime" nil="true"/>
  <biodb-id nil="true"/>
  <synthesis-reference>&lt;p&gt;U.S. Patents 3,412,193; 3,546,226.&lt;/p&gt;</synthesis-reference>
  <structure-image-caption nil="true"/>
</compound>
