StartseiteMCPWorkbenchSkills
StartseiteWorkbenchBenachrichtigungenMein Bereich
Huagongshe Open Project：[email protected]KI-Anbindung: llms.txt · MCP-AnleitungDatenschutz · Nutzungsbedingungen · Supportv1.7.8
Zurück
HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HCID 3964Erstellt: 4. November 2026

Loxapin

2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine · C07104 · Loxapine (Standard) · Loxapine, 10 mM in DMSO · Dibenz[b,f][1,4]oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)- · Inhibitor,schizophrenia,IL-2,Loxapine,inhibit,5-HT Receptor,5-hydroxytryptamine Receptor,Dopamine Receptor,Serotonin Receptor,serotonin,IL-1β,antipsychotics

https://huagongshe.com/de/chemical/3964

Molekülstruktur von Loxapin

Identifikatoren & physikalische Daten

CAS No.1977-10-2
SummenformelC18H18ClN3O
Durchschnittliche Molmasse327,8 g/mol
Monoisotopische Masse327,1138399 g/mol
SMILESCN1CCN(C2=Nc3ccccc3Oc3ccc(Cl)cc32)CC1
InChIKeyXJGVXQDUIWGIRW-UHFFFAOYSA-N
PubChem CID3964
ChEMBLCHEMBL831
ChEBICHEBI:50841
EC No.217-835-3
DTXSIDDTXSID7023229
Lokaler NameLoxapin

Chemische & physikalische Eigenschaften

XLogP3,1
Polarare Oberfläche (TPSA)28,1
H-Brücken-Donoren0
H-Brücken-Akzeptoren3
Frei drehbare Bindungen1
Schwere Atome23
Formalladung0
Komplexität450
ArzneimittelPharmaceuticals -> Listed in ZINC15
LogP (Verteilungskoeffizient)3.63.86
Color/FormPale yellowish crystals from petroleum ether
Löslichkeit1.03e-01 g/LSoluble in DMSO
Human DrugsBreast FeedingLactationAntipsychotic AgentsFDA approved drugs -> Active ingredientEMA approved medicines: Human medicinePharmaceuticals
DecompositionWhen heated to decomposition it emits very toxic fumes of /hydrogen chloride/ and nitroxides.
Schmelzpunkt109-111 °C109-110 °C109 - 110 °C109-110°
Physical DescriptionSolid
Dissociation Constants7.487.5
Collision Cross Section175.7 Ų [M+H]+ [CCS Type: TWMethod: Major Mix IMS/Tof Calibration Kit (Waters)]178.56 Ų [M+Na]+ [CCS Type: TWMethod: calibrated with polyalanine and drug standards]
Dichte1.2299 (rough estimate)
Brechungsindex1.5800 (estimate)
LagerbedingungenStore at -20°C
AggregatzustandPowder
FarbeLight yellow to yellow
CAS Datenbank1977-10-2

Sicherheit & Vorschriften

GHS-EinstufungDangerH301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]P264, P270, P301+P316, P321, P330, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 4 reports by companies from 2 notifications to the ECHA C&L Inventory.
Regulatorische InformationenREACH registered substance: Loxapine (EC: 217-835-3)
FDA-AnforderungenManufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended21 U.S.C. 321-392).
Hazard Classes and CategoriesAcute Tox. 3 (100%)
EntsorgungsverfahrenSRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.
TreatmentThe 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)
WechselwirkungenLOXAPINE MAY BE ADDITIVE WITH OR MAY POTENTIATE ACTION OF OTHER CNS DEPRESSANTS (INCLUDING BARBITURATES & ALCOHOL) OR ANTICHOLINERGIC AGENTS...INHIBITS VASOPRESSOR EFFECT OF EPINEPHRINEConcurrent use /with alcohol or other central nervous system (CNS) depression-producing medications, especially anesthetics, barbiturates, and opiod (narcotic) analgesics/ may potentiate and prolong the CNS depressant effects of either these medications or loxapine

Anwendungen & Verwendung

Verwenden

Tranquilizer (minor).

dosage adjustments to approximately 1/2 to 1/4 of the ususal dose may be necessary.
Concurrent use /with amphetamines/ may decrease the effects of amphetamines since loxapine produces alpha-adrenergic blockade.
Concurrent use /with antacids or adsorbent antidiarrheals/ may inhibit the absorption of orally administered loxapine.
For more Interactions (Complete) data for LOXAPINE (18 total), please visit the HSDB record page.
HepatotoxicityLiver test abnormalities have been reported to occur in a small proportion of patients on long term therapy with loxapine, but elevations are uncommonly above 3 times the upper limit of normal. The aminotransferase abnormalities are usually mild, asymptomatic and transient, reversing even with continuation of medication. Instances of clinically apparent acute liver injury have been reported due to loxapine and to the structurally related tricylic amoxapine (not available in the United States), but cases are rare. In reported cases, the onset of jaundice was within 4 to 8 weeks, and the pattern of serum enzyme elevations was typically hepatocellular. Immunoallergic features and autoantibody formation were not prominent. All cases were self-limited without fatalities or residual chronic liver injury.
ExpositionspfadeOral, Intramuscular. Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers.
ToxizitätsübersichtLoxapine 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.
Signs and SymptomsLD<sub>50</sub>=65 mg/kg (Orally in mice)
Human Toxicity ExcerptsOverdosage of loxapine presumably may be manifested by seizures, severe extrapyramidal symptoms, and other effects ranging from mild CNS depression to profound hypotension and coma.
Carcinogen ClassificationNo indication of carcinogenicity to humans (not listed by IARC).
Drug Induced Liver InjuryDrug-Induced Liver Injury Severity and Toxicity (DILIst)loxapineDILI NegativeOralDOI:10.1016/j.drudis.2019.09.022
Effects During Pregnancy and Lactation◉ Summary of Use during Lactation◈ What is loxapine?
Toxicity DataLD<sub>50</sub>=65 mg/kg (Orally in mice)
Non-Human Toxicity ValuesLD50 Rat oral 151 mg/kgLD50 Rat ip 35 mg/kgLD50 Rat sc 350 mg/kgLD50 Rat iv 18 mg/kgFor more Non-Human Toxicity Values (Complete) data for LOXAPINE (8 total), please visit the HSDB record page.
ToxizitätLD50 orally in mice: 65 mg/kg (Stille)
Gefahrstoffdaten1977-10-2(Hazardous Substances Data)