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Loxapine succinate

Loxapine succinate structure

CAS No:
27833-64-3
Formula:
C18H18ClN3O.C4H6O4
Chemical Name:
Loxapine succinate
Synonyms:
Butanedioic acid,compd. with 2-chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine (1:1);Succinic acid,compd. with 2-chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine (1:1);Dibenz[b,f][1,4]oxazepine,2-chloro-11-(4-methyl-1-piperazinyl)-,butanedioate (1:1);Loxapine succinate;CL 71563;2-Chloro-11-(4-methyl-1-piperazinyl)-dibenz[b,f][1,4]oxazepine succinate;Loxapac;Loxitane;Loxitane Capsules;Daxolin
Categories:
Biochemical Engineering > Inhibitors

Description

Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.IC50 value: Target: D2DR/D4DR; 5-HT receptorin vitro: In the presence of Loxapine, [3H]ketanserin binds to 5-HT2 receptor in Frontal cortex of brain in human and bovine with ki value of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows:5-HT2≥D4>>>D1>D2 in comparing competition experiments

Loxapine Succinate is the succinate salt form of loxapine, a tricyclic dibenzoxazepine antipsychotic agent with antiemetic, sedative, anticholinergic, and antiadrenergic actions. Loxapine succinate exerts its actions by blocking the dopamine receptors at postsynaptic receptor sites in the limbic system, cortical system and basal ganglia, thereby reducing the hallucinations and delusions that are associated with schizophrenia. This agent also exerts extrapyramidal side effects.|An antipsychotic agent used in schizophrenia.

Loxapine succinate Basic Attributes

Molecular Weight：

445.9

Exact Mass：

445.140442

EC Number：

248-682-0

UNII：

X59SG0MRYU

NSC Number：

759578

DSSTox ID：

DTXSID3045227

NCI Thesaurus Code：

C47590

HScode：

29329990

Characteristics

PSA：

103

Appearance：

white solid

Melting Point：

150-152°C

Boiling Point：

458.6°C at 760 mmHg

Flash Point：

231.1ºC

Water Solubility：

H2O: soluble

Storage Conditions：

-20°C Freezer

Collision Cross Section：

176.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

UN 2811 6.1 / PGII

wgk germany：

RTECS Number：

WM5750000

Precautionary statement(s)：

P264, P270, P280, P301+P310, P305+P351+P338, P321, P330, P337+P313, P405, P501

Hazard Statements：

H301

GHS Classification：

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P280, P301+P310, P305+P351+P338, P321, P330, P337+P313, P405, and P501|Aggregated GHS information provided by 7 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

MeSH：

Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)|Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. (See all compounds classified as Dopamine Antagonists.)

MeSH Entry Terms：

2-Chloro-11-(4-methyl-1-piperazinyl)-dibenz(b,f)(1,4)oxazepine

Loxapine succinate Use and Manufacturing

Uses

choleretic

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:445.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:4
Exact Mass:445.1404486
Monoisotopic Mass:445.1404486
Topological Polar Surface Area:103
Heavy Atom Count:31
Complexity:542
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Unspecified

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Loxapine succinate
Manufacturer	Zhejiang Hisun Pharmaceutical Co., Ltd.

Loxapine Succinate Capsules
Ingredients	2-Chloro-11-(4-methyl-1-piperazinyl)dibenzo[b,f][1,4]oxazepine dicarboxylate
Indication	Loxapine succinate can also accelerate the metabolism of phenytoin, and when the two drugs are used together for more than 3 months, the plasma level of phenytoin may not reach the therapeutic concentration. Loxapine succinate increases the inhibitory effect of barbiturates, anesthetic analgesics, antihistamines and other antipsychotic drugs on the central nervous system.
Specifications	13.6mg
Manufacturer	Han Hui Pharmaceuticals Company Limited

Registered Holders

MEDICHEM SA

Spain
Active
Zhejiang Hisun Pharmaceutical Co., Ltd.

China
Active
CENTAUR PHARMACEUTICALS PRIVATE LTD

United States
Active

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Recommended Suppliers of Loxapine succinate

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Loxapine succinate salt

CAS No.: 27833-64-3

Content: 99.00%

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