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Prochlorperazine Edisylate

HCID 91499
노트반응
기본 정보개요이름 및 식별자물성안전 및 규제화학 및 산업관련 반응화합물 노트
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기본 정보

CAS
1257-78-9
표준 SMILES
CN1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1.O=S(=O)(O)CCS(=O)(=O)O
InChIKey
SWOUGRBFXFILIB-UHFFFAOYSA-N
분자식
C22H30ClN3O6S3
평균 분자량
564.1 g/mol
단동위원소 질량
563.0985269

개요

Prochlorperazine Edisylate is the edisylate salt form of prochlorperazine, a derivative of phenothiazine with antipsychotic and antiemetic properties. Prochlorperazine edisylate blocks postsynaptic dopamine receptors in cortical and limbic areas of the brain, thereby preventing the excess of dopamine in the brain. This leads to a reduction in psychotic symptoms, including hallucinations and delusions. Prochlorperazine edisylate appears to exert its antiemetic activity by blocking the dopamine and histamine receptors in the chemical trigger zone (CTZ) in the brain, thereby relieving nausea and vomiting.

이름 및 식별자

우선 이름
Prochlorperazine Edisylate
IUPAC
2-chloro-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine;ethane-1,2-disulfonic acid
영어명
PROCHLORPERAZINE EDISYLATE
분자식
C20H24ClN3S.C2H6O6S2
분자량
564.14

이름 및 동의어

Prochlorperazine edisylate1257-78-9prochlorperazine ethanedisulfonateProchlorperazine Edisylate SaltPG20W5VQZSNSC-757299Prochlorperazine edisilateDTXSID4074483Prochlorperazine edisylate (USP)Prochlorperazine edisylate [USP]2-Chloro-10-(3-(1-methyl-4-piperazinyl)propyl)phenothiazine edisylateNSC665801
이름 더 보기
prochlorperazine edisylate uspPROCHLORPERAZINE EDISYLATE MEETS USP TE2-chloro-10-(3-(1-methyl-4-piperazinyl)propyl)phenothiazineedisylate2-chloro-10-(3-(1-methyl-4-piperazinyl)propyl)-phenothiazinethanedisulfona2-chloro-10-(3-(4-methyl-1-piperazinyl)propyl)phenothiazine1,2-ethanedisulfoethane-1,2-disulphonic acid, compound with 2-chloro-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine (1:1)
2-Chloro-10-(3-(4-methyl-1-piperazinyl)propyl)phenothiazine 1,2-ethanedisulfonate (1:1)Phenothiazine, 2-chloro-10-(3-(1-methyl-4-piperazinyl)propyl)-, ethanedisulfonate2-Chloro-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazine 1,2-ethanedisulfonate (1:1)RefChem:55922DTXCID1033872215-019-1Prochlorperazine Edisylate, USPProchlorperazine ethane disulfonate

물성

구조 계산 물성

극성 표면적
161 Ų
수소 결합 공여자 수
2
수소 결합 수용자 수
10
회전 가능 결합 수
7
무거운 원자 수
35
형식 전하
0
복잡도
668

실험 및 물리화학적 성질

Solubility73.3 [ug/mL] (The mean of the results at pH 7.4)
Human Drugs · 2건

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

Animal DrugsFDA approved animal drugs -> Active ingredient
Collision Cross Section182.9 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

물리화학적 성질

저장 조건
2 · 2-8°C
EPA
Prochlorperazine edisylate (1257-78-9)

안전 및 규제

안전 정보는 참고용이며, 공급업체의 물질안전보건자료(SDS), 관련 법규 및 전문가 평가를 대체하지 않습니다.

GHS 분류

GHS Classification · 4건

Warning

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]

P264, P270, P301+P317, P330, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 39 reports by companies from 1 notifications to the ECHA C&L Inventory.

유해성 정보

Hazard Classes and CategoriesAcute Tox. 4 (100%)

독성 정보

Exposure RoutesIntravenous, Oral, Rectal. Rapidly absorbed following oral administration.
Toxicity Summary · 1건

The mechanism of action of prochlorperazine has not been fully determined, but may be primarily related to its antidopaminergic effects. Prochlorperazine blocks the D2 somatodendritic autoreceptor, resulting in the blockade of postsynaptic dopamine receptors in the mesolimbic system and an increased dopamine turnover. Prochlorperazine also has anti-emetic effects, which can be attributed to dopamine blockade in the chemoreceptor trigger zone. Prochlorperazine also blocks anticholinergic and alpha-adrenergic receptors, the blockade of alpha(1)-adrenergic receptors resulting in sedation, muscle relaxation, and hypotension.

Signs and Symptoms · 1건

Symptoms of central nervous system depression to the point of somnolence or coma. Agitation and restlessness may also occur. Other possible manifestations include convulsions, EKG changes and cardiac arrhythmias, fever and autonomic reactions such as hypotension, dry mouth and ileus; LD<sub>50</sub>=400mg/kg (orally in mice)

Carcinogen ClassificationNo indication of carcinogenicity to humans (not listed by IARC).

화학 및 산업

약리 정보

Metabolism/MetabolitesHepatic. Undergoes metabolism in the gastric mucosa and on first pass through the liver, CYP2D6 and/or CYP3A4. Half Life: 6 to 8 hours
FDA Pharmacological Classification · 2건

PROCHLORPERAZINE EDISYLATE

Phenothiazines [CS]; Phenothiazine [EPC]

MeSH Pharmacological Classification · 3건

Drugs used to prevent NAUSEA or VOMITING.

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.

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.

용도 및 제조

UsesFor the symptomatic management of psychotic disorders, short term management of nonpsychotic anxiety in patients with generalized anxiety disorder, and for the control of severe nausea and vomiting of various causes.

응용 분야

용도Phenothiazine antipsychotic; D2 antagonist; antispasmodic

공급사

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이 페이지에서기본 정보개요이름 및 식별자물성안전 및 규제화학 및 산업관련 반응화합물 노트

데이터베이스 식별자

CAS
1257-78-9
PubChem CID
91499
DTXSID
DTXSID4074483
ChEMBL
CHEMBL1201154
ChEBI
CHEBI:232994
UNII
PG20W5VQZS
EC Number
215-019-1
Toxicity Data
LD<sub>50</sub>=400mg/kg (orally in mice)

안전 데이터

rtecs
SO2975000
risk_code
22
hazard_code
Xn
safety_code
22
17 곳
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