マレイン酸アセプロマジン

Acepromazine Maleate

HCID 6420038

基本情報

CAS
3598-37-6
標準SMILES
CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2.O=C(O)/C=C\C(=O)O
InChIKey
FQRHOOHLUYHMGG-BTJKTKAUSA-N
分子式
C23H26N2O5S
平均分子量
442.5 g/mol
単同位体質量
442.15624293

概要

Acepromazine Maleate is the maleate salt of acepromazine, a phenothiazine derivative with depressant effect on the central nervous system. Acepromazine acts as a dopamine receptor antagonist in the CNS, thereby causing sedation, muscular relaxation and a reduction in spontaneous activity. Its fast-acting neuroleptic effect with low toxicity is of particular value in veterinary medicine.

名称と識別子

優先名称
Acepromazine Maleate
IUPAC
(Z)-but-2-enedioic acid;1-[10-[3-(dimethylamino)propyl]phenothiazin-2-yl]ethanone
現地名
マレイン酸アセプロマジン
英語名
ACEPROMAZINE MALEATE
分子式
C23H26N2O5S
分子量
442.53

名称と別名

Acepromazine maleate3598-37-6SoprontinPlegicilSedalin37862HP2OMNSC-264522Ethanone, 1-(10-(3-(dimethylamino)propyl)-10H-phenothiazin-2-yl)-, (Z)-2-butenedioate (1:1)10-(3-(Dimethylamino)propyl)phenothiazin-2-yl methyl ketone maleate (1:1)NSC26452210-[3-(Dimethylamino)propyl]phenothiazin-2-yl methyl ketone maleate (1:1)PromAce Injectable
名称をさらに表示
アセプロマジンマレアート1-[10-[3-(ジメチルアミノ)プロピル]-10H-フェノチアジン-2-イル]エタノン·(Z)-2-ブテン二酸1-[10-[3-(ジメチルアミノ)プロピル]-10H-フェノチアジン-2-イル]エタノン/マレイン酸,(1:1)マレイン酸アセプロマジンアセプロマジンマレイン酸塩1-[10-[3-(ジメチルアミノ)プロピル]-10H-フェノチアジン-2-イル]エタノン・(Z)-2-ブテン二酸ATAVETTindalaacepromeCALMIVETnotensilmaleate
Maleate, AcepromazineRefChem:53845Acepromazine Maleate Injection222-748-9PromAceVetranquilAnatranAcetopromazine maleate

データベース識別子

CAS
3598-37-6
PubChem CID
6420038
DTXSID
DTXSID6047783
ChEMBL
CHEMBL1883146
UNII
37862HP2OM
EC Number
222-748-9

物性

構造計算による物性

極性表面積
123 Ų
水素結合供与体数
2
水素結合受容体数
8
回転可能結合数
7
重原子数
31

実験および物理化学的性質

Animal DrugsActive Ingredients (Acepromazine Maleate) -> FDA Greenbook

物理化学的性質

融点
135 · 135-136°C
貯蔵温度
room temp
溶解性
2 O: · H2O: >10mg/mL
酸解離定数(Pka)
9.3 · 9.3(at 25℃)
外見
粉
色
黄色

化学的性質

化学的特性Yellow Crystalline Solid

安全と法規制

GHS分類

GHS Classification · 4 件

Warning

H302 (97.7%): Harmful if swallowed [Warning Acute toxicity, oral]

P261, P264, P270, P271, P280, P301+P317, P302+P352, P304+P340, P317, P321, P330, P362+P364, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 44 reports by companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

危険有害性情報

Regulatory InformationAcepromazine maleate: Does not have an individual approval but may be used under an appropriate group standard
Other Safety InformationIMAP assessments - Ethanone, 1-[10-[3-(dimethylamino)propyl]-10H-phenothiazin-2-yl]-, (Z)-2-butenedioate (1:1): Human health tier I assessment
Hazard Classes and CategoriesAcute Tox. 4 (97.7%)

安全データ

wgk
2
rtecs
2664-15-5
ridadr
UN 3077
毒性
LD50 orally in rats: 400 mg/kg; i.v. in mice: 59 mg/kg (Wirth)
hs_code
2934302300
risk_code
22-50/53-20/21/22-43-36/37/38-23/24/25

化学と産業

薬理情報

MeSH Pharmacological Classification · 2 件

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.

用途と製造

Use ClassificationAnimal Drugs -> FDA Approved Animal Drug Products (Green Book) -> Active Ingredients
応用分野 · 2 件

説明Acepromazine is a phenothiazine antipsychotic, analog of chlorpromazine , and a dopamine receptor antagonist. It also binds to muscarinic receptors in rat brain (IC50 = 350 nM) and inhibits contractions of guinea pig ileum induced by acetylcholine (; IC50 = 840 nM). Acepromazine inhibits morphine-induced vomiting in dogs. It also inhibits development of a conditioned avoidance response, unconditioned escape response, and catalepsy in rats (ED50s = 0.98, 3.1, and 17 mg/kg, respectively). Formulations containing acepromazine have been used as tranquilizers and anesthetics premedicant in small and large animal veterinary care.

使用Acepromazine maleate has been used:as a component of anesthesia cocktail to test its effects on behavioral changes in ratsas a component of anesthesia cocktail to study its effects on lung resistance of ratsas an anti-psychotic pharmaceutical agent to study its cytotoxic effects on malignant glioma in glioblastoma (GBM) cells

上流・下流製品情報

サプライヤー100 社

国药集团化学试剂有限公司86-21-63210123 · [email protected]
上海阿拉丁生化科技股份有限公司400-6206333 13167063860 · [email protected]
湖南韵邦生物科技股份有限公司85561037 15386497078 · [email protected]
南通飞宇生物科技有限公司0513-68819626 15152877458 · [email protected]
成都超九八生物科技有限公司13348960310 13348960310 · [email protected]

関連反応

2 件

化合物ノート

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