基本情報
- CAS
7104-38-3- 標準SMILES
COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2.O=C(O)/C=C\C(=O)O- InChIKey
IFLZPECPTYCEBR-VIEYUMQNSA-N- 分子式
- C23H28N2O5S
- 平均分子量
- 444.5 g/mol
- 単同位体質量
- 444.17189317
概要
Methotrimeprazine is only found in individuals that have used or taken this drug. It is a phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604). Methotrimeprazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, its binding to 5HT2 receptors may also play a role.
名称と識別子
- 優先名称
- Methotrimeprazine maleate
- IUPAC
- (Z)-but-2-enedioic acid;(2R)-3-(2-methoxyphenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine
- 現地名
- レボメプロマジン·マレイン酸
- 英語名
- Levomepromazine maleate
- 分子式
- C19H24N2OS.C4H4O4
- 分子量
- 444.55
名称と別名
levomepromazine maleate7104-38-3Methotrimeprazine maleateMinozinanNeuractilNeurocilMilezinSofminMethoprazineHirnaminLevomepromazine Hydrogen MaleateDTXSID4045399
名称をさらに表示
ヒルナミンレボメプロマジン·マレイン酸レボトミンレボホルテ(βR)-2-メトキシ-N,N,β-トリメチル-10H-フェノチアジン-10-(1-プロパンアミン)·(Z)-2-ブテン二酸ソフミンレボメプロマジン·マレイン酸塩マレイン酸レボメプロマジンレボメプロマジンマレイン酸塩レボメプロマジンマレイン酸塩 (JP17)レボメプロマジン・マレイン酸塩(βR)-2-メトキシ-N,N,β-トリメチル-10H-フェノチアジン-10-(1-プロパンアミン)・(Z)-2-ブテン二酸レボメプロマジン/マレイン酸レボメプロマジン・マレイン酸NeruocilLevohalteNeurocil (tablet)Levomepromazine meleateRP 7044 hydrogen maleateLevomepromazine·maleic acidLevomepromazine maleate CRS
Veractil5KN5Y9V01KDTXCID202539910H-Phenothiazine-10-propanamine, 2-methoxy-N,N,beta-trimethyl-, (betaR)-, (2Z)-2-butenedioate (1:1)LevinanRefChem:799026(2R)-3-(2-Methoxy-10H-phenothiazin-10-yl)-N,N,2-trimethylpropylamine monomaleate230-412-8
物性
構造計算による物性
- 極性表面積
- 116 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
- 形式電荷
- 0
- 複雑度
- 497
物理化学的性質
- 融点
- 176 · 176-179°C
- 比旋光度
- 20 · D20 -17° (c = 5 in chloroform)
- 貯蔵温度
- -20 °C · -20°C Freezer
- 溶解性
- クロロホルム（微量）、DMF（微量）、メタノール（微量）
- 外見
- solid
- 色
- オフホワイトからペールベージュ
- 主な用途
- 医薬品（低分子化合物）
- InChIKey
- IFLZPECPTYCEBR-VIEYUMQNSA-N
- SMILES
- S1c2c(cc(cc2)OC)N(c3c1cccc3)C[C@@H](CN(C)C)C.OC(=O)\C=C/C(=O)O
化学的性質
化学的特性Pale Beige Solid
安全と法規制
安全情報は参考情報です。供給元の安全データシート（SDS）、適用法令、専門家による評価に代わるものではありません。
GHS分類
GHS Classification
Warning
H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]
P261, P264, P264+P265, P270, P272, P273, P280, P301+P317, P302+P352, P305+P351+P338, P321, P330, P333+P317, P337+P317, P362+P364, P391, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 34 reports by companies from 8 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
危険有害性情報
Regulatory InformationMethotrimeprazine maleate: Does not have an individual approval but may be used under an appropriate group standard
Other Safety InformationIMAP assessments - 10H-Phenothiazine-10-propanamine, 2-methoxy-N,N,.beta.-trimethyl-, (Z)-2-butenedioate (1:1), (-)-: Human health tier I assessment
Hazard Classes and CategoriesAcute Tox. 4 (100%)
毒性情報
Exposure RoutesOral; parental (intramuscular). Methotrimeprazine has an incomplete oral bioavailability, because it undergoes considerable first-pass-metabolism in the liver. Oral bioavailability is approximately 50 to 60%.
Toxicity Summary
Methotrimeprazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, its binding to 5HT2 receptors may also play a role. Methotrimeprazine exerts its actions through a central adrenergic-blocking, a dopamine-blocking, a serotonin-blocking, and a anticholinergic blocking.
Signs and SymptomsSymptoms of overdose include convulsions, spastic movements, and coma.
化学と産業
薬理情報
Metabolism/MetabolitesHepatic. Methotrimeprazine is metabolized in the liver and degraded to a sulfoxid-, a glucuronid- and a demethyl-moiety.
Half Life: Approximately 20 hours.
用途と製造
Uses
For the treatment of psychosis, particular those of schizophrenia, and manic phases of bipolar disorder. As a potentiator of anesthetics: In general anesthesia where it can be used as both a pre- and post-operative sedative and analgesic. (L1857) As an anti-emetic: For the treatment of nausea and vomiting of central origin.(L1857) As a sedative: For the management of insomnia. (L1857)
応用分野
用途フェノチアジン系化合物です。 ドーパミンD2 受容体遮断作用を示します。
用途フェノチアジン系化合物です。 ドパミンD2 受容体遮断作用を示します。
使用The (R) optical isomer of Methotrimeprazine (M260785), an analgesic/neuroleptic.
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