基本情報
- CAS
105431-72-9- 標準SMILES
O=C1N(c2ccccc2)c2ccccc2C1(Cc1ccncc1)Cc1ccncc1- InChIKey
YEJCDKJIEMIWRQ-UHFFFAOYSA-N- 分子式
- C26H21N3O
- 平均分子量
- 391.5 g/mol
- 単同位体質量
- 391.1684623
概要
Linopirdine is a member of indoles.
名称と識別子
- 優先名称
- Linopirdine
- IUPAC
- 1-phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one
- 現地名
- リノピルジン
- 英語名
- 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one dihydrochloride
- 分子式
- C26H21N3O
- 分子量
- 391.46
名称と別名
Linopirdine105431-72-9Dup 9961-phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-oneDuP-996LinopirdinaI5TB3NZ94T2H-Indol-2-one, 1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-1-phenyl-3,3-bis(4-pyridylmethyl)indolin-2-one3,3-bis(4-pyridylmethyl)-1-phenylindolin-2-onelinopirdinum3,3-dipyridylmethyl-1-phenyl-2-indolinone
名称をさらに表示
1,3-ジヒドロ-1-フェニル-3,3-ビス[(4-ピリジニル)メチル]-2H-インドール-2-オン1-フェニル-3,3-ビス(4-ピリジニルメチル)-1H-インドール-2(3H)-オン1-フェニル-3,3-ビス(4-ピリジニルメチル)-1,3-ジヒドロ-2H-インドール-2-オン1-フェニル-3,3-ビス(4-ピリジニルメチル)-2,3-ジヒドロ-1H-インドール-2-オン1,3-ジヒドロ-1-フェニル-3,3-ビス(4-ピリジルメチル)-2H-インドール-2-オンリノピルジン1-フェニル-3,3-ビス[(4-ピリジル)メチル]-1H-インドール-2(3H)-オンリノプリジン1-フェニル-3,3-ビス(4-ピリジルメチル)-1H-インドール-2(3H)-オン1-フェニル-3,3-ビス[(ピリジン-4-イル)メチル]-2,3-ジヒドロ-1H-インドール-2-オンlinopiridineLinopirdine2HClLINOPIRDINE (DUP996)Linopirdine, 10 mM in DMSOLINOPIRDINE DIHYDROCHLORIDE1-Phenyl-3,3-bis(4-pyridinylmethyl)-2,3-dihydro-1H-indole-2-one
物性
構造計算による物性
- XLogP
- 4.1
- 極性表面積
- 46.1 Ų
- 水素結合供与体数
- 0
- 水素結合受容体数
- 3
- 回転可能結合数
- 5
- 重原子数
- 30
- 形式電荷
- 0
- 複雑度
- 555
物理化学的性質
- 融点
- 186 · 186-186.5 °C
- 沸点
- 655.9 · 655.9±50.0 °C(Predicted)
- 比重(密度)
- 1 · 1+-.0.06 g/cm3(Predicted)
- 貯蔵温度
- Desiccate at RT
- 溶解性
- 10 mg/mL · DMSO：>10mg/mL
- 酸解離定数(Pka)
- 6.01 · 6.01±0.10(Predicted)
- 外見
- A crystalline solid
- 色
- ホワイトからオフホワイト
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。
安全データ
- wgk
- 3
化学と産業
薬理情報
ATC Code
N - Nervous system
QN - Nervous system
MeSH Pharmacological Classification
Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids.
A class of drugs that act by inhibition of potassium efflux through cell membranes. Blockade of potassium channels prolongs the duration of ACTION POTENTIALS. They are used as ANTI-ARRHYTHMIA AGENTS and VASODILATOR AGENTS.
応用分野
説明Linopirdine is an enhancer of the stimulus-evoked but not basal release of several neurotransmitters, including acetylcholine, dopamine, serotonin, and glutamate. It increases acetylcholine release in rat hippocampal CA1 neurons by blocking voltage-gated, calcium-activated and leak (M-type; Kv7.2/7.3; KCNQ2/3) K+ current with an IC50 value of 2.4 μM. Inhibition of M-channels is reported to result in the depolarization of CA3 pyramidal neurons and activated presynaptic voltage-gated P/Q- and N-type calcium channels, which leads to Ca2+ influx and increased neurotransmitter release. Linopirdine has been shown to produce a number of effects including EEG patterns of enhanced vigilance, induction of c-fos expression in cerebral cortex, reduction of the increase of cerebral glucose utilization induced by hypoxia, and improved performance in animal models of learning and memory. Linopirdine has also been identified as an agonist of transient receptor potential vanilloid type 1 (EC50 = 115 μM in HEK293 cells voltage clamped at -60 mV).
使用Alzheimer’s disease treatment (cognition enhancer).
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