バレニクリン

バレニクリン 化学構造式
249296-44-4
CAS番号.
249296-44-4
化学名:
バレニクリン
别名:
バレニクリン;7,8,9,10-テトラヒドロ-6α,10α-メタノ-1,4,8-トリアザ-6H-シクロヘプタ[b]ナフタレン;(1R,12S)-5,8,14-トリアザテトラシクロ[10.3.1.02,11.04,9]ヘキサデカ-2(11),3,5,7,9-ペンタエン
英語名:
Varenicline
英語别名:
Chantix;Varenciline;10-tetrahydro-;7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline;(1R,12S)-5,8,14-triazatetracyclo[10.3.1.0^{2,11}.0^{4,9}]hexadeca-2,4(9),5,7,10-pentaene;CS-861;Hsdb 7591;Cp 526555;Vareniclene;VARENICLINE
CBNumber:
CB61011764
化学式:
C13H13N3
分子量:
211.26
MOL File:
249296-44-4.mol

バレニクリン 物理性質

融点 :
138.5 °C
沸点 :
400.6±40.0 °C(Predicted)
比重(密度) :
1.247±0.06 g/cm3(Predicted)
貯蔵温度 :
Store at -20°C
溶解性:
Soluble in DMSO
外見 :
Powder
酸解離定数(Pka):
9.60±0.20(Predicted)
BCS Class:
1
安定性::
Hygroscopic

安全性情報

有毒物質データの 249296-44-4(Hazardous Substances Data)

バレニクリン 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

バレニクリン 化学特性,用途語,生産方法

効能

禁煙補助薬, ニコチン性アセチルコリン受容体部分作動薬

説明

Varenicline, a partial agonist of the a4b2 nicotinic receptor, is a first-in-class drug launched by Pfizer as an aid to smoking cessation treatment. Varenicline exhibits dual action by decreasing craving and withdrawal symptoms, and by decreasing the reinforcement associated with smoking. The addictive properties of nicotine are thought to be mediated in part through its action as an agonist at α4β2 neuronal nicotinic acetylcholine receptors (nAChRs). Activation of α4β2 receptors by nicotine increases the release of dopamine in the mesolimbic system, an effect that is shared by most drugs of abuse. As nicotine levels decrease, dopamine levels decline, which in turn stimulates the urge to smoke. Additionally, a reduced dopaminergic tone due to abstinence from smoking stimulates craving and the withdrawal syndrome. A partial agonist of α4β2 receptors such as varenicline is expected to elicit a moderate and sustained increase in dopamine levels to relieve craving and withdrawal symptoms. In addition, by competitively binding to a4b2 receptors and inhibiting nicotineinduced dopaminergic activation, a partial agonist could attenuate the pharmacologic reward associated with smoking.

使用

Varenicline is a useful medication for smoking cessation.

定義

ChEBI: An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking.

バレニクリン 上流と下流の製品情報

原材料

準備製品


バレニクリン 生産企業

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249296-44-4(バレニクリン)キーワード:


  • 249296-44-4
  • 3-h][3]benzazepine
  • Varenicline Impurity
  • VARENICLINE
  • 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine
  • Vareniclene
  • Varenicline free base
  • Cp 526555
  • Hsdb 7591
  • Unii-W6hs99o8zo
  • 10-Methano-6H-pyrazino[2
  • 6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine, 7,8,9,10-tetrahydro-
  • CS-861
  • CP 526555;CHAMPIX;CHANTIX;CP526555;CP-526555
  • Varenicline base
  • Varenicline (CP 526555)
  • Varenicline 13C15N
  • (1R,12S)-5,8,14-triazatetracyclo[10.3.1.0^{2,11}.0^{4,9}]hexadeca-2,4(9),5,7,10-pentaene
  • 10-tetrahydro-
  • 7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline
  • Chantix
  • Varenciline
  • VERENICLINE
  • Vancomycin Impurity 20
  • 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine (Vareniclene)
  • バレニクリン
  • 7,8,9,10-テトラヒドロ-6α,10α-メタノ-1,4,8-トリアザ-6H-シクロヘプタ[b]ナフタレン
  • (1R,12S)-5,8,14-トリアザテトラシクロ[10.3.1.02,11.04,9]ヘキサデカ-2(11),3,5,7,9-ペンタエン
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