(±)-Epibatidine dihydrochloride hydrate

• 产品号: E1145
• 分子式: C11H17Cl3N2O
• 分子量: 299.62448
• 纯 度: ≥98% (HPLC)

产品别名

• 标题: (±)-Epibatidine dihydrochloride hydrate
• IUPAC标准名: (2R)-2-(6-chloropyridin-3-yl)-7-azabicyclo[2.2.1]heptane hydrate dihydrochloride
• IUPAC传统名: (2R)-2-(6-chloropyridin-3-yl)-7-azabicyclo[2.2.1]heptane hydrate dihydrochloride
• 别名: exo-(±)-2-(6-Chloro-3-pyridinyl)-7-azabicyclo[2.2.1]heptane dihydrochloride hydrate

产品登记号

• PubChem SID: 24894390

产品性质

• Empirical Formula (Hill Notation): C11H13ClN2 · 2HCl · xH2O
• 纯度: ≥98% (HPLC)
• 外观: off-white powder
• 溶解度: DMSO: >4 mg/mL
• 溶解度: methanol: soluble4 mg/mL
• GHS警示词: Danger
• GHS危险声明: H300-H310
• 欧盟危险性物质标志: 剧毒(Highly toxic) (T+)
• 个人保护装置: Eyeshields, Faceshields, full-face particle respirator type N100 (US), Gloves, respirator cartridge type N100 (US), type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges
• GHS警示性声明: P264-P280-P301 + P310-P302 + P350-P310
• RID/ADR: UN 2811 6.1/PG 1
• 危险公开号: 27/28
• 安全公开号: 28-36/37-45
• 联合国危险货物等级: 6.1
• 联合国危险货物编号: 2811
• 联合国危险货物包装类别(PG): 1
• 德国WGK号: 3

产品详细信息

详细说明 (English)

Biochem/physiol Actions
The activity of epibatidine at neuronal and neuromuscular nicotinic acetylcholine receptors was compared with the activity of nicotine and suxamethonium. Activation of ganglionic nicotinic receptors by epibatidine was shown in the guinea-pig ileum (contraction mediated by the cholinergic neurons of the ileum) and in pithed and atropinized rats (rise in blood pressure). Epibatidine also activated nicotinic receptors at the peripheral terminals of afferent C-fibres (rabbit ear) and in the brain (antidiuresis in rats). The agonistic effects of epibatidine were followed by long-lasting receptor desensitization. No antinociceptive effect of epibatidine was seen in rats at a dose free of motor impairment. On muscle end plate nicotinic receptors of the rat diaphragm (not responding to depolarizing agents by contraction), epibatidine was equipotent with suxamethonium in causing neuromuscular inhibition. On an extraocular muscle of the rabbit (responding to depolarizing agents by contraction) epibatidine in vitro and in situ caused a contraction at a 100-fold lower dose than suxamethonium. The Straub tail reaction in mice to epibatidine could be attributed to the sustained stimulation of motor end plate receptors of the "slow contracting" type of muscle fibres by epibatidine. Epibatidine was the most potent agonist on all neuronal and neuromuscular nicotinic receptors examined.

详细说明 (简体中文)

Biochem/physiol Actions
The activity of epibatidine at neuronal and neuromuscular nicotinic acetylcholine receptors was compared with the activity of nicotine and suxamethonium. Activation of ganglionic nicotinic receptors by epibatidine was shown in the guinea-pig ileum (contraction mediated by the cholinergic neurons of the ileum) and in pithed and atropinized rats (rise in blood pressure). Epibatidine also activated nicotinic receptors at the peripheral terminals of afferent C-fibres (rabbit ear) and in the brain (antidiuresis in rats). The agonistic effects of epibatidine were followed by long-lasting receptor desensitization. No antinociceptive effect of epibatidine was seen in rats at a dose free of motor impairment. On muscle end plate nicotinic receptors of the rat diaphragm (not responding to depolarizing agents by contraction), epibatidine was equipotent with suxamethonium in causing neuromuscular inhibition. On an extraocular muscle of the rabbit (responding to depolarizing agents by contraction) epibatidine in vitro and in situ caused a contraction at a 100-fold lower dose than suxamethonium. The Straub tail reaction in mice to epibatidine could be attributed to the sustained stimulation of motor end plate receptors of the "slow contracting" type of muscle fibres by epibatidine. Epibatidine was the most potent agonist on all neuronal and neuromuscular nicotinic receptors examined.