别名：(1S,9S)-3,11-二氮杂三环[7.3.1.03,8]三癸-5,7-二烯-4-酮；野靛碱；(-)-金雀花碱；Laburnin, Ulexine, Sophorine, (1S,9S)-3,11-Diazatricyclo[7.3.1.03,8]trideca-5,7-dien-4-one, (1R,5S)-1,2,3,4,5,6-Hexahydro-1,5-methano-8H-pyrido[1,2a][1,5]diazocin-8-one, (−)-Cytisine, Baptitoxin
Empirical Formula (Hill Notation): C11H14N2O CAS号: 485-35-8 分子量: 190.24 EC 号: 207-616-0 MDL编号: MFCD00136048 PubChem化学物质编号: 329763123 NACRES: NA.22
货号（SKU）: 712264
CAS号: 485-35-8
MDL号: MFCD00136048
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说明
Cystine ((1R,5S)-1,2,3,4,5,6-hexahydro-1,5-methano-8H-pyrido[1,2a][1,5]diazocin-8-one) 显示经典抗抑郁药在各种动物模型中发挥抗抑郁功效。红外和拉曼光谱研究表明它具有两个稳定的构象异构体。
发现 Cytisine 在帮助吸烟者戒烟方面比尼古丁替代疗法更有效。它是一种α4β2烟碱受体部分激动剂。它是一种植物生物碱，可在商业上提取用作戒烟药物。已有报道通过“原位”Stille 或 Suzuki 联芳基吡啶偶联制备尼古丁部分激动剂金雀花碱。 Cytisine 是对含 α4 亚基的烟碱乙酰胆碱 (nACh) 受体的竞争性部分激动剂，而在同聚的 α7-nACh 受体中，它表现为具有相对较低效力的完全激动剂。
胱氨酸可用作尼古丁成瘾治疗中的尼古丁替代品。
金雀花碱适用于一项研究，以比较伐尼克兰和金雀花碱对作为高酒精饮用者饲养了多代的大鼠的乙醇消耗量的影响。
一般描述
Cystine ((1R,5S)-1,2,3,4,5,6-hexahydro-1,5-methano-8H-pyrido[1,2a][1,5]diazocin-8-one) displays classical antidepressant action in various animal models of antidepressant efficacy. Infrared and Raman spectral studies suggest that it has two stable conformers.
Cytisine was found to be more effective than nicotine-replacement therapy in helping smokers to quit smoking. It is an α4 β2 nicotinic receptor partial agonist. It is a plant alkaloid which is commercially extracted for use as a smoking cessation medication. Preparation of nicotine partial agonist cytisine via “in situ” Stille or Suzuki biaryl pyridine coupling has been reported. Cytisine is a competitive partial agonist at α4 subunit-containing nicotinic acetylcholine (nACh) receptors while at homomeric α7-nACh receptors it behaves as a full agonist with a relatively lower potency.
应用
Cystine may be used as nicotine substitute in nicotine addiction therapy.
Cytisine is suitable for use in a study to compare the effects of varenicline and cytisine on ethanol consumption by rats bred for many generations as high ethanol drinkers.
生化/生理作用
α3β4 和 α7 烟碱型乙酰胆碱受体的强效激动剂，α4β2 烟碱型乙酰胆碱受体的部分激动剂。
属性
旋光性
[α]/D -108±3°, c = 1% in ethanol
SMILES string
O=C1C=CC=C2C3CNCC(C3)CN12
InChI
1S/C11H14N2O/c14-11-3-1-2-10-9-4-8(5-12-6-9)7-13(10)11/h1-3,8-9,12H,4-7H2/t8-,9+/m0/s1
InChI key
ANJTVLIZGCUXLD-DTWKUNHWSA-N
安全信息
危险分类
Acute Tox. 3 Dermal - Acute Tox. 3 Inhalation - Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
个人防护装备
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
