硝酸毛果芸香碱
| 中文名称 | 硝酸毛果芸香碱 |
|---|---|
| 中文同义词 | (3S,4R)-3-乙基二氢-4-[(1-甲基-1H-咪唑-5-基)甲基]-2(3H)-呋喃酮硝酸盐;硝酸异毛果芸香碱;硝酸匹鲁卡品(硝酸毛果芸香碱);毛果芸香碱硝酸盐;硝酸匹鲁卡品;硝酸毛果芸香碱;毛果芸香碱 硝酸酯;硝酸毛果芸香碱杂质Ⅰ( 硝酸异毛果芸香碱)（3R，4R）-3-乙基-4-[（1-甲基-1H-咪唑-5-基）甲基]二氢呋喃-2（3H）-酮，硝酸盐 |
| 英文名称 | Pilocarpine nitrate |
| 英文同义词 | 3-ETHYLDIHYDRO-4-[(1-METHYL-1H-IMIDAZOL-5-YL)-METHYL]-2-(3H)-FURANONE NITRATE;2(3H)-Furanone, 3-ethyldihydro-4-(1-methyl-1H-imidazol-5-yl)methyl-, (3S,4R)-, mononitrate;PILOCARPINENITRATE,CRYSTAL,USP;Pilagan;Pilocarpinnitrat;(3S)-3-Ethyl-4-[(3-methylimidazol-4-yl)methyl]oxolan-2-one nitrate;(3S,4R)-3-Ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-2(3H)-furanone mononitrate;Pilocarpini nitras |
| CAS号 | 148-72-1 |
| 分子式 | C11H17N3O5 |
| 分子量 | 271.27 |
| EINECS号 | 205-723-7 |
| 相关类别 | 标准品;对照品;中药对照品;小分子抑制剂;小分子抑制剂，天然产物;原料;Inhibitors;AgonistsDrugs of Abuse;Alkaloids;Alkaloids (Others);Biochemistry;Chemical Structure;Cholinergics;Neurotransmitters;Others;API |
| Mol文件 | 148-72-1.mol |
| 结构式 |  |
硝酸毛果芸香碱 性质
| 熔点 | 173,5-174°C |
|---|---|
| 比旋光度 | D +77 to +83° (c = 10) |
| 折射率 | 81 ° (C=2, H2O) |
| 储存条件 | 2-8°C |
| 溶解度 | 在水中的溶解度0.1 g/mL，清澈，非常淡黄色 |
| 形态 | 粉末 |
| 颜色 | 白色 |
| 旋光性 (optical activity) | [α]25/D +83°, c = 10 in H2O(lit.) |
| Merck | 14,7424 |
| BRN | 4171406 |
| CAS 数据库 | 148-72-1(CAS DataBase Reference) |
| EPA化学物质信息 | Pilocarpine nitrate (148-72-1) |
硝酸毛果芸香碱呈无色结晶或白色结晶性粉末；无臭；遇光易变质。其可用于青光眼、虹膜炎的治疗。
1．对本药过敏者。
2．支气管哮喘患者。
3．急性虹膜炎、虹膜睫状体炎等不应缩瞳的眼病患者。
Pilocarpine nitrate 是一种选择性的 M3 型毒蕈碱乙酰胆碱受体 (M3 muscarinic receptor) 激动剂。M3 muscarinic receptor
To evaluate the cytotoxicity of Pilocarpine, the morphology and viability of human corneal stromal (HCS) cells are examined by light microscopy and MTT assay, respectively. Morphological observations show that HCS cells exposed to Pilocarpine at a concentration from 0.625 to 20 g/L exhibit dose- and time-dependent proliferation retardation and morphological abnormality such as cellular shrinkage, cytoplasmic vacuolation, detachment from culture matrix, and eventually death, while no obvious difference is observed between those exposed to Pilocarpine below the concentration of 0.625 g/L and controls. Results of MTT assay reveal that the cell viability of HCS cells decrease with time and concentration after exposing to Pilocarpine above the concentration of 0.625 g/L (P<0.01 or 0.05), while that of HCS cells treated with Pilocarpine below the concentration of 0.625 g/L show no significant difference to controls. The partial muscarinic agonist, Pilocarpine, evokes concentration-dependent relaxation with an EC 50 of 2.4 mM in isolated segments of rat tail artery that were constricted with Penylephrine (10 to 200 nM).
The Pilocarpine-induced saliva secretion of the control rats (CN) and exercised (EX) rats is examined. A significantly greater amount of saliva is induced by Pilocarpine in the EX rats than in the CN rats (P<0.01). Conversely, the Na + concentration in the saliva of the EX rats is significantly lower than that of the CN rats (P<0.05).
可由植物毛果芸香提取毛果芸香碱后，再用硝酸处理而制得。
安全信息
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英文
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