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148-72-1

中文名稱 硝酸毛果蕓香堿
英文名稱 Pilocarpine nitrate
CAS 148-72-1
EINECS 編號 205-723-7
分子式 C11H17N3O5
MDL 編號 MFCD00078497
分子量 271.27
MOL 文件 148-72-1.mol
更新日期 2024/10/30 11:29:00
148-72-1 結(jié)構(gòu)式 148-72-1 結(jié)構(gòu)式

基本信息

中文別名
硝酸毛果蕓香堿
硝酸匹魯卡品
硝酸匹魯卡品(硝酸毛果蕓香堿)
(3S,4R)-3-乙基二氫-4-[(1-甲基-1H-咪唑-5-基)甲基]-2(3H)-呋喃酮硝酸鹽
英文別名
3-ETHYLDIHYDRO-4-[(1-METHYL-1H-IMIDAZOL-5-YL)-METHYL]-2-(3H)-FURANONE NITRATE
PILOCARPINE NITRATE
PILOCARPINE NITRATE SALT
3-ethyldihydro-4-[(1-methyl-1h-imidazol-5-yl)methyl]-2(3h)-furanon(3s-cis)
p.v.carpineliquifilm
pilocarpine,mononitrate
Pilocarpinenitrateusp
pilocarpinesubnitrate
pilofrin
PILOCARPINE NITRATE, PH EUR
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

物理化學(xué)性質(zhì)

熔點(diǎn)173,5-174°C
比旋光度D +77 to +83° (c = 10)
折射率81 ° (C=2, H2O)
儲存條件2-8°C
溶解度H2O: 0.1 g/mL, clear, very faintly yellow
形態(tài)粉末
顏色白色
旋光性 (optical activity)[α]25/D +83°, c = 10 in H2O(lit.)
Merck7424
BRN4171406
CAS 數(shù)據(jù)庫148-72-1(CAS DataBase Reference)
EPA化學(xué)物質(zhì)信息Pilocarpine nitrate (148-72-1)

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS03,GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H272-H302-H330
危險(xiǎn)品標(biāo)志Xn,T+
危險(xiǎn)類別碼R22-R26/28
安全說明S1-S25-S45
危險(xiǎn)品運(yùn)輸編號3087
WGK Germany3
RTECS號TK1455000
危險(xiǎn)等級6.1(b)
包裝類別III
海關(guān)編碼2939800000
毒性LD50 oral in rat: 911mg/kg

制備方法

方法1

可由植物毛果蕓香提取毛果蕓香堿后,再用硝酸處理而制得。

常見問題列表

簡介

硝酸毛果蕓香堿呈無色結(jié)晶或白色結(jié)晶性粉末;無臭;遇光易變質(zhì)。其可用于青光眼、虹膜炎的治療。

禁忌癥

1.對本藥過敏者。

2.支氣管哮喘患者。

3.急性虹膜炎、虹膜睫狀體炎等不應(yīng)縮瞳的眼病患者。

生物活性
Pilocarpine nitrate 是一種選擇性的 M3 型毒蕈堿乙酰膽堿受體 (M3 muscarinic receptor) 激動劑。
靶點(diǎn)

M3 muscarinic receptor

體外研究

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).

體內(nèi)研究

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).

知名試劑公司產(chǎn)品信息

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