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硝酸毛果芸香碱

硝酸毛果芸香碱用途

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。
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硝酸毛果芸香碱名称

[ CAS 号 ]:
148-72-1

[ 中文名 ]:
毛果芸香碱 硝酸盐

[ 英文名 ]:
Pilocarpine nitrate

[中文别名 ]:

[英文别名 ]:

硝酸毛果芸香碱生物活性

[ 描述 ]:

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。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR
信号通路 >> 神经信号通路 >> mAChR
研究领域 >> 神经疾病

[ 靶点 ]

M3 muscarinic receptor[1]


[体外研究]

为了评估毛果芸香碱的细胞毒性,分别通过光学显微镜和MTT测定检查人角膜基质(HCS)细胞的形态和活力。形态学观察显示暴露于毛果芸香碱的浓度为0.625至20g/L的HCS细胞表现出剂量和时间依赖性的增殖迟缓和形态学异常,例如细胞收缩,细胞质空泡化,从培养基质中脱离,最终死亡,而没有暴露于浓度为0.625g/L的毛果芸香碱和对照之间观察到明显的差异。 MTT法检测结果显示,暴露于毛果芸香碱后,HCS细胞的活力随着时间和浓度的增加而降低至0.625 g/L以上(P <0.01或0.05),而毛果芸香碱处理的HCS细胞的活力低于0.625 g/L显示对照没有显着差异[2]。部分毒蕈碱激动剂毛果芸香碱引起浓度依赖性松弛,在大鼠尾动脉的分离段中EC50为2.4 mM,其中用去氧肾上腺素(10至200 nM)收缩[3]。

[体内研究]

检测毛果芸香碱诱导的对照大鼠(CN)和运动(EX)大鼠的唾液分泌。毛果芸香碱在EX大鼠中诱导的唾液量显着高于CN大鼠(P <0.01)。相反,EX大鼠唾液中Na +浓度显着低于CN大鼠(P <0.05)[1]。

[细胞实验]

通过MTT测定确定细胞活力。简而言之，将HCS细胞以1×10 4个细胞/100μL/孔的密度接种到96孔培养板（Nunc）中，并进行培养和处理。以4小时的间隔，将含有毛果芸香碱（0.625至20g / L）的培养基完全替换为含有1.0g / L MTT的100μL无血清DMEM / F12培养基，并将细胞在37℃下在黑暗中孵育。持续4小时。在小心丢弃含有MTT的培养基后，加入150μLDMSO以在37℃在黑暗中溶解产生的甲crystals晶体15分钟，并用Multiskan GO酶标仪读取490nm处的吸光度[2]。 。

[动物实验]

大鼠[1]将10周龄雄性Wistar大鼠分为两组中的一组，运动（EX，n = 6）和对照（CN，n = 6）。将EX大鼠在带有滚轮（SN-451）的笼子中保持40天，允许它们进行自愿运动，同时将CN大鼠保持在笼子中并锁定行驶轮。在第40天，毛果芸香碱诱导的唾液测量如下。简而言之，将大鼠麻醉，将预先称重的棉花舌下放入口中，腹膜内注射毛果芸香碱（0.5mg / kg）以诱导唾液分泌。然后每10分钟更换一个棉球1小时。将收集的棉球再次称重，并通过从最终重量中减去初始值来计算分泌的唾液的质量。

[参考文献]

[1]. Matsuzaki K, et al. Daily voluntary exercise enhances pilocarpine-induced saliva secretion and aquaporin 1 expression in rat submandibular glands. FEBS Open Bio. 2017 Dec 7;8(1):85-93.

[2]. Yuan XL, et al. Cytotoxicity of pilocarpine to human corneal stromal cells and its underlying cytotoxic mechanisms. Int J Ophthalmol. 2016 Apr 18;9(4):505-11.

[3]. Tonta MA, et al. Pilocarpine-induced relaxation of rat tail artery by a non-cholinergic mechanism and in the absence of an intact endothelium. Br J Pharmacol. 1994 Jun;112(2):525-32.


[相关活性小分子]

卡巴胆碱 | 氢溴酸达非那新 | 氢溴酸槟榔碱 | 盐酸哌仑西平 | 甘罗溴铵 | 咪达那新 | 苯扎托品 | 诺美林草酸盐 | Batefenterol | 氯贝胆碱 | 盐酸西维美林 | 奥替溴铵 | 索利那新 | VU0467154 | 山莨菪碱

硝酸毛果芸香碱物理化学性质

[ 沸点 ]:
520.5ºC at 760 mmHg

[ 熔点 ]:
173,5-174°C

[ 分子式 ]:
C11H17N3O5

[ 分子量 ]:
271.27000

[ 闪点 ]:
268.6ºC

[ 精确质量 ]:
271.11700

[ PSA ]:
110.17000

[ LogP ]:
1.33730

[ 蒸汽压 ]:
1.16E-11mmHg at 25°C

[ 折射率 ]:
81 ° (C=2, H2O)

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: 0.1 g/mL, clear, very faintly yellow

硝酸毛果芸香碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TK1455000
CHEMICAL NAME :
Pilocarpine, mononitrate
CAS REGISTRY NUMBER :
148-72-1
LAST UPDATED :
199701
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C11-H16-N2-O2.H-N-O3
MOLECULAR WEIGHT :
271.31
WISWESSER LINE NOTATION :
T5OVTJ C2 D1- ET5N CNJ A1 &WNO

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
911 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - fluid intake Kidney, Ureter, Bladder - urine volume decreased
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
345 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
15600 mg/kg/15W-I
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - urine volume increased Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
2200 mg/kg
SEX/DURATION :
female 1-22 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - skin and skin appendages
TYPE OF TEST :
Micronucleus test
TYPE OF TEST :
Mutation test systems - not otherwise specified

MUTATION DATA

TEST SYSTEM :
Rodent - mouse
DOSE/DURATION :
8 mg/kg
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 344,103,1995 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 81934 No. of Facilities: 42 (estimated) No. of Industries: 2 No. of Occupations: 4 No. of Employees: 980 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 81934 No. of Facilities: 22 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 1525 (estimated) No. of Female Employees: 1273 (estimated)
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硝酸毛果芸香碱安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300 + H330

[ 警示性声明 ]:
Missing Phrase - N15.00950417-P260-P304 + P340 + P310-P403 + P233

[ 个人防护装备 ]:
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

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S1-S25-S45

[ 危险品运输编码 ]:
3087

[ WGK德国 ]:
3

[ RTECS号 ]:
TK1455000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2934999090

硝酸毛果芸香碱合成路线

详细合成路线

硝酸毛果芸香碱制备

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。

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硝酸毛果芸香碱海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

硝酸毛果芸香碱文献

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Function of inhibitory micronetworks is spared by Na+ channel-acting anticonvulsant drugs.

J. Neurosci. 34(29) , 9720-35, (2014)

The mechanisms of action of many CNS drugs have been studied extensively on the level of their target proteins, but the effects of these compounds on the level of complex CNS networks that are compose...

Development and characterization of pilocarpine loaded Eudragit nanosuspensions for ocular drug delivery.

J. Biomed. Nanotechnol. 9(1) , 124-31, (2013)

With aim of improving the availability of drug at intraocular level and to reduce the frequency of drug administration, pilocarpine nitrate nanosuspensions were made from inert polymer resin (Eudragit...


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公司名：上海创赛科技有限公司

区域：上海市嘉定区

价格：
￥919.0/100mg ￥3208.0/500mg

联系人：夏言

产品详情：[Perfemiker]Pilocarpine nitrate,98%

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥539.9/50mg ￥861.9/100mg ￥1719.9/250mg ￥需询单/1g

联系人：阿拉丁李高志

产品详情：Pilocarpine nitrate

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