< 生产厂家价格 >

盐酸毛果芸香碱

盐酸毛果芸香碱用途

Pilocarpine Hydrochloride 是一种选择性的 M3 型毒蕈碱乙酰胆碱受体 (M3 muscarinic receptor) 激动剂。

点击显示

盐酸毛果芸香碱名称

[ CAS 号 ]:
54-71-7

[ 中文名 ]:
盐酸毛果芸香碱

[ 英文名 ]:
Pilocarpine Hydrochloride

[中文别名 ]:

[英文别名 ]:

(3S,4R)
pilocel
Akarpine
Pilocarpine HCl
Salagen
Pilocarpine
pilovisc
EINECS 200-212-5
Sanpilo
Pilocarpine (Hydrochloride)

盐酸毛果芸香碱生物活性

[ 描述 ]:

Pilocarpine Hydrochloride 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.

[4]. Wang RF, et al. Post-treatment with the GLP-1 analogue liraglutide alleviate chronic inflammation and mitochondrial stress induced by Status epilepticus. Epilepsy Res. 2018 Mar 9;142:45-52.

[相关活性小分子]

盐酸毛果芸香碱物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
431.8±18.0 °C at 760 mmHg

[ 熔点 ]:
202-205 °C(lit.)

[ 分子式 ]:
C₁₁H₁₇ClN₂O₂

[ 分子量 ]:
208.257

[ 闪点 ]:
215.0±21.2 °C

[ 精确质量 ]:
208.121185

[ PSA ]:
44.12000

[ LogP ]:
-0.09

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.585

[ 储存条件 ]:
室温，惰性气体

[ 水溶解性 ]:
soluble

盐酸毛果芸香碱MSDS

详细MSDS(安全技术说明书)

盐酸毛果芸香碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TK1450000

CHEMICAL NAME :: Pilocarpine, monohydrochloride

CAS REGISTRY NUMBER :: 54-71-7

LAST UPDATED :: 199701

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C11-H16-N2-O2.Cl-H

MOLECULAR WEIGHT :: 244.75

WISWESSER LINE NOTATION :: T5OVTJ C2 D1- DT5N CNJ C1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Ocular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 200 ug/kg/7H-I

TOXIC EFFECTS :: Cardiac - other changes

REFERENCE :: AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 147,586,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 203 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,901,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 230 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,901,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,646,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 155 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - other (direct) parasympathomimetic

REFERENCE :: ATXKA8 Archiv fuer Toxikologie. (Berlin, Fed. Rep. Ger.) V.15-31, 1954-74. For publisher information, see ARTODN. Volume(issue)/page/year: 29,39,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,901,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,901,1990

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 131,171,1928

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraarterial

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 131,171,1928

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Bird - pigeon

DOSE/DURATION :: 353 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: HBAMAK "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." (Leipzig, Ger. Dem. Rep.) Volume(issue)/page/year: 4,1289,1935 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 130 mg/kg

SEX/DURATION :: female 7-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 85,79,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 20 mg/kg

SEX/DURATION :: female 24-27 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - respiratory system

REFERENCE :: AJANA2 American Journal of Anatomy. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1-192, 1901-91. Volume(issue)/page/year: 154,163,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 800 ug/kg

SEX/DURATION :: male 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Fertility - mating performance (e.g. # sperm positive females per # females mated; # copulations per # estrus cycles)

REFERENCE :: JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 8,297,1964 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - M2736 No. of Facilities: 112 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 3136 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M2736 No. of Facilities: 110 (estimated) No. of Industries: 1 No. of Occupations: 7 No. of Employees: 5031 (estimated) No. of Female Employees: 3716 (estimated)

点击显示

盐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

[ 危害码 (欧洲) ]:
T+:Verytoxic;

[ 风险声明 (欧洲) ]:
R26/28

[ 安全声明 (欧洲) ]:
S25-S45

[ 危险品运输编码 ]:
UN 1544 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
TK1450000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2934999090

盐酸毛果芸香碱合成路线

详细合成路线

盐酸毛果芸香碱海关

[ 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%

盐酸毛果芸香碱文献

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...

更多文献