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木防己苦毒宁

木防己苦毒宁用途

Picrotoxinin 是一种有效的惊厥药,是一种氯通道 (chloride channel) 阻断剂。Picrotoxinin 是一种非竞争性的 GABAA 受体拮抗剂,负向调节 GABA 对 GABAA受体的作用。

木防己苦毒宁名称

[ CAS 号 ]:
17617-45-7

[ 中文名 ]:
木防己苦毒宁

[ 英文名 ]:
Picrotoxinin

[中文别名 ]:

汉中防己提取物

[英文别名 ]:

picrotoxinin
MFCD00078765

木防己苦毒宁生物活性

[ 描述 ]:

Picrotoxinin 是一种有效的惊厥药,是一种氯通道 (chloride channel) 阻断剂。Picrotoxinin 是一种非竞争性的 GABAA 受体拮抗剂,负向调节 GABA 对 GABAA受体的作用。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 氯离子通道

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[参考文献]

[1]. Ng CC, et al. Effects of bilobalide, ginkgolide B and picrotoxinin on GABA_A receptor modulation by structurally diverse positive modulators. Eur J Pharmacol. 2017 Jul 5;806:83-90.

木防己苦毒宁物理化学性质

[ 密度 ]:
1.52g/cm3

[ 沸点 ]:
551.6ºC at 760mmHg

[ 熔点 ]:
203-205ºC

[ 分子式 ]:
C₁₅H₁₆O₆

[ 分子量 ]:
292.28400

[ 闪点 ]:
214ºC

[ 精确质量 ]:
292.09500

[ PSA ]:
85.36000

[ 蒸汽压 ]:
1.82E-14mmHg at 25°C

[ 折射率 ]:
1.625

木防己苦毒宁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: PC5150000

CHEMICAL NAME :: 3,6-Methano-8H-1,5,7-trioxacyclopenta(ij)cycloprop(a) azulene-4,8(3H)-dione, hexahydro- 2a-hydroxy-8b-methyl-9-(1-methylethenyl)-, (1aR-(1a-alpha,2a-beta,3-beta,6-beta,6a-beta, 8as*,8b-beta,9R*))-

CAS REGISTRY NUMBER :: 17617-45-7

LAST UPDATED :: 199806

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C15-H16-O6

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8980 ug/kg

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

REFERENCE :: CUTOEX Current Toxicology. (Nova Science Publishers, Inc., 6080 Jericho Turnpike, Suite 207, Commack, NY 11725) V.1 1993- Volume(issue)/page/year: 1,199,1993

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1600 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: JPHAA3 Journal of the American Pharmaceutical Association. (Washington, DC) V.1-28, 1912-39; New series: V.1-17, 1961-77. Volume(issue)/page/year: 23,98,1934

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

ROUTE OF EXPOSURE :: Intracerebral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 10 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 60,289,1992

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1100 ug/kg

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

REFERENCE :: FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1350 ug/kg

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

REFERENCE :: FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Bird - pigeon

DOSE/DURATION :: 1600 ug/kg

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

REFERENCE :: FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Bird - pigeon

DOSE/DURATION :: 1600 ug/kg

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

REFERENCE :: JPHAA3 Journal of the American Pharmaceutical Association. (Washington, DC) V.1-28, 1912-39; New series: V.1-17, 1961-77. Volume(issue)/page/year: 23,98,1934

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Amphibian - frog

DOSE/DURATION :: 1100 ug/kg

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

REFERENCE :: FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931

木防己苦毒宁安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
Missing Phrase - N15.00950417

[ 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) ]:
T+: Very toxic;

[ 风险声明 (欧洲) ]:
25-28

[ 安全声明 (欧洲) ]:
S13;S20;S28;S45;S36/S37

[ 危险品运输编码 ]:
UN 3172

[ RTECS号 ]:
PC5150000

[ 包装等级 ]:
I

[ 危险类别 ]:
6.1(a)

木防己苦毒宁文献

Rat alpha6beta2delta GABAA receptors exhibit two distinct and separable agonist affinities.

J. Physiol. 581(Pt 3) , 1001-18, (2007)

The onset of motor learning in rats coincides with exclusive expression of GABAA receptors containing alpha6 and delta subunits in the granule neurons of the cerebellum. This development temporally co...

Cys-Loop Receptor Channel Blockers Also Block GLIC

Biophys. J. 101(12) , 2912-8, (2011)

The Gloeobacter ligand-gated ion channel (GLIC) is a bacterial homolog of vertebrate Cys-loop ligand-gated ion channels. Its pore-lining region in particular has a high sequence homology to these rela...

Amyloid precursor proteins interact with the heterotrimeric G protein Go in the control of neuronal migration.

J. Neurosci. 33(24) , 10165-81, (2013)

Amyloid precursor protein (APP) belongs to a family of evolutionarily conserved transmembrane glycoproteins that has been proposed to regulate multiple aspects of cell motility in the nervous system. ...

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