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环噻嗪

环噻嗪用途

环噻嗪是AMPA受体的一种正变构调节剂,经常用于阻断天然和异源表达的AMPA受体的脱敏。已知环噻嗪能快速抑制AMPA受体脱敏,并缓慢增强AMPA电流[1]。

环噻嗪名称

[ CAS 号 ]:
2259-96-3

[ 中文名 ]:
环噻嗪

[ 英文名 ]:
Cyclothiazide

[中文别名 ]:

莰烯氯噻嗪

[英文别名 ]:

cyclothiazidum [INN_la]
Cyclothiazide
UNII:P71U09G5BW
MFCD00210192

环噻嗪生物活性

[ 描述 ]:

环噻嗪是AMPA受体的一种正变构调节剂,经常用于阻断天然和异源表达的AMPA受体的脱敏。已知环噻嗪能快速抑制AMPA受体脱敏,并缓慢增强AMPA电流[1]。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> iGluR

[参考文献]

[1]. Fucile S, et al. Effects of cyclothiazide on GluR1/AMPA receptors. Proc Natl Acad Sci U S A. 2006;103(8):2943-2947.

环噻嗪物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
627.3±65.0 °C at 760 mmHg

[ 熔点 ]:
234ºC

[ 分子式 ]:
C₁₄H₁₆ClN₃O₄S₂

[ 分子量 ]:
389.878

[ 闪点 ]:
333.2±34.3 °C

[ 精确质量 ]:
389.027069

[ PSA ]:
135.12000

[ LogP ]:
1.15

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.654

[ 储存条件 ]:
2-8°C

环噻嗪MSDS

环噻嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DK9610000

CHEMICAL NAME :: 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 3,4-dihydro-6-chloro-3-(5-norbornen-2-yl)-, 1,1-dioxide

CAS REGISTRY NUMBER :: 2259-96-3

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C14-H16-Cl-N3-O4-S2

MOLECULAR WEIGHT :: 389.90

WISWESSER LINE NOTATION :: T66 BSWM EM DHJ HG ISZW D- FL55 A CUTJ

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 :: >5 gm/kg

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

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 101,929,1962

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1500 mg/kg

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

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 101,929,1962

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/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: 6,460,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 18,487,1968 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - A1012 No. of Facilities: 24 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 141 (estimated)

环噻嗪安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ RTECS号 ]:
DK9610000

环噻嗪合成路线

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环噻嗪文献

Nicotinic receptors modulate the function of presynaptic AMPA receptors on glutamatergic nerve terminals in the trigeminal caudal nucleus.

Neurochem. Int. 90 , 166-72, (2015)

In this study, we demonstrate the existence on trigeminal caudal nucleus (TCN) glutamatergic terminals of α4β2 nicotinic receptors (nAChRs) capable of enhancing the terminals' spontaneous release of [...

AMPA receptor desensitization is the determinant of AMPA receptor mediated excitotoxicity in purified retinal ganglion cells.

Exp. Eye Res. 132 , 136-50, (2015)

The ionotropic glutamate receptors (iGLuR) have been hypothesized to play a role in neuronal pathogenesis by mediating excitotoxic death. Previous studies on iGluR in the retina have focused on two br...

Molecular mechanisms contributing to TARP regulation of channel conductance and polyamine block of calcium-permeable AMPA receptors.

J. Neurosci. 34(35) , 11673-83, (2014)

Many properties of fast synaptic transmission in the brain are influenced by transmembrane AMPAR regulatory proteins (TARPs) that modulate the pharmacology and gating of AMPA-type glutamate receptors ...

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环噻嗪