盐酸美加明_MSDS_用途_熔点_盐酸美加明CAS号【826-39-1】

Mecamylamine hydrochloride 是一种口服活性,非选择性,非竞争性 nAChR 拮抗剂,可以治疗各种神经精神疾病。Mecamylamine hydrochloride 是一种神经节阻滞剂,最初用作治疗高血压。Mecamylamine hydrochloride 可以很容易地穿过血脑屏障。

[ 描述 ]:

Mecamylamine hydrochloride 是一种口服活性,非选择性,非竞争性 nAChR 拮抗剂,可以治疗各种神经精神疾病。Mecamylamine hydrochloride 是一种神经节阻滞剂,最初用作治疗高血压。Mecamylamine hydrochloride 可以很容易地穿过血脑屏障。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

研究领域 >> 神经疾病

[ 靶点 ]

nAChR[1]

[体外研究]

甲淀粉酶胺以一种依赖于使用和电压的方式阻断肌肉nAChRs。麦卡明通过诱捕机制阻断烟碱电流。这种阻滞的主要特征是阻滞解除现象,这种现象可能是由nAChRs的去极化和活化共同作用所揭示的。mecadamamine对肌肉nAChR s作用的实验研究表明：(1)mecadamamine(1-20μM)在保持电位为70mv时,Hill常数为1.2,IC50=7.8μM,降低诱发终板电流(EPC)振幅；(2)其与肌肉nAChR通道相互作用的计算深度几乎是神经性nAChRs(0.37比0.72)；(3)运动神经刺激同时膜去极化和突触后nAChRs重复激活产生快速的阻滞缓解,依赖于去极化程度、条件信号数目和meccalymine浓度,且仅与速度有轻微关系刺激[2]。

[体内研究]

甲淀粉酶胺(0.5-1 mg/kg；腹腔注射；C57BL/6J小鼠)对TST和FST都有抗抑郁作用,这些作用依赖于β2和α7亚单位[3]。动物模型：C57BL/6J小鼠(3-4个月)强迫游泳试验(FST)和尾部悬吊试验(TST)[3]剂量：0.5 mg/kg、0.75 mg/kg、1 mg/kg给药：腹腔注射结果：在1.0 mg/kg剂量下,TST中的静止时间显著缩短,但不改变基线运动活性。也显著减少了FST中的不动时间。

[参考文献]

[1]. Bacher I, et al. Mecamylamine - a nicotinic acetylcholine receptor antagonist with potential for the treatment of neuropsychiatric disorders. Expert Opin Pharmacother. 2009 Nov;10(16):2709-21.

[2]. Ostroumov K, et al. Modeling study of mecamylamine block of muscle type acetylcholine receptors. Eur Biophys J. 2008 Apr;37(4):393-402.

[3]. Rabenstein RL, et al. The nicotinic antagonist mecamylamine has antidepressant-like effects in wild-type but not beta2- or alpha7-nicotinic acetylcholine receptor subunit knockout mice. Psychopharmacology (Berl). 2006 Dec;189(3):395-401.

[ 沸点 ]:
189.3ºC at 760 mmHg

[ 熔点 ]:
>240ºC (dec.)

[ 分子式 ]:
C₁₁H₂₂ClN

[ 分子量 ]:
203.752

[ 闪点 ]:
58.1ºC

[ 精确质量 ]:
203.144073

[ PSA ]:
12.03000

[ LogP ]:
3.61350

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
Desiccate at RT

[ 水溶解性 ]:
ethanol: 122 mg/mL

详细MSDS(安全技术说明书)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RB6900000

CHEMICAL NAME :: 2-Norbornanamine, N,2,3,3-tetramethyl-, hydrochloride

CAS REGISTRY NUMBER :: 826-39-1

LAST UPDATED :: 199603

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C11-H21-N.Cl-H

MOLECULAR WEIGHT :: 203.79

WISWESSER LINE NOTATION :: L55 ATJ CM1 C1 D1 D1 &GH

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 :: 208 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 117,169,1956

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 53 mg/kg

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

REFERENCE :: RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,301,1970

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 177 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 117,169,1956

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 21 mg/kg

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

REFERENCE :: RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,300,1970

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 92 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: 6,814,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 17 mg/kg

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

REFERENCE :: RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,300,1970

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 81 mg/kg

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

REFERENCE :: RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,300,1970

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 14 mg/kg

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

REFERENCE :: RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,300,1970

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 175 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 117,169,1956

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 63 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 117,169,1956

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 155 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 117,169,1956 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1 gm/kg/8W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Sense Organs and Special Senses (Eye) - lacrimation Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 13,501,1958

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H315-H319-H335

[ 警示性声明 ]:
Missing Phrase - N15.00950417-P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
36/37/39

[ 危险品运输编码 ]:
UN 2811 6

[ WGK德国 ]:
3

[ RTECS号 ]:
RB6900000

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2921300090

[ 海关编码 ]: 2921300090

[ 中文概述 ]:
2921300090 其他环（烷，烯，萜烯）单胺或多胺（包括其衍生物及它们的盐）. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2921300090 other cyclanic, cyclenic or cyclotherpenic mono- or polyamines, and their derivatives; salts thereof。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%

A nicotinic receptor-mediated anti-inflammatory effect of the flavonoid rhamnetin in BV2 microglia.

Fitoterapia 98 , 11-21, (2014)

The alpha7 nicotinic acetylcholine receptor (nAChR) is a potential target in neuroinflammation. Screening a plant extract library identified Solidago nemoralis as containing methyl-quercetin derivativ...

Profiling the role of deacylation-reacylation in the lymphatic transport of a triglyceride-mimetic prodrug.

Pharm. Res. 32(5) , 1830-44, (2015)

Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that fac...

Toxicity induced by F. poae-contaminated feed and the protective effect of Montmorillonite supplementation in broilers.

Food Chem. Toxicol. 74 , 120-30, (2014)

The T-2 and HT-2 toxins, the main metabolites of Fusarium poae, induce toxicity in broilers and accumulate in tissues. Consequently, during the breeding process of broilers, diets are frequently suppl...

更多文献

公司名：上海吉至生化科技有限公司

区域：上海市奉贤区

价格：
￥428.0/5mg ￥4718.0/100mg ￥1548.0/25mg

联系人：刘佳

产品详情：盐酸美加明

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Mecamylamine hydrochloride

公司名：上海脉铂医药科技有限公司