二氢-β-刺桐定氢溴酸盐

二氢-β-刺桐定氢溴酸盐用途

Dihydro-β-erythroidine (DHβE) hydrobromide 是一种有效竞争性的,具有口服活性的神经 nAChRs 拮抗剂。Dihydro-β-erythroidine hydrobromide 对 α4β4 和 α4β2 有选择性,IC50 分别为 0.19 和 0.37 μM。具有抗抑郁类活性。

二氢-β-刺桐定氢溴酸盐名称

[ CAS 号 ]:
29734-68-7

[ 中文名 ]:
二氢-β-刺桐定氢溴酸盐

[ 英文名 ]:
Dihydro-β-erythroidine hydrobromide

[中文别名 ]:

[英文别名 ]:

DIHYDRO-B-ERYTHROIDINE HYDROBROMIDE
Beta-Erythroidine, Dihydro-, Hydrobromide

二氢-β-刺桐定氢溴酸盐生物活性

[ 描述 ]:

[ 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

[体内研究]

在全身注射尼古丁(0.2 mg/kg；SC)之前,将氢溴酸二氢β-红霉素(DHβE氢溴酸；10 nmol/0.5 μL)注入相应区域。DHβE注入腹侧被盖区(VTA)、伏隔核(NAcc)或边缘下(IL)皮质,而不是前(PrL)皮质,减弱尼古丁增强对条件增强剂(CRf)的反应[2]。与尼古丁(0.2和0.4 mg/kg；s.c.)共给药二氢β-氢溴化红(5.0 mg/kg；s.c.)可防止条件味觉厌恶(CTAs)的发生[4]。动物模型：雄性蒙面李斯特大鼠[4]剂量：0.5、1.6、5.0mg/kg给药：S.c.结果：完全阻断训练剂量(0.2mg/kg)产生的尼古丁效应。

[参考文献]

[1]. Harvey SC, et al. Multiple determinants of dihydro-beta-erythroidine sensitivity on rat neuronal nicotinic receptor alpha subunits. J Neurochem. 1996 Nov;67(5):1953-9.

[2]. Tabbara RI, et al. Nicotine enhances responding for conditioned reinforcement via α4β2 nicotinic acetylcholine receptors in the ventral tegmental area, but not the nucleus accumbens or the prefrontal cortex. Neuropharmacology. 2019 Apr;148:68-76.

[3]. Clementson S, et al. Enantioselective Total Synthesis of (+)-Dihydro-β-erythroidine. J Am Chem Soc. 2019 Jun 5;141(22):8783-8786.

二氢-β-刺桐定氢溴酸盐物理化学性质

[ 沸点 ]:
475.5ºC at 760 mmHg

[ 分子式 ]:
C₁₆H₂₂BrNO₃

[ 分子量 ]:
356.25500

[ 闪点 ]:
241.4ºC

[ 精确质量 ]:
355.07800

[ PSA ]:
38.77000

[ LogP ]:
2.70930

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
3.29E-09mmHg at 25°C

[ 储存条件 ]:
2-8°C，密封，干燥

二氢-β-刺桐定氢溴酸盐MSDS

详细MSDS(安全技术说明书)

二氢-β-刺桐定氢溴酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KF3325000

CHEMICAL NAME :: beta-Erythroidine, dihydro-, hydrobromide

CAS REGISTRY NUMBER :: 29734-68-7

LAST UPDATED :: 198612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C16-H21-N-O3.Br-H

MOLECULAR WEIGHT :: 356.30

WISWESSER LINE NOTATION :: T B6656 1A Q AX DVO JN XU XUTJ PO1 &EH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - changes in structure or function of salivary glands

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: 75,270,1942

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 8900 ug/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: 82,266,1944

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1100 ug/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: 82,266,1944

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2100 ug/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: 82,266,1944

二氢-β-刺桐定氢溴酸盐安全信息

[ 安全声明 (欧洲) ]:
22-36

[ WGK德国 ]:
3

[ RTECS号 ]:
KF3325000