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α-育亨宾

α-育亨宾用途

能选择性地阻断突触前的α2受体，促进去甲肾上腺素的释放。它使海绵体神经末梢释放较多的去甲肾上腺素，减少阴茎静脉回流，利于充血勃起。少量应用时，可使会阴部肿胀，刺激脊髓勃起中枢而使性功能亢进。可用于功能性阳痿

α-育亨宾名称

[ CAS 号 ]:
131-03-3

[ 中文名 ]:
Alpha-育亨宾

[ 英文名 ]:
Rauwolscine

[中文别名 ]:

Α-育亨宾

[英文别名 ]:

isoyohimbine
KEOXIFENE
Corynanthidine
a-Yohimbine
α-Yohimbine
EINECS 205-006-9
Rauwolscine
RALOXIFENE HCL
KEOXIFENE HYDROCHLORIDE

α-育亨宾生物活性

[ 描述 ]:

Rauwolscine是一种选择性α2-肾上腺素受体拮抗剂,可抑制肿瘤生长并诱导细胞凋亡[1]。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

[体内研究]

劳沃尔辛(0.5 mg/kg,每日)通过增强细胞凋亡和减少细胞增殖来减少余额/c雌性小鼠的肿瘤生长[1]。劳沃司汀(静脉注射,2.24 mg/kg)能明显释放大鼠的舔食冲突反应,类似于α受体激动剂可乐定(0.022 mg/kg)和苯二氮卓类安定(0.5 mg/kg)[2]

[参考文献]

[1]. A Bruzzone, et al. Alpha2-adrenoceptor action on cell proliferation and mammary tumour growth in mice. Br J Pharmacol. 2008 Oct;155(4):494-504.

[2]. S La Marca, et al. The alpha-2 antagonists idazoxan and rauwolscine but not yohimbine or piperoxan are anxiolytic in the Vogel lick-shock conflict paradigm following intravenous administration. Life Sci. 1994;54(10):PL179-84.

α-育亨宾物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
543.0±50.0 °C at 760 mmHg

[ 熔点 ]:
270-280ºC

[ 分子式 ]:
C₂₁H₂₆N₂O₃

[ 分子量 ]:
354.443

[ 闪点 ]:
282.2±30.1 °C

[ 精确质量 ]:
354.194336

[ PSA ]:
65.56000

[ LogP ]:
2.20

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.661

[ 储存条件 ]:
2-8℃，干燥，密闭

α-育亨宾毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: ZG1005000

CHEMICAL NAME :: 20-alpha-Yohimban-16-beta-carboxylic acid, 17-alpha-hydroxy-, methyl ester

CAS REGISTRY NUMBER :: 131-03-3

LAST UPDATED :: 198708

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C21-H26-N2-O3

MOLECULAR WEIGHT :: 354.49

WISWESSER LINE NOTATION :: T F6 D5 C666 EM ON&&TTTJ TQ UVO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 134,447,1961

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2500 mg/kg

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

REFERENCE :: 85IXA4 "Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948 Volume(issue)/page/year: -,317,1948

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 80 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 134,447,1961

α-育亨宾安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
23/24/25

[ 安全声明 (欧洲) ]:
22-36/37/39-45

[ 危险品运输编码 ]:
UN 1544 6.1/PG 2

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)