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酚妥拉明

酚妥拉明用途

酚妥拉明是一种有效、选择性和口服活性的α1肾上腺素能和α2肾上腺素能受体拮抗剂。酚妥拉明可用于治疗勃起功能障碍[1][2][3]。

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酚妥拉明名称

[ CAS 号 ]:
50-60-2

[ 中文名 ]:
酚妥拉明

[ 英文名 ]:
Phentolamine

[中文别名 ]:

[英文别名 ]:

Fentolamin
EINECS 200-053-1
MFCD00242985
Phentalamine
Regitin
Phenotolamine
Dibasin
Fentolamina
Regitine
Phentolaminum

酚妥拉明生物活性

[ 描述 ]:

酚妥拉明是一种有效、选择性和口服活性的α1肾上腺素能和α2肾上腺素能受体拮抗剂。酚妥拉明可用于治疗勃起功能障碍[1][2][3]。

[ 相关类别 ]:

研究领域 >> 内分泌

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]

酚妥拉明(5-20mg/kg；i.p.)有效抑制士的宁(2mg/kg,i.p.),并减弱DOP(4mg/kg,i.p.)对小鼠的惊厥增强作用[2]。酚妥拉明(1mg/kg；i.p.)通过抑制小鼠b细胞a2A肾上腺素受体增加胰岛素分泌[3]。动物模型：WT小鼠[3]剂量：1mg/kg给药：IP结果：血糖降低,胰岛素水平升高。

[参考文献]

[1]. Goldstein I I. Oral phentolamine: an alpha-1, alpha-2 adrenergic antagonist for the treatment of erectile dysfunction. Int J Impot Res. 2000 Mar;12(S1):S75-S80

[2]. Amabeoku G, et al. Strychnine-induced seizures in mice: the role of noradrenaline. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Jul;18(4):753-63.

[3]. Fagerholm V, et al. alpha2A-adrenoceptor antagonism increases insulin secretion and synergistically augments the insulinotropic effect of glibenclamide in mice. Br J Pharmacol. 2008 Jul;154(6):1287-96.

酚妥拉明物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
551.0±45.0 °C at 760 mmHg

[ 熔点 ]:
177 - 178ºC

[ 分子式 ]:
C₁₇H₁₉N₃O

[ 分子量 ]:
281.352

[ 闪点 ]:
287.0±28.7 °C

[ 精确质量 ]:
281.152802

[ PSA ]:
47.86000

[ LogP ]:
3.60

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.626

[ 储存条件 ]:
-20°C

酚妥拉明毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SL0700000

CHEMICAL NAME :: Phenol, 3-(((4,5-dihydro-1H-imidazol-2-yl)methyl)(4-methylphe nyl)amino)-

CAS REGISTRY NUMBER :: 50-60-2

BEILSTEIN REFERENCE NO. :: 0272944

LAST UPDATED :: 199612

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C17-H19-N3-O

MOLECULAR WEIGHT :: 281.39

WISWESSER LINE NOTATION :: T5M CN BUTJ B1NR CQ&R D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1 gm/kg

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

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: 112,319,1957

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - tremor Behavioral - ataxia

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,1727,1971

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 mg/kg

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

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: 105,317,1956

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2 gm/kg

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

REFERENCE :: CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change Behavioral - convulsions or effect on seizure threshold

REFERENCE :: SMWOAS Schweizerische Medizinische Wochenschrift. (Schwabe & Co., Steintorst 13, 4010 Basel, Switzerland) V.50- 1920- Volume(issue)/page/year: 81,352,1951

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 28 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis Lungs, Thorax, or Respiration - respiratory depression

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: 174,243,1968 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 100 ug/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

REFERENCE :: DPTHDL Developmental Pharmacology and Therapeutics. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 7(Suppl 1),72,1984

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酚妥拉明安全信息

[ 安全声明 (欧洲) ]:
S26-S36/37/39-S45-S8-S25

[ 危险品运输编码 ]:
UN 3264 8/PG 2

[ WGK德国 ]:
3

[ 包装等级 ]:
II

[ 危险类别 ]:
8

[ 海关编码 ]:
2933290090

酚妥拉明合成路线

详细合成路线

酚妥拉明上下游产品

酚妥拉明上游产品

酚妥拉明下游产品

酚妥拉明海关

[ 海关编码 ]: 2933290090

[ 中文概述 ]:
2933290090. 其他结构含非稠合咪唑环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%