盐酸苯海索理化性质

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性质:又名安坦。白色结晶性粉末,无臭,味微苦,微溶于水,溶于乙醇和氯仿。由哌啶为原料制得,常用其盐酸盐。为抗震颤麻痹药,其对中枢纹状体胆碱受体有阻断作用,外周抗胆碱作用较弱,约为阿托品的(1/10)~(1/3)。用于震颤麻痹(脑炎后或动脉硬化引起的震颤麻痹)对改善流涎有效,对缓解僵直,运动迟缓效较差,改善震颤明显,但总的疗效不及左旋多巴、金刚烷胺。主要用于轻症及不能耐受左旋多巴的患者。也用于药物利血平和吩噻嗪类引起的锥体外系反应以及肝豆状核变性。制剂有片剂,胶囊剂。

盐酸苯海索

分子量:暂无

CAS号:52-49-3

化学物质索引数据库

Title: Trihexyphenidyl Hydrochloride

CAS Registry Number: 52-49-3

CAS Name:α-Cyclohexyl-α-phenyl-1-piperidinepropanol hydrochloride

Additional Names: 3-(1-piperidyl)-1-cyclohexyl-1-phenyl-1-propanol hydrochloride;

1-phenyl-1-cyclohexyl-3-piperidyl-1-propanol hydrochloride; benzhexol chloride Trademarks: Aparkane (ICN); Artane (Wyeth); Broflex (Bioglan); Cyclodol; Pacitane (Wyeth); Paralest (Parachemie); Pargitan (Abigo); Parkinane (Wyeth); Parkopan (Hexal); Peragit (AFI); Pipanol (Winthrop); Sedrena (Daiichi); Tremin (Schering-Plough); Triphedinon (Toho); Triphenidyl (Leciva); Tsiklodol

Molecular Formula: C20H32ClNO

Molecular Weight: 337.93

Percent Composition: C 71.08%, H 9.54%, Cl 10.49%, N 4.14%, O 4.73%

Literature References: Anticholinergic. Synthesis: Denton et al.,J. Am. Chem. Soc.71, 2053 (1949); Adamson, Wilkinson, US2682543 (1954 to Burroughs Wellcome); Denton, US

2716121 (1955 to Am. Cyanamid). Resolution into isomers: Adamson, Duffin, GB750156 (1956 to Wellcome Found.).

Properties: Crystals, dec 258.5°. Free base, mp 114.3-115.0°. Soly (g/100 ml): water at 25°, 1.0; alcohol 6; chloroform 5. More sol in methanol; very slightly sol in ether, benzene. pH of a 1% aq soln 5.5-6.0.

Melting point: Free base, mp 114.3-115.0°

Derivative Type:l-Form

Properties: Crystals from isopropyl alc, mp 264°. [α]D20 -30° (c = 0.4 in chloroform). Free base, mp 112-113°. [α]D20 -25° (c = 0.4 in ethanol).

Melting point: mp 264°; Free base, mp 112-113°

Optical Rotation: [α]D20 -30° (c = 0.4 in chloroform); [α]D20 -25° (c = 0.4 in ethanol)

Therap-Cat: Antiparkinsonian.

Keywords: Antiparkinsonian; Antimuscarinic.

Properties

State solid

Melting point 258.5 oC

Experimental Properties

Property Value Source logP 4.5 PhysProp

Predicted Properties

Property Value Source water solubility 3.14e-03 g/l ALOGPS logP 4.93 ALOGPS

logP 4.23

ChemAxon

Molconvert logS -5 ALOGPS

pKa 0

ChemAxon

Molconvert hydrogen acceptor

count

2

ChemAxon

Molconvert hydrogen donor

count

1

ChemAxon

Molconvert

polar surface area 23.47

ChemAxon

Molconvert rotatable bond

count

5

ChemAxon

Molconvert refractivity 93.21 ChemAxon

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