药品详细

Pentolinium(安血定)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

安血定

英文名

Pentolinium

分子式

C₁₅H₃₂N₂

化学名

1-methyl-1-[5-(1-methylpyrrolidin-1-ium-1-yl)pentyl]pyrrolidin-1-ium

分子量

Average: 240.428
Monoisotopic: 240.256549034

CAS号

52-62-0

ATC分类

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

A nicotinic antagonist that has been used as a ganglionic blocking agent in hypertension. [PubChem]

生产厂家

Wyeth ayerst laboratories

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Pyrrolidines
Quaternary Ammonium Salts

Substructures

Pyrrolidines
Quaternary Ammonium Salts
Heterocyclic compounds
Cations

适应症

药理

Indication	Used to produce controlled hypotension during surgical procedures and in hypertensive crises.
Pharmacodynamics	Pentolinium acts as a ganglionic blocking agent. Pentolinium inhibits release of adrenaline and noradrenaline from adrenergic nerves. It is used as an antihypertensive, and can be administered orally, intramuscularly, and subcutaneously.
Mechanism of action	Pentolinium binds to the nicotinic (ganglion) acetylcholine receptor. This receptor/channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. Blockage of the receptor leads to smooth muscle relaxation and vasodilaton.
Absorption	Not Available
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	Not Available
Route of elimination	Not Available
Half life	Not Available
Clearance	Not Available
Toxicity	Oral, mouse: LD₅₀ = 512 mg/kg; Oral, rat: LD₅₀ = 890 mg/kg.
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	213 °C (tartrate salt)	Not Available

Predicted Properties

Property	Value	Source
water solubility	1.16e-05 g/l	ALOGPS
logP	-2.3	ALOGPS
logP	-6.3	ChemAxon
logS	-7.4	ALOGPS
physiological charge	2	ChemAxon
hydrogen acceptor count	0	ChemAxon
hydrogen donor count	0	ChemAxon
polar surface area	0	ChemAxon
rotatable bond count	6	ChemAxon
refractivity	99.03	ChemAxon
polarizability	31.36	ChemAxon

药物相互作用

食物相互作用

Not Available

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