中文名称:

1-苯基双胍

中文同义词:

苯基双胍;1-苯基双胍

英文名称:

PHENYLBIGUANIDE

英文同义词:

phenyldiguanide;1-PHENYLBIGUANIDE;N-PHENYLIMINODICARBONIMIDIC-DIAMIDE;PHENYLBIGUANIDE;2-(N2-Phenylamidino)guanidine;1-phenyl-biguanid;n-phenyl-n’-guanylguanidine;p1426

CAS号:

102-02-3

分子式:

C8H11N5

分子量:

177.21

EINECS号:

202-998-5

相关类别:

胍;有机化学;AgonistsOrganic Building Blocks;Guanidines;Neurotransmitters;Nitrogen Compounds;Serotonergics

Mol文件:

102-02-3.mol

熔点 

135-142 °C (lit.)

沸点 

299.13°C (rough estimate)

密度 

1.2512 (rough estimate)

折射率 

1.6900 (estimate)

储存条件 

Keep in dark place,Sealed in dry,Room Temperature

溶解度 

alcohol: freely soluble

酸度系数(pKa)

10.76, 2.13(at 25℃)

Merck 

14,7276

InChIKey

CUQCMXFWIMOWRP-UHFFFAOYSA-N

CAS 数据库

102-02-3(CAS DataBase Reference)

生物活性

1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide)是一种 5-hydroxytryptamine3 (5-HT3) receptor 激动剂，EC50为3.0 μM。

靶点

Target Value 5-HT3 receptor (Cell-free assay) 3.0 μM(EC50)

Target

Value

5-HT3 receptor (Cell-free assay)

3.0 μM(EC50)

体外研究

Phenylbiguanide (1-Phenylbiguanide) is a 5-HT 3 receptor selective agonist with pEC 50 s of 5.57, 4.07, and 4.47 for r5-HT 3A(b) , h5-HT 3A , m5-HT 3A(b) , respectively. The effect of Phenylbiguanide (1-Phenylbiguanide hydrochloride) in promoting the growth of the HT29 cell line is investigated. Phenylbiguanide causes a dose dependent proliferation of HT29 cells after 48 hours incubation. The maximum proliferation is at a 5HT concentration of 12.5 μM (P≤0.01). Phenylbiguanide significantly stimulates the growth of cells at concentrations of 3.125 μM (P≤0.05) and 6.25 μM (P≤0.01).

体内研究

In anaesthetised mice, Phenylbiguanide (PBG), a drug that is known to stimulate cardiopulmonary afferent C-fibres,is injected into the right atrium of the heart and mapped c-Fos expression within specific regions of the central nervous system. Intraatrial injection of PBG produces a reflex cardiorespiratory response including a pronounced bradycardia and a respiratory depression.

WGK Germany 

3

RTECS号

DU2450000