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G蛋白偶联受体/G蛋白
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/ 5-羟色胺受体 / Phenylbiguanide

苯基双胍 /Phenylbiguanide {[allProObj[0].p_purity_real_show]}

货号：A401395 同义名： 1-苯基双胍 / N-Phenylbiguanide;PBG

Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.

Phenylbiguanide 化学结构 CAS号：102-02-3
Phenylbiguanide 化学结构
CAS号：102-02-3
Phenylbiguanide 3D分子结构
CAS号：102-02-3
Phenylbiguanide 化学结构 CAS号：102-02-3
Phenylbiguanide 3D分子结构 CAS号：102-02-3
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Phenylbiguanide 纯度/质量文件 产品仅供科研

货号：A401395 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

 		98%
Venlafaxine ✔ 98%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 98%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 98%
Fluoxetine HCl ✔ 99.5%
Paroxetine hydrochloride ✔ AChR 97%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		98%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

 		99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

 		99%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

 		99%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

 		98%
Tropisetron ✔ 99%
Palonosetron ✔ 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron hydrochloride dihydrate ✔ 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

 		98%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

 		++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

 		++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

 		++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Phenylbiguanide 生物活性

描述 Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM. Phenylbiguanide (1-Phenylbiguanide) is a 5-HT3 receptor selective agonist with pEC50s of 5.57, 4.07, and 4.47 for r5-HT3A(b), h5-HT3A, m5-HT3A(b), respectively[4]. PBG (Phenylbiguanide) (10 μg/kg) produced hypotension, bradycardia and apnoea-bradypnoea[5]. 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)[6]. Intra-atrial injection of PBG produced a reflex cardiorespiratory response including a pronounced bradycardia and a respiratory depression. In addition, c-Fos expression in the crescent part of the lateral parabrachial nucleus was decreased in PBG-injected mice whereas no significant differences were detected between PBG-injected and control mice in the number of c-Fos-positive nuclei in the dorsal part of the lateral parabrachial nucleus[7].

Phenylbiguanide 参考文献

[1]Mair ID, et al. Pharmacological characterization of a rat 5-hydroxytryptamine type3 receptor subunit (r5-HT3A(b)) expressed in Xenopus laevis oocytes. Br J Pharmacol. 1998 Aug;124(8):1667-74.

[2]Ataee R, et al. Study of 5HT3 and HT4 receptor expression in HT29 cell line and human colon adenocarcinoma tissues. Arch Iran Med. 2010 Mar;13(2):120-5.

[3]de Vries A, et al. Characterisation of c-Fos expression in the central nervous system of mice following right atrialinjections of the 5-HT3 receptor agonist Phenylbiguanide. Auton Neurosci. 2005 Dec 30;123(1-2):62-75.

[4]Mair ID, Lambert JJ, Yang J, Dempster J, Peters JA. Pharmacological characterization of a rat 5-hydroxytryptamine type3 receptor subunit (r5-HT3A(b)) expressed in Xenopus laevis oocytes. Br J Pharmacol. 1998 Aug;124(8):1667-74

[5]Dutta A, Akella A, Deshpande SB. Mechanisms underlying the augmentation of phenylbiguanide and capsaicin induced cardiorespiratory reflexes by Mesobuthus tamulus venom. Pulm Pharmacol Ther. 2012 Oct;25(5):383-91

[6]Ataee R, Ajdary S, Rezayat M, Shokrgozar MA, Shahriari S, Zarrindast MR. Study of 5HT3 and HT4 receptor expression in HT29 cell line and human colon adenocarcinoma tissues. Arch Iran Med. 2010 Mar;13(2):120-5

[7]de Vries A, Paton JF, Lightman SL, Lowry CA. Characterisation of c-Fos expression in the central nervous system of mice following right atrial injections of the 5-HT3 receptor agonist phenylbiguanide. Auton Neurosci. 2005 Dec 30;123(1-2):62-75

Phenylbiguanide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.64mL

1.13mL

0.56mL

28.22mL

5.64mL

2.82mL

56.43mL

11.29mL

5.64mL

Phenylbiguanide 技术信息

CAS号102-02-3
分子式C8H11N5
分子量 177.206
别名 1-苯基双胍 ;N-Phenylbiguanide;PBG;1-Phenylbiguanide
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Room Temperature
溶解度

DMSO: 145 mg/mL(818.25 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 25 mg/mL(141.08 mM)
动物实验配方

Tags: Phenylbiguanide | 102-02-3 | N-Phenylbiguanide | PBG | 1-Phenylbiguanide | 5-HT3 Receptor Agonist | GPCR/G Protein | Neuronal Signaling | 5-HT Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Phenylbiguanide 纯度/质量文件 | Phenylbiguanide 亚型比较 | Phenylbiguanide 生物活性 | Phenylbiguanide 参考文献 | Phenylbiguanide 实验方案 | Phenylbiguanide 技术信息

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