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Phenylbiguanide

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Chemical Structure| 102-02-3 同义名 : 1-苯基双胍 ;N-Phenylbiguanide;PBG;1-Phenylbiguanide
CAS号 : 102-02-3
货号 : A401395
分子式 : C8H11N5
纯度 : 98%
分子量 : 177.206
MDL号 : MFCD00179077
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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