[CAS NO. 102-02-3] Phenylbiguanide
PRODUCTS SPECIFICATIONS [102-02-3]
DESCRIPTION [102-02-3]
Overview
| MDL | MFCD00179077 |
|---|---|
| Molecular Weight | 177.21 |
| Molecular Formula | C8H11N5 |
| SMILES | NC(NC(NC1=CC=CC=C1)=N)=N |
Summary
Phenylbiguanide is a 5-HT 3 receptor selective agonist with an EC 50 of 3.0±0.1 μM.
IC50 & Target
|
5-HT 3 Receptor 3 μM (EC 50 ) |
In Vitro
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 [1] . 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) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 150 mg/mL ( 846.45 mM ; Need ultrasonic)
H 2 O : ≥ 25 mg/mL ( 141.08 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 5.6430 mL | 28.2151 mL | 56.4302 mL |
| 5 mM | 1.1286 mL | 5.6430 mL | 11.2860 mL |
| 10 mM | 0.5643 mL | 2.8215 mL | 5.6430 mL |
References
- [1] Mair ID, et al. Pharmacological characterization of a rat 5-hydroxytryptamine type3 receptor subunit (r5-HT ) expressed in 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.
Synonyms
