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1-Phenylbiguanide hydrochloride

5-HT3 agonist CAS# 55-57-2

1-Phenylbiguanide hydrochloride

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1-Phenylbiguanide hydrochloride

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Chemical Properties of 1-Phenylbiguanide hydrochloride

Cas No. 55-57-2 SDF Download SDF
PubChem ID 5932 Appearance Powder
Formula C8H12ClN5 M.Wt 213.67
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 25 mM in DMSO
Chemical Name 1-(diaminomethylidene)-2-phenylguanidine;hydrochloride
SMILES C1=CC=C(C=C1)N=C(N)N=C(N)N.Cl
Standard InChIKey FHUDRDSKZQDCBC-UHFFFAOYSA-N
Standard InChI InChI=1S/C8H11N5.ClH/c9-7(10)13-8(11)12-6-4-2-1-3-5-6;/h1-5H,(H6,9,10,11,12,13);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of 1-Phenylbiguanide hydrochloride

Description5-HT3 receptor agonist.

1-Phenylbiguanide hydrochloride Dilution Calculator

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Preparing Stock Solutions of 1-Phenylbiguanide hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.6801 mL 23.4006 mL 46.8011 mL 93.6023 mL 117.0029 mL
5 mM 0.936 mL 4.6801 mL 9.3602 mL 18.7205 mL 23.4006 mL
10 mM 0.468 mL 2.3401 mL 4.6801 mL 9.3602 mL 11.7003 mL
50 mM 0.0936 mL 0.468 mL 0.936 mL 1.872 mL 2.3401 mL
100 mM 0.0468 mL 0.234 mL 0.468 mL 0.936 mL 1.17 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on 1-Phenylbiguanide hydrochloride

Study of 5HT3 and HT4 receptor expression in HT29 cell line and human colon adenocarcinoma tissues.[Pubmed:20187666]

Arch Iran Med. 2010 Mar;13(2):120-5.

BACKGROUND: Serotonin (5HT) has been shown to be a mitogenic factor in several carcinomas. Its mitogenic effect is elicited through a wide range of 5HT receptor subtypes. In this study, the effects of 5HT, 5HT3 (1-Phenylbiguanide hydrochloride) and 5HT4 (cisapride) agonists in promoting the growth of the HT29 cell line and the growth-inhibition effect of the 5HT3 receptor antagonist (Y-25130 hydrochloride) and 5HT4 receptor antagonist (RS 23597-190) were investigated. The expressions of 5HT3 and 5HT4 receptors in human colon cancer tissues and the HT29 cell line were studied. METHODS: The growth-promoting and growth-inhibition effects of 5-HT, 5HT3 and 5HT4 agonists and antagonists on the HT29 cell line were studied using MTT assay. Receptor expression has been demonstrated by western blotting. RESULTS: The results showed that 5HT, 5HT3, and 5HT4 agonists caused significant proliferation of HT29 cells. 5HT3 and 5HT4 receptor antagonists had an inhibitory effect on the growth of these cells. Western blot analysis gave bands from colon tissue extracts and the HT29 cell line. CONCLUSION: The results indicate which 5HT3 and 5HT4 receptors are significantly expressed in both colon cancer tissue and the HT29 cell line. Expression for the 5HT3 receptor is more potent. Furthermore, 5HT plays a mitogenic role in colon cancer cells and antagonists of 5HT3, and 5HT4 receptors can inhibit cancer cell growth.

Receptor subtype specific activation of the rat gastric vagal afferent fibers to serotonin.[Pubmed:12467882]

Life Sci. 2002 Dec 20;72(4-5):415-23.

Systemic administration (i.v.) of serotonin (5-HT) evoked a transient vagal afferent nerve discharge, bradycardia, and hypotension in the rat. The half-effective dose of 5-HT for nerve discharge was 13 micro g/kg. The time- and dose-dependent kinetics of the nerve discharge rate were similar to the change of heart rate. The afferent neuronal discharge was mimicked by a selective 5-HT3 receptor agonist, 1-Phenylbiguanide hydrochloride (PBA), and inhibited by a selective 5-HT3 antagonist, granisetron. The 5-HT(3/4) agonist, cisapride partially activated the vagus nerve, but the 5-HT4 agonist, RS6733 had no effect on the vagal afferent activity. Intra-gastric perfusion of lidocaine, moreover, abolished the 5-HT-induced vagal activation. These results indicate that the 5-HT transmission signal in the gastric mucosa inputs to the brain stem via 5-HT3 receptor-mediated vagal nerve afferent.

Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerve.[Pubmed:3814920]

Br J Pharmacol. 1987 Jan;90(1):229-38.

A study has been made of the pharmacology of the 5-hydroxytryptamine (5-HT)-induced depolarization responses that can be recorded extracellularly from the rat isolated cervical vagus nerve. Phenylbiguanide (PBG) and 2-methyl-5-hydroxytryptamine (2-methyl-5-HT) were found to mimic the effects of 5-HT on the vagus nerve. Their EC50 values were respectively 2.0 fold and 3.9 fold greater than that of 5-HT. Metoclopramide behaved as a reversible competitive antagonist of depolarization induced by PBG and 2-methyl-5-HT, with pKB values of 6.48 +/- 0.04, respectively. These agreed well with the pKB value of 6.60 +/- 0.04 obtained previously for metoclopramide against 5-HT on the rat vagus nerve. 5-HT, PBG and 2-methyl-5-HT had no demonstrable agonist effects at non-5-HT receptors on the rat vagus nerve. Tropacaine and m-chlorophenylpiperazine were found to behave as reversible competitive antagonists of 5-HT-induced depolarization of the vagus nerve. The pKB values were 6.29 +/- 0.03 and 6.90 +/- 0.03, respectively. Quipazine, MDL 72222 and ICS 205-930 were also shown to be effective antagonists of 5-HT on the vagus nerve. However, although these compounds were highly potent, they all caused a marked concentration-dependent reduction in the amplitude of the maximum response to 5-HT. This behaviour was not consistent with a simple reversible competitive mechanism. The results are discussed with reference to the current classification of mammalian peripheral neuronal 5-HT receptors.

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