Drug intelligence / Profile preview

phenyl biguanide

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal
01

Overview

Phenyl biguanide is a small molecule biguanide derivative primarily utilized in pharmacological research as a selective agonist for the 5-hydroxytryptamine receptor 3 (5-HT3). While structurally related to anti-diabetic biguanides like metformin and phenformin, phenyl biguanide exhibits distinct pharmacokinetic and pharmacodynamic properties, notably poor mitochondrial uptake. In oncology research, it has been investigated for its potential effects on cancer cell metabolism and growth; however, studies indicate it has minimal growth inhibitory effects on bladder and colon cancer cell lines compared to other biguanides. It is most commonly employed as a tool to study 5-HT3-mediated physiological responses, such as the Bezold-Jarisch reflex, in animal models.

Other names
1-phenylbiguanideN-phenylbiguanidephenylbiguanide
02

Targets

ND1 (Mitochondrial electron transport chain complex I)HTR3A (5-hydroxytryptamine receptor 3A)

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