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m-Chlorophenylbiguanide hydrochloride is a 5-HT3 receptor agonist. m-Chlorophenylbiguanide hydrochloride selectively binds 5-HT3(Ki: 0.002 µM) over 5-HT1A(Ki: 10 µM) and 5-HT2(Ki: 10 µM) receptors but also binds to high and low affinity sites on the dopamine transporter(DAT; IC50s: 0.4 and 34.8 µM, respectively, in rat caudate putamen synaptosomal membranes).