Overview
- Kilpatrick, G.J. et al. (1990) Eur. J. Pharmacol. 182, 193.
- Alomone Labs m-Chlorophenylbiguanide hydrochloride activates 5-HT3A receptors expressed in HEK 293T cells.Currents were elicited by 1 or 10 µM m-Chlorophenylbiguanide hydrochloride (#M-160), as indicated. Currents elicited by m-Chlorophenylbiguanide hydrochloride were comparable in amplitude to the cells response to 10 µM 5-HT (not shown).
- Hannon, J. and Hoyer, D. (2008) Behav. Brain Res. 195, 198.
- Sepulveda, M.I. et al. (1991) Br. J. Pharmacol. 104, 536.
- Schlicker, E. et al. (1994) Naunyn Schmiedebergs Arch. Pharmacol. 349, 20.
- Rothlin, C.V. et al. (2003) Mol. Pharmacol. 63, 1067.
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid tryptophan by the enzyme tryptophan-decarboxylase. The 5-HT3 channel is a ligand gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.
m-Chlorophenylbiguanide hydrochloride (mCPG) is a prototypical, potent and selective 5-HT3 receptor agonist. In a study conducted in N1E-115 neuroblastoma cells mCPG exhibited inward rectification and reversed currents similar to those induced by 5-HT binding to the 5-HT3 receptor. The rate of receptor desensitization is similar to that of 5-HT binding but the peak current amplitude provoked by the agonist was found to be only 20% at saturating concentration2. Interestingly, mCPG seems to facilitate noradrenaline release in mouse brain cortex cell. When mouse brain slices were incubated with H-noradrenaline, electrical field stimulation was facilitated by mCPG and this effect was blocked by the α2 adrenergic receptor antagonist, Rauwolscine3. mCPG binds and activates recombinant α9/α10 acetylcholine receptors in Xenopus oocytes (although 5-HT does not) thus producing inwards currents that are 3.1±0.7% of the maximum effect obtained by ACh binding4.
m-Chlorophenylbiguanide hydrochloride (#M-160) is a highly pure, synthetic, and biologically active compound.