Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Editor

Personal info

View

About

Terms

Javascript disabled

Please enable Javascript support in your browser to use this application.

Instructions on how to enable JavaScript on different browsers can be found here: http://www.google.com/support/bin/answer.py?answer=23852.

[edit this page]

Chemical Compound Review:

mCPBG 2-(3-chlorophenyl)-1- (diaminomethylidene)g...

Synonyms: Lopac-C-144, Tocris-0440, CHEMBL13790, Bio-0861, AG-K-81604, ...

Monti, J.M. et al., Lang, P.M. et al., Kamato, T. et al., Libert, F. et al., Castro, L. et al., et al.

Monti, Ponzoni, Jantos, Lagos, Silveira, Banchero,

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of N-m-Chlorophenylbiguanide hydrochloride

The agonist properties of m-chlorophenylbiguanide and 2-methyl-5-hydroxytryptamine on 5-HT3 receptors in N1E-115 neuroblastoma cells [1].
Intracerebroventricularly (4th ventricle) administered YM060 inhibited cisplatin- and m-chlorophenylbiguanide-induced emesis only at higher doses (0.01-0.1 and 0.01-0.03 microgram, respectively) [2].
The 5-HT3 receptor agonist, m-chlorophenylbiguanide (mCPBG), attenuated the effect of tropisetron; of the three mCPBG doses (500 ng, 1000 ng, 1500 ng) examined, 1000 ng was the most effective, perhaps because, alone, 1500 ng mCPBG slightly reduced lordosis behavior [3].
In the present paper, we studied in rats the effect of third ventricle administration of m-chlorophenylbiguanide hydrochloride (1-(3-chlorophenyl)biguanide (m-CPBG), a selective 5-HT(3) agonist, on water intake induced by three different physiological stimuli: water deprivation, acute salt load and hypovolemia [4].

Psychiatry related information on N-m-Chlorophenylbiguanide hydrochloride

Bilateral injections of m-chlorophenylbiguanide into the nucleus accumbens of the control and the vehicle-infused animals significantly increased waking and reduced slow wave sleep [5].
The effects of selective activation of the 5-HT3 receptor with m-chlorophenylbiguanide on sleep and wakefulness in the rat [6].

High impact information on N-m-Chlorophenylbiguanide hydrochloride

(ii) The specific agonists for 5-HT3, m-chlorophenylbiguanide, and 5-HT4, 3-(4-allylpiperazin-1-yl)-2-quinoxaline chloronitrile, mimicked the effects of serotonin [7].
Moreover, pretreatment with AODNs did not reverse the acetaminophen-induced antinociceptive effect, although it suppressed the antinociceptive effect of m-chlorophenylbiguanide, a specific agonist of 5-HT(3) receptors, and significantly reduced (30%) the expression of these receptors in the dorsal horn of the spinal cord [8].
We employed site-directed mutagenesis to investigate the role of amino acids from the loop C region of the murine 5-HT(3AS)R in interacting with two structurally different agonists, serotonin (5-HT) and m-chlorophenylbiguanide (mCPBG) [9].
3. The effect was mimicked by two other 5-HT3 receptor agonists, 2-methyl-5-HT and m-chlorophenylbiguanide (mCPBG) which gave 50% inhibition at approximately 600 nM and approximately 20 nM, respectively [10].
In the present study, we have tested the effects of m-chlorophenylbiguanide (mCPBG), an agonist at the 5-HT(3) serotonin receptor, on activity- and potential-dependent variations in membrane threshold and conduction velocity of unmyelinated C-fiber axons of isolated rat sural nerve segments [11].

Biological context of N-m-Chlorophenylbiguanide hydrochloride

Similar effects on excitability changes were found when latency instead of threshold was recorded, but only at higher action potential frequencies: at 1.8 Hz, mCPBG increased conduction velocity and reduced postspike supernormality [11].

Anatomical context of N-m-Chlorophenylbiguanide hydrochloride

2-Methyl-5-HT and m-chlorophenylbiguanide concentration-dependently contracted the ferret ileum, whereas they had no effect in piglets and rats [12].

Associations of N-m-Chlorophenylbiguanide hydrochloride with other chemical compounds

In the presence of nomifensine, 1-(m-chlorophenyl)biguanide, classified as a 5-HT3 agonist, also induced a greater fractional release from weaver compared with +/+ striatum [13].
However, differences in 5-HT3 receptors of different tissues and species were detected on the basis of statistically significant differences in the affinities of phenylbiguanide, and 1-(m-chlorophenyl)biguanide when displacing [3H]RS-42358-197 binding [14].
Pretreatment with the 5-HT3 receptor antagonist MDL 72222 (1aH,3a,5a, H-tropan-3-yl-3,5-dichloro-benzoate) (0.5 mg/kg s.c.) reversed the effects of m-chlorophenylbiguanide (10.0-20.0 micrograms) on sleep and waking [15].
Effects of accumbens m-chlorophenylbiguanide microinjections on sleep and waking in intact and 6-hydroxydopamine-treated rats [5].
Only high concentrations of the 5-HT3 receptor agonist m-chlorophenylbiguanide increased [3H]noradrenaline release from hippocampal slices, and this effect was not blocked by ondansetron nor by (S)-zacopride [16].

Analytical, diagnostic and therapeutic context of N-m-Chlorophenylbiguanide hydrochloride

Pretreatment with the selective 5-HT3 receptor antagonist, MDL 72222 (1aH,3a,5a, H-tropan-3-yl-3,5-dichloro-benzoate) (0.5 mg/kg, s.c.), reversed the effects of m-chlorophenylbiguanide (10.0-20.0 microg) on sleep and waking in the control group [5].
A highly selective and potent 5-HT3 receptor agonist, m-chlorophenylbiguanide (1-10 mg/kg i.p.), dose dependently elicited emesis an effect which was inhibited by YM060 (0.003-0.3 microgram/kg i.v.). Vagotomy markedly reduced this emesis, and the combination of abdominal vagotomy and greater splanchnicectomy abolished emesis [2].

References

The agonist properties of m-chlorophenylbiguanide and 2-methyl-5-hydroxytryptamine on 5-HT3 receptors in N1E-115 neuroblastoma cells. Sepúlveda, M.I., Lummis, S.C., Martin, I.L. Br. J. Pharmacol. (1991) [Pubmed]
Mechanisms of cisplatin- and m-chlorophenylbiguanide-induced emesis in ferrets. Kamato, T., Ito, H., Nagakura, Y., Nishida, A., Yuki, H., Yamano, M., Miyata, K. Eur. J. Pharmacol. (1993) [Pubmed]
5-HT3 receptors in the ventromedial nucleus of the hypothalamus and female sexual behavior. Maswood, N., Caldarola-Pastuszka, M., Uphouse, L. Brain Res. (1997) [Pubmed]
Central 5-HT(3) receptors and water intake in rats. Castro, L., Varjão, B., Maldonado, I., Campos, I., Duque, B., Fregoneze, J., Reis de Oliveira, I., De Castro-e-Silva, E. Physiol. Behav. (2002) [Pubmed]
Effects of accumbens m-chlorophenylbiguanide microinjections on sleep and waking in intact and 6-hydroxydopamine-treated rats. Monti, J.M., Ponzoni, A., Jantos, H., Lagos, P., Silveira, R., Banchero, P. Eur. J. Pharmacol. (1999) [Pubmed]
The effects of selective activation of the 5-HT3 receptor with m-chlorophenylbiguanide on sleep and wakefulness in the rat. Ponzoni, A., Monti, J.M., Jantos, H. Eur. J. Pharmacol. (1993) [Pubmed]
Involvement of c-Src and protein kinase C delta in the inhibition of Cl(-)/OH- exchange activity in Caco-2 cells by serotonin. Saksena, S., Gill, R.K., Tyagi, S., Alrefai, W.A., Sarwar, Z., Ramaswamy, K., Dudeja, P.K. J. Biol. Chem. (2005) [Pubmed]
Acetaminophen: a central analgesic drug that involves a spinal tropisetron-sensitive, non-5-HT(3) receptor-mediated effect. Libert, F., Bonnefont, J., Bourinet, E., Doucet, E., Alloui, A., Hamon, M., Nargeot, J., Eschalier, A. Mol. Pharmacol. (2004) [Pubmed]
The loop C region of the murine 5-HT3A receptor contributes to the differential actions of 5-hydroxytryptamine and m-chlorophenylbiguanide. Suryanarayanan, A., Joshi, P.R., Bikádi, Z., Mani, M., Kulkarni, T.R., Gaines, C., Schulte, M.K. Biochemistry (2005) [Pubmed]
Electrophysiological consequences of ligand binding to the desensitized 5-HT3 receptor in mammalian NG108-15 cells. Bartrup, J.T., Newberry, N.R. J. Physiol. (Lond.) (1996) [Pubmed]
Activity-Dependent Modulation of Axonal Excitability in Unmyelinated Peripheral Rat Nerve Fibers by the 5-HT(3) Serotonin Receptor. Lang, P.M., Moalem-Taylor, G., Tracey, D.J., Bostock, H., Grafe, P. J. Neurophysiol. (2006) [Pubmed]
Species differences in the 5-hydroxytryptamine-induced contraction in the isolated distal ileum. Yamano, M., Ito, H., Miyata, K. Jpn. J. Pharmacol. (1997) [Pubmed]
Dopamine transporter-dependent and -independent endogenous dopamine release from weaver mouse striatum in vitro. Richter, J.A., Bare, D.J., Yu, H., Ghetti, B., Simon, J.R. J. Neurochem. (1995) [Pubmed]
Labelling of 5-hydroxytryptamine3 receptors with a novel 5-HT3 receptor ligand, [3H]RS-42358-197. Wong, E.H., Bonhaus, D.W., Wu, I., Stefanich, E., Eglen, R.M. J. Neurochem. (1993) [Pubmed]
Increased waking after intra-accumbens injection of m-chlorophenylbiguanide: prevention with serotonin or dopamine receptor antagonists. Ponzoni, A., Monti, J.M., Jantos, H., Altier, H., Monti, D. Eur. J. Pharmacol. (1995) [Pubmed]
Activation of 5-HT3 receptors enhances the electrically evoked release of [3H]noradrenaline in rat brain limbic structures. Mongeau, R., De Montigny, C., Blier, P. Eur. J. Pharmacol. (1994) [Pubmed]

Contributions to this collaborative article are from individual authors of WikiGenes or mined by the WikiGenes Data Mining Engine from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.About WikiGenes Open Access Licence Privacy Policy Terms of Use apsburg

The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.