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Chemical Compound Review:

alpha-Mcpg 4-(1-amino-1-carboxy- ethyl)benzoic acid

Synonyms: CHEMBL299683, SureCN715285, AG-J-02329, ACMC-20cchr, M4796_SIGMA, ...

Li, D.P. et al., Chu, Z. et al., Song, D.K. et al., Amos, B.J. et al., Cozzi, A. et al., et al.

Thomsen, Bruno, Nicoletti, Marinozzi, Pellicciari, Song, Suh, Jung, Wie, Song, Kim,

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Disease relevance of alpha-Methyl-cpgly

Bilateral microinjection (50 nl) of a metabotropic receptor antagonist (alpha-methyl-4-carboxyphenylglycine, MCPG, 100 mM) into the rostral commissural NTS produced no change in the gain of the baroreflex bradycardia [1].

High impact information on alpha-Methyl-cpgly

PCCG-IV was significantly more potent and selective as an antagonist at mGluR2 compared with previously described mGluR2 antagonists, including alpha-methyl-4-carboxyphenylglycine [2].
However EGTA-AM or alpha-methyl-4-carboxyphenylglycine (MCPG) removed the very slow depolarizing component of the EPSP and prevented the sustained firing at very low rate [3].
The ACPD response was mimicked by S-3-hydroxyphenylglycine (3-HPG) and by (s)-4-carboxy-3-hydroxyphenylglycine (4C-3HPG) but was not blocked by alpha-methyl-4-carboxyphenylglycine (MCPG) or (RS)-1-aminoindan-1, 5-dicarboxcylic acid (AIDA), features consistent with an mGluR5 receptor-mediated mechanism [4].
Moreover, the protective effect of 1-aminocyclo-pentane-trans-1,3-dicarboxylic acid is prevented by alpha-methyl-4-carboxyphenylglycine, an antagonist of mGluR1 and 5, but not by alpha-methyl-4-tetrazoylphenylglycine, an antagonist of mGluR2 and 3 [5].
On the contrary, alpha-methyl-4-carboxyphenylglycine, an antagonist of type 1 and type 2 mGlu receptors, increased the glutamate concentration in dialysates by up to 3.5-fold, and its effects were prevented by the simultaneous administration of L-CCG-1, a preferential type 2 mGlu receptor agonist [6].

Biological context of alpha-Methyl-cpgly

The effects of MCCG and MAP4 were compared with alpha-methyl-4-carboxyphenylglycine (MCPG), which non-selectively antagonizes group II mGluRs, as well as group I mGluRs (mGluR1,5) which are positively coupled to phosphatidylinositol (PI) hydrolysis [7].
Microinjection of alpha-methyl-4-carboxyphenylglycine, a metabotropic receptor antagonist, into the NTSlat or NTSmid produced no changes in baseline mean arterial pressure or heart rate or in the chemoreflex responses [8].

Anatomical context of alpha-Methyl-cpgly

1S,3R-ACPD-stimulated [3H]InsP formation was inhibited by alpha-methyl-4-carboxyphenylglycine, indicating that cultured hepatocytes express functional mGlu receptors coupled to polyphosphoinositide hydrolysis [9].

Associations of alpha-Methyl-cpgly with other chemical compounds

The ability of the selective metabotropic glutamate receptor (mGluR) antagonist alpha-methyl-4-carboxyphenylglycine (MCPG) to protect hippocampal CA1 neurons from a hypoxic/hypoglycemic injury was examined [10].
The group I and II mGlu receptor agonist (1S,3R)-ACPD (1-amino-cyclopentane-1,3-dicarboxylate; 1-3 mM) increased dopamine release (367% of basal levels) which was prevented by the non-selective mGlu receptor antagonist, (+)-MCPG (alpha-methyl-4-carboxyphenylglycine; 10 mM) [11].
The broad-spectrum antagonist alpha-methyl-4-carboxyphenylglycine (MCPG) and/or (RS)-alpha-cyclopropyl-4-phosphonophenylglycine (CPPG) (group III antagonist) enhanced spontaneous PSC frequency, particularly when initial frequency was low, suggesting that endogenous activation of mGluRs regulates GABA transmission to GnRH neurons [12].

Gene context of alpha-Methyl-cpgly

3. The amplitude of the EPSC was not significantly affected by the bath application of the mGluR antagonist (+) alpha-methyl-4-carboxyphenylglycine (MCPG) [13].
Application of the putative antagonist, alpha-methyl-4-carboxyphenylglycine (MCPG), failed to antagonize the biphasic actions of ACPD [14].
Neither 6-cyano-7-nitro-quinoxaline-2,3-dione (CNQX) (0.01-0.5 micrograms) nor alpha-methyl-4-carboxyphenylglycine (MCPG) (1-20 micrograms), antagonists of non-NMDA and metabotropic glutamate receptors, respectively, i.c.v. administered, affected the basal and stress-induced plasma interleukin-6 levels [15].

Analytical, diagnostic and therapeutic context of alpha-Methyl-cpgly

However, microinjection of 2-amino-5-phosphonopentanoic acid (0.1 and 1 nmol, n = 8), an NMDA- receptor antagonist, or alpha-methyl-4-carboxyphenylglycine (0.1 and 1 nmol, n = 5), a glutamate metabotropic receptor antagonist, failed to attenuate significantly the pressor and RSNA responses to stimulation of cardiac receptors with BK [16].

References

Antagonism of glutamatergic metabotropic receptors in the NTS of awake rats does not affect the gain of the baroreflex. Antunes, V.R., Machado, B.H. Autonomic neuroscience : basic & clinical. (2003) [Pubmed]
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a potent and selective antagonist of type 2 metabotropic glutamate receptors. Thomsen, C., Bruno, V., Nicoletti, F., Marinozzi, M., Pellicciari, R. Mol. Pharmacol. (1996) [Pubmed]
Dynamics of excitatory synaptic components in sustained firing at low rates. Wyart, C., Cocco, S., Bourdieu, L., Léger, J.F., Herr, C., Chatenay, D. J. Neurophysiol. (2005) [Pubmed]
Characterization of an intracellular alkaline shift in rat astrocytes triggered by metabotropic glutamate receptors. Amos, B.J., Chesler, M. J. Neurophysiol. (1998) [Pubmed]
Activation of the metabotropic glutamate receptor mGluR5 prevents glutamate toxicity in primary cultures of cerebellar neurons. Montoliu, C., Llansola, M., Cucarella, C., Grisolía, S., Felipo, V. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
Type 2 metabotropic glutamate (mGlu) receptors tonically inhibit transmitter release in rat caudate nucleus: in vivo studies with (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a new potent and selective antagonist. Cozzi, A., Attucci, S., Peruginelli, F., Marinozzi, M., Luneia, R., Pellicciari, R., Moroni, F. Eur. J. Neurosci. (1997) [Pubmed]
Attenuation of morphine withdrawal symptoms by subtype-selective metabotropic glutamate receptor antagonists. Fundytus, M.E., Ritchie, J., Coderre, T.J. Br. J. Pharmacol. (1997) [Pubmed]
Sympathoexcitatory neurotransmission of the chemoreflex in the NTS of awake rats. Haibara, A.S., Bonagamba, L.G., Machado, B.H. Am. J. Physiol. (1999) [Pubmed]
Metabotropic glutamate receptor agonists stimulate polyphosphoinositide hydrolysis in primary cultures of rat hepatocytes. Sureda, F., Copani, A., Bruno, V., Knöpfel, T., Meltzger, G., Nicoletti, F. Eur. J. Pharmacol. (1997) [Pubmed]
The metabotropic glutamate receptor antagonist (+)-alpha-methyl-4-carboxyphenylglycine protects hippocampal CA1 neurons of the rat from in vitro hypoxia/hypoglycemia. Opitz, T., Richter, P., Reymann, K.G. Neuropharmacology (1994) [Pubmed]
Group I mGlu receptor modulation of dopamine release in the rat striatum in vivo. Bruton, R.K., Ge, J., Barnes, N.M. Eur. J. Pharmacol. (1999) [Pubmed]
Endogenous activation of metabotropic glutamate receptors modulates GABAergic transmission to gonadotropin-releasing hormone neurons and alters their firing rate: a possible local feedback circuit. Chu, Z., Moenter, S.M. J. Neurosci. (2005) [Pubmed]
Metabotropic glutamate receptors depress afferent excitatory transmission in the rat nucleus tractus solitarii. Glaum, S.R., Miller, R.J. J. Neurophysiol. (1993) [Pubmed]
Modulation of epileptiform activity by metabotropic glutamate receptors in immature rat neocortex. Burke, J.P., Hablitz, J.J. J. Neurophysiol. (1995) [Pubmed]
Involvement of NMDA receptor in the regulation of plasma interleukin-6 levels in mice. Song, D.K., Suh, H.W., Jung, J.S., Wie, M.B., Song, J.H., Kim, Y.H. Eur. J. Pharmacol. (1996) [Pubmed]
Differential roles for glutamate receptor subtypes within commissural NTS in cardiac-sympathetic reflex. Li, D.P., Averill, D.B., Pan, H.L. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2001) [Pubmed]

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