MAP4 - CAS 157381-42-5
Category: Inhibitor
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MAP4 is a selective group III metabotropic glutamate receptor (mGluR) antagonist in some electrophysiological systems. It acts as a group II/group III agonist in certain neurochemical systems. It modulates transmission of gustatory inputs in the brain system. It has displayed its potency in the perforant path of rat hippocampal slices.
≥96% by HPLC
(S)-2-Amino-2-methyl-4-phosphonobutyric acid; α-Methyl-AP4; MAP-4; MAP 4
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1.Activation of spinal metabotropic glutamate receptors elicits cardiovascular responses in pentobarbital anesthetized rats.
Celuch SM1, García Mdel C. Naunyn Schmiedebergs Arch Pharmacol. 2002 Oct;366(4):343-9. Epub 2002 Jul 31.
The aim of this study was to examine whether intrathecal (i.t.) injection of metabotropic glutamate (mGlu) receptor agonists at the thoracolumbar level of the spinal cord causes changes either in the blood pressure or in the heart rate of pentobarbital anesthetized rats. The broad spectrum mGlu receptor agonist (+/-)-1-aminocyclopentane- trans-1,3-dicarboxylic acid ( trans-ACPD) and the Group III mGluR agonist L-(+)-2-amino-4-phosphonobutyric acid ( L-AP4) induced pressor effects at doses of 300 nmol and 600 nmol (i.t.) but did not induce changes at a lower dose (150 nmol, i.t.). The specific Group I mGlu receptor agonist ( RS)-3,5-dihydroxyphenylglycine (3,5-DHPG), as well as the highly selective Group II mGlu receptor agonist 2 R,4 R-4-aminopyrrolidine-2,4-dicarboxilate (2 R,4 R-APDC), induced pressor effects at a dose of 300 nmol only. The compounds (150-600 nmol) did not modify the heart rate in these experiments. On the other hand, low doses of Group II mGlu receptor agonists (75 nmol 2 R,4 R-APDC; 1.
2.Group III metabotropic glutamate receptor agonists selectively suppress excitatory synaptic currents in the rat prefrontal cortex induced by 5-hydroxytryptamine2A receptor activation.
Zhang C1, Marek GJ. J Pharmacol Exp Ther. 2007 Jan;320(1):437-47. Epub 2006 Oct 4.
Activation and blockade of prefrontal cortical 5-hydroxytryptamine2A (5-HT2A) receptors have been linked to the action of hallucinogenic and antidepressant/antipsychotic drugs; these effects may involve modulation of glutamate release from thalamocortical afferents. Although activation of metabotropic glutamate 2 (mGlu2) receptors may suppress 5-HT-induced excitatory postsynaptic currents (EPSCs), group III mGlu receptors (mGlu4/7/8) also are expressed in the thalamus and may suppress 5-HT-induced EPSCs. We have found by intracellular recordings from layer V pyramidal cells of the medial prefrontal cortex (mPFC) that group III mGlu receptor agonists (R,S)-4-phosphonophenylglycine (PPG), L-4-phosphono-2-aminobutyric acid (L-AP4), L-serine-O-phosphate (L-SOP), and (S)-2-amino-2-methyl-4-phosphonobutanoic acid (MAP4) preferentially suppress 5-HT-induced EPSCs compared with excitatory postsynaptic potentials evoked by electrical stimulation of the white matter.
3.Potentiation of dopamine-induced cAMP formation by group I metabotropic glutamate receptors via protein kinase C in cultured striatal neurons.
Paolillo M1, Montecucco A, Zanassi P, Schinelli S. Eur J Neurosci. 1998 Jun;10(6):1937-45.
Metabotropic glutamate receptors have been shown to potentiate the cyclic adenosine monophosphate (cAMP) formation induced by activation of several receptors linked to adenylyl cyclase via Gs-protein. Here we show that, in primary cultures of striatal neurons, group I metabotropic receptors potentiate the cAMP formation induced by activation of D1-like dopamine receptors. Reverse transcription associated with polymerase chain reaction revealed that mGluR5, mGluR3, mGluR4 and mGluR7 are present in striatal cell cultures. The potentiation of cAMP formation is induced by the selective group I mGluRs agonist (S)-3,5-dihydroxyphenylglycine and by other non-selective mGluRs agonists with a typical group I-like pharmacology (quisqualate > ibotenate > 1-aminocyclopentane-1,3-dicarboxylic acid). The rank order potency of mGluRs agonists in potentiating cAMP formation correlates with their ability to induce inositol phosphates production; the potentiation of cAMP formation and the inositol phosphates production are blocked by the group I mGluRs antagonists (S)-4-carboxyphenylglycine and are not affected by group II antagonist 2S,3S,4S)-2-methyl-2-(carboxycyclopropyl)-glycine or group III antagonist (S)-2-amino-2-methyl-4-phosphonobutanoic acid.
4.(+)-MCPG blocks induction of LTP in CA1 of rat hippocampus via agonist action at an mGluR group II receptor.
Breakwell NA1, Rowan MJ, Anwyl R. J Neurophysiol. 1998 Mar;79(3):1270-6.
We investigated the effect of metabotropic glutamate receptor (mGluR) ligands on the induction of long-term potentiation (LTP) of field excitatory postsynaptic potentials (EPSPs) in CA1 of rat hippocampus, in particular the manner by which the nonsubtype selective mGluR ligand alpha-methyl-4-carboxyphenylglycine [(+)-MCPG] blocks LTP induction. Normalized control LTP was blocked by (+)-MCPG (250 microM), but not by the mGluRI selective antagonist (S)-4-carboxyphenylglycine (4-CPG), the mGluRII selective antagonist 1/(2S,3S, 4S)-2-methyl-2-(carboxycyclopropyl) glycine (MCCG), or the mGluRIII antagonist (S)-2-amino-2-methyl-4-phosphonobutanoic acid/alpha-methyl (MAP4). In contrast the mGluRII agonist ((1S, 3S)-1-aminocyclopentante-1,3-dicarboxylic acid -(1S,3S)-ACPD-; 10 or 25 microM) completely and consistently blocked LTP. The block of LTP by both (1S,3S)-ACPD and (+)-MCPG could be prevented by preincubation with the mGluRII antagonist MCCG.
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CAS 157381-42-5 MAP4

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