Protein Information

Name mGluR5
Synonyms GPRC1E; GRM 5; GRM5; MGLUR 5; MGLUR5; MGLUR5A; MGLUR5B; Metabotropic glutamate receptor 5…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
11102477 Ango F, Pin JP, Tu JC, Xiao B, Worley PF, Bockaert J, Fagni L: Dendritic and axonal targeting of type 5 metabotropic glutamate receptor is regulated by homer1 proteins and neuronal excitation. J Neurosci. 2000 Dec 1;20(23):8710-6.

Depolarization of the neurons with a mixture of ionotropic glutamate receptor agonists, NMDA and kainate, or potassium channel blockers, tetraethylammonium and 4-aminopyridine, induced transient expression of endogenous Homer1a and persistent neuritic localization of transfected mGluR5 even long after degradation of Homer1a.
37(0,1,1,7) Details
12364493 Lee AC, Wong RK, Chuang SC, Shin HS, Bianchi R: Role of synaptic metabotropic glutamate receptors in epileptiform discharges in hippocampal slices. J Neurophysiol. 2002 Oct;88(4):1625-33.

Addition of 4-aminopyridine (4-AP; 100 microM) prolonged these bursts to 0.7-2 s.
The mGluR1 antagonist (S)-(+)-alpha-amino-4-carboxy-2-methylbenzeneacetic acid (LY 367385; 25-100 microM) and the mGluR5 antagonist 2-methyl-6-(phenylethynyl) pyridine (MPEP; 10-50 microM), applied separately, significantly reduced the duration of the synchronized discharges.
4(0,0,0,4) Details
18675825 Witkin JM, Baez M, Yu J, Eiler WJ 2nd: mGlu5 receptor deletion does not confer seizure protection to mice. Life Sci. 2008 Aug 29;83(9-10):377-80. Epub 2008 Jul 15.

Metabotropic glutamate mGlu5 receptors have been implicated in the regulation of seizures and have been suggested as a target against which discovery of novel anticonvulsants may be possible.
Chemically induced seizures induced by a variety of mechanisms including pentylenetetrazole, N-methyl-d-aspartic acid (NMDA), cocaine, kainic acid, aminophylline, 4-aminopyridine, strychnine, and nicotine did not differentially increase clonic, clonic/tonic, or lethality in WT vs. mGlu5 receptor KO mice.
2(0,0,0,2) Details
12629172 Gebremedhin D, Yamaura K, Zhang C, Bylund J, Koehler RC, Harder DR: Metabotropic glutamate receptor activation enhances the activities of two types of Ca2+-activated k+ channels in rat hippocampal astrocytes. J Neurosci. 2003 Mar 1;23(5):1678-87.

Patch-clamp analysis of K (+) channel currents in cultured astrocytes identified the existence of 71 +/- 6 and 161 +/- 11 pS single-channel K (+) currents that were sensitive to changes in voltage and [Ca (2+)](i) and blocked by external TEA but not by charybdotoxin, iberiotoxin, apamin, or 4-aminopyridine.
Expression of the metabotropic glutamate receptor (mGluR) subtypes mGluR1 and mGluR5 and the ionotropic glutamate receptor (iGluR) subtypes iGluR1 and iGluR4 were detected by RT-PCR and immunofluorescence analysis in cultured astrocytes.
1(0,0,0,1) Details
18538357 Salah A, Perkins KL: Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. Neuropharmacology. 2008 Jul;55(1):47-54. Epub 2008 Apr 23.

Here we tested the effects of the group I metabotropic glutamate receptor (mGluR) subtype-selective antagonists LY 367385 (mGlu1, 100 microM), MPEP (mGlu5, 10 microM), and MTEP (mGlu5, 500 nM) on this synchronous activity.
2(0,0,0,2) Details
14623765 White AM, Kylanpaa RA, Christie LA, McIntosh SJ, Irving AJ, Platt B: Presynaptic group I metabotropic glutamate receptors modulate synaptic transmission in the rat superior colliculus via 4-AP sensitive K (+) channels. Br J Pharmacol. 2003 Dec;140(8):1421-33. Epub 2003 Nov 17.

The K+ channel antagonist 4-aminopyridine (4-AP, 50-100 microm) converted the inhibitory effect of DHPG into facilitation.
The putative mGluR5-specific agonist (RS)-2-chloro-5-hydroxyphenylglycine (CHPG, 500 microm) also inhibited EPSPs.
1(0,0,0,1) Details