Protein Information

Name mGluR1
Synonyms GPRC1A; GRM 1; GRM1; GRM1 alpha; GRM1A; MGLUR 1; MGLUR1; MGLUR1A…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
12213266 Cozzi A, Meli E, Carla V, Pellicciari R, Moroni F, Pellegrini-Giampietro DE: Metabotropic glutamate 1 (mGlu1) receptor antagonists enhance GABAergic neurotransmission: a mechanism for the attenuation of post-ischemic injury and epileptiform activity?. Neuropharmacology. 2002 Aug;43(2):119-30.

In a mouse cortical wedge model, both muscimol and 3-MATIDA reduced the frequency of spontaneous bursts induced by 4-aminopyridine and this reduction was prevented by co-perfusion with bicuculline.
5(0,0,0,5) 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
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
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
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.
0(0,0,0,0) Details