Metabotropic glutamate receptor subtype

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Azkue, J..J., Murga, M., Fernandez-Capetillo, O., Mateos, J. M., Elezgarai, I., Benitez, R., Osorio, A., Diez, J., Puente, N., Bilbao, A., Bidaurrazaga, A., Kuhn, R., Grandes, P.. Immunoreactivity for the group III metabotropic glutamate receptor subtype mGluR4a in the superficial laminae of the rat spinal dorsal horn. J. Comp. Neurol. 2001, 430, 448-57. 

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The NMDA, AMPA, and kainate subtypes of glutamate receptors are probably all linked to an ion channel. The metabotropic glutamate receptor subtype, however, belongs to the G protein—linked superfamily of receptors. The specific functioning of the various subtypes of glutamate receptors is the focus of intense debate. The actions at NMDA receptors will be emphasized here in our discussions on excitotoxicity. 

In the third and last section, we will report the construction of a new pharmacophore model for metabotropic glutamate receptor subtype 4 (mGlu4R) agonists. In spite of the fact that the available dataset is particularly difficult for pharmacophore modeling, we will show that the validation methods used allowed us to have great confidence in the hypotheses generated. 

Pharmacology of Metabotropic Glutamate Receptor Subtype 4 (mGlu4)... 

Karim, F., Wang, C. C., and Gereau, R. W. (2001). Metabotropic glutamate receptor subtypes 1 and 5 are activators of extracellular signal-regulated kinase signaling required for inflammatory pain in mice. J. Neurosci. 21, 3771-3779. 

Benquet P, Gee CE, Gerber U. 2002. Two distinct signaling pathways upregulate NMDA receptor responses via two distinct metabotropic glutamate receptor subtypes. J Neu-rosci 22 9679-9686. 

Lindsley CW, Wisnoski DD, Leister WH, O Brien JA, Lemi-are W, Williams DL Jr, Burno M, Sur C, Kinney GG, Petti-bone DJ, Miller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR. Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of V-(l,3-Diphenyl-lH-pyrazol-5-yl) benzamides that potentiate receptor function in vivo J. Med. Chem. 2004 47 5825. 

Pettibone, D. J., Tiller, P. R., Smith, S., Duggan, M. E., Hartman, G. D., Conn, P. J., and Huff, J. R. (2004). Discovery of the positive allosteric modulators of the metabotropic glutamate receptor subtype 5 from a series of N-(l,3-diphenyl-l-H-pyrazol-5-yl)benzamides that potentiate receptor function. J. Med. Chem. 47 5825-5828. 

Wada E, Shigemoto R, Kinoshita A, Ohishi H, Mizuno N. 1998. Metabotropic glutamate receptor subtypes in ajoan terminals of projection fibers from the main and accessory olfactory bulbs A light and electron microscopic immunohistochemical study in the rat. J Comp Neurol 393 493-504. 

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Tang FR, Sim MK (1997) Metabotropic glutamate receptor subtype-la (mGluRla) immunoreactivity in ependymal cells of the rat caudal medulla oblongata and spinal cord. Neurosci Lett 225 177-180. 

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Minakami R, lida K, Hirakawa N, Sugiyama H (1995) The expression of two splice variants of metabotropic glutamate receptor subtype 5 in the rat brain and neuronal cells during development. J Neurochem 65 1536-1542. 

Ossowska K, Konieczny J, Wolfarth S et al (2001) Blockade of the metabotropic glutamate receptor subtype 5 (mGluR5) produces antiparkinsonian-like effects in rats. Neuropharmacology 41 413-420... 

Layton ME (2005) Subtype-selective noncompetitive modulators of metabotropic glutamate receptor subtype 1 (mGluRl). Curr Top Med Chem 5 859-867... 

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