Excitatory amino acid receptor

Compounds that have agonistic properties at glutamate or aspartate receptors are also CNS stimulants, readily cause convulsions, and presumably could also be employed as analeptics. Three separate excitatory amino acid receptor subtypes have been characterized pharmacologically, based on the relative potency of synthetic agonists. These three receptors are named for their respective prototypical agonists A/-methyl-D-aspartate [6384-92-5]... 

Lynch DR, Guttmann RP (2002) Excitotoxicity perspectives based on N-methyl-D-aspartate receptor subtypes. J Pharmacol Exp Ther 300(3) 717-723 Magnuson DS, Knudsen BE, Geiger JD, Brownstone RM, Nath A (1995) Human immunodeficiency virus type 1 tat activates non-N-methyl-D-aspartate excitatory amino acid receptors and causes neurotoxicity. Ann Neurol 37(3) 373-380 Mamdouh Z, Chen X, Kerini LM, Maxfield FR, Muller WA (2003) Targeted recycling of PECAM from endothelial surface-connected compartments during diapedesis. Nature 421(6924) 748-753... 

Colingridge, G and Singer, W (1990) Excitatory amino acid receptors and synaptic plasticity. Trends Pharm. Sci. 11 290-296. 

MacDonald, J. F. and Nowak, L. M., Mechanisms of blockade of excitatory amino acid receptor channels, TIPS, 11(4), 167-172, 1990. 

Collingridge, G. L. Lester, R. A. (1989). Excitatory amino acid receptors in the vertebrate central nervous system. Pharmacol Rev. 41, 143-210. 

Monaghan, D. T., Bridges, R. J. Cotman, C. W. (1989). The excitatory amino acid receptors their classes, pharmacology and distinct properties in the function of the central nervous system. A Rev. Pharmacol Toxicol. 29, 365-402. 

Excitatory amino acid-receptor antagonists can provide neuroprotection in experimental models of hypoxia-ischemia 565... 

Siegel, S. J., Janssen, W. G Tullai, J. W Rogers, S. W., Moran, T., Heinemann, S. F., and Morrison, J. H. (1995) Distribution of the excitatory amino acid receptor subunits GluR2(4) in monkey hippocampus and colocalization with subunits GluR5-7 and NMDAR1../. Neurosci. 15, 2707-2719. 

Boss V, Conn PJ. (1992). Metabotropic excitatory amino acid receptor activation stimulates phospholipase D in hippocampal slices. J Neurochem. 59(6) 2340-43. 

Laudrup P, Kiitgaard H. (1993). Metabotropic and ionotropic excitatory amino acid receptor agonists induce different behaviorai effects in mice. EurJ Pharmacol. 250(1) 15-22. 

Excitatory amino acid receptors glutamate receptor... 

In addition to epilepsy, neuronal death due to the toxic effects of glutamate has also been implicated in cerebral ischaemia associated with multi-infarct dementia and possibly Alzheimer s disease. With the plethora of selective excitatory amino acid receptor antagonists currently undergoing development, some of which are already in clinical trials, one may expect definite advances in the drug treatment of neurodegenerative disorders in the near future. 

Modification of ligand properties (affinity, agonist, or antagonist character) toward amino acid receptors (e.g., excitatory amino acid receptors). 

Dingledine, R., McBain, C.J., and McNamara, J.O. (1990) Excitatory amino acid receptors in epilepsy. Trends Tharmacol Set 11 334-338. 

Excitatory Amino Acid Receptors. Design of Agonists and Antagonists, Krogsgaard-Larsen, P, Hansen, J. J., Eds. Ellis Horwood Chichester, UK, 1992. 

Southam, E., East, S. J., and Garthwaite, J. (1991). Excitatory amino acid receptors coupled to the nitric oxide/cyclic GMP pathway in rat cerebellum during development. 

Colladocano, I., Gonzalez-Garcia, R., Lopez de Uralde-Garmendia, B. (Eli Lilly) Excitatory amino acid receptor modulators, WO 0192213. 

Zheng, F., Gallagher, J.P., Connor, J.A. Activation of a metabotropic excitatory amino acid receptor potentiates spike-driven calcium increases in neurons of the dorsolateral septum, J. Neurosci. 1996, 16, 6079-6088. 

Chapman, V., Dickenson, A. H. Time-related roles of excitatory amino acid receptors during persistent noxiously evoked responses of rat dorsal horn neurones, Brain Res., 1995, 703, 45-50. 

Hao, J.-X. and Xu, X.-J. Treatments of a chronic allodynia-like response in spinally injured rats effects of systemically administered excitatory amino acid receptor antagonists, Pain 1996, 66, 279-285. 

Hunter, J. C and Singh, L. Role of excitatory amino acid receptors in the mediation of the nociceptive response to formalin in the rat, Neurosci. Lett. 1994, 174, 217-221. 

Kemp, J. A., Foster, A. C., Wong, E. H. F. Noncompetitive antagonists of excitatory amino acid receptors, Trends Neurosci., 1987, 10, 294-298. 

Mao, J., Price, D. D., Mayer, D. J. Thermal hyperalgesia in association with the development of morphine tolerance in rats roles of excitatory amino acid receptors and protein kinase C, J. Neurosci. 1994, 14, 2301-2312. 

In brain tissue, low concentrations of glutamate and aspartate perform as neurotransmitters, but at high concentration these amino acids act as neurotoxins. Major advances in the excitatory amino acid receptor field have come from the identification, characterization, and cloning of different families of receptors and transporters (Dingledine and McBain, 1999). These receptors and transporters are specialized... 

---