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- W1486194914 abstract "Summaryo1.Glutamate is the predominant endogenous EAA at fast-acting synapses in the CNS but also serves an equally important function as an intermediate in carbohydrate and nitrogen metabolism.2.Other endogenous EAAs such as aspartate, cysteine sulphinate, and homocysteate may also function as excitatory transmitters.3.Information transfer between neurons using the EAAs is mediated by at least four subtypes of receptor, namely, the NMDA, AMPA, KA, and metabotropic receptors.4.The NMDA, AMPA, and KA receptor subtypes are directly linked to cation channels, whereas the mGluR is coupled via a G protein to various intracellular second messengers.5.The NMDA receptor exhibits special pharmacological properties consistent with an involvement in higher neural functions.6.Paradoxically, the same properties of the NMDA receptor may be responsible for initiating neuronal cell damage evident in a number of acute and chronic neuropathologies.7.AMPA and KA receptors contribute to the faster excitatory neurotransmission; AMPA receptor activation appears to provide the initial depolarizing stimulus necessary for removing the voltage-block of the NMDA receptor-coupled ion channel.8.The slower-acting mGluRs may serve a modulatory role in neurotransmission. At present, their role in normal and abnormal brain function is uncertain.9.A number of highly potent and selective EAA receptor antagonists have been synthesized; unfortunately, their inability to permeate the blood-brain barrier following systemic administration means that none are currently in clinical use. It is expected, however, that suitable drugs will soon be developed. Glutamate is the predominant endogenous EAA at fast-acting synapses in the CNS but also serves an equally important function as an intermediate in carbohydrate and nitrogen metabolism. Other endogenous EAAs such as aspartate, cysteine sulphinate, and homocysteate may also function as excitatory transmitters. Information transfer between neurons using the EAAs is mediated by at least four subtypes of receptor, namely, the NMDA, AMPA, KA, and metabotropic receptors. The NMDA, AMPA, and KA receptor subtypes are directly linked to cation channels, whereas the mGluR is coupled via a G protein to various intracellular second messengers. The NMDA receptor exhibits special pharmacological properties consistent with an involvement in higher neural functions. Paradoxically, the same properties of the NMDA receptor may be responsible for initiating neuronal cell damage evident in a number of acute and chronic neuropathologies. AMPA and KA receptors contribute to the faster excitatory neurotransmission; AMPA receptor activation appears to provide the initial depolarizing stimulus necessary for removing the voltage-block of the NMDA receptor-coupled ion channel. The slower-acting mGluRs may serve a modulatory role in neurotransmission. At present, their role in normal and abnormal brain function is uncertain. A number of highly potent and selective EAA receptor antagonists have been synthesized; unfortunately, their inability to permeate the blood-brain barrier following systemic administration means that none are currently in clinical use. It is expected, however, that suitable drugs will soon be developed." @default.
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- W1486194914 date "1997-01-01" @default.
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- W1486194914 title "Chapter 6 Excitatory amino acid receptors" @default.
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- W1486194914 doi "https://doi.org/10.1016/s1569-2582(97)80068-2" @default.
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