薬理学　　２１世紀への架け橋　　グルタミン酸受容体の薬理学　　アゴニストを中心として

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書誌事項

タイトル別名
  • Pharmacology. The Bridge to the 21st Century. Pharmacology of the glutamate receptor.
  • グルタミンサン ジュヨウタイ ノ ヤクリガク アゴニスト オ チュウシン ト シテ
  • 薬理学－21世紀への架け橋

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The history of pharmacological examinations of glutamate receptor agonists such as kainic acid, quisqualic acid, acromelic acid, L-CCG-I, DCG-IV and L-F2CCG-I was described. Kainic acid is one of the most potent excitants in the mammalian central neurons, and its powerful excitatory actions gave rise to the excitotoxic concept that glutamate destroys neurons by excessive activation of excitatory receptors. Single systemic administration of acromelic acid, a kainate analog, caused behavioral and pathological effects quite different from those seen after systemic administration of kainate in the rat, demonstrating that the distribution of neuron damage caused by various excitatory amino acids is not always identical even if their receptors are in the same pharmacological category. 2-(Carboxycyclopropyl) glycine (CCG) is a conformationally restricted analogue of glutamate. CCG and its derivatives demonstrate unique neuropharmacological actions; for example, L-CCG-I and DCG-IV (a carboxylated derivative of L-CCG-I) relatively preferentially activate group II mGluRs. Prolonged infusion of very small amounts of DCG-IV showed a bell-shaped doseresponse relationship with regard to protection against kainate-induced neurotoxicity. Low concentrations of L-glutamate neither affected spinal reflexes nor the resting membrane potentials of motoneurons, but preferentially potentiated the depression of monosynaptic excitation caused by L-F2CCG-I. Following L-F2 CCG-I treatment, L-glutamate decreased the monosynaptic spinal reflexes in a concentration-dependent manner, indicating a ‘priming’ effect of L-F2CCG-I. Thus, pharmacological actions of mGluR agonists are of great interest and remain to be clarified.

収録刊行物

  • 日本薬理学雑誌

    日本薬理学雑誌 116 (3), 125-131, 2000

    公益社団法人 日本薬理学会

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