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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Watkins J C, Pook P C, Sunter D C, Davies J, Honore T

Department of Pharmacology, School of Medical Sciences, Bristol, UK.

Adv Exp Med Biol. 1990;268:49-55. doi: 10.1007/978-1-4684-5769-8_6.

The KD values for a range of antagonists including DGG, pCB-PzDA, pBB-PzDA, HDC-QXCA, DNQX and CNQX have been determined using a series of non-NMDA receptor agonists in the isolated spinal cord of the neonatal rat. 2) CNQX and DNQX, and, to a lesser extent, DCH-QXCA, were by far the most potent antagonists, although the degree of selectivity did not vary much throughout the whole range of antagonists used. 3) AMPA and domoate were the most and least sensitive agonists, respectively, to the action of all the antagonists. Ionophoretic experiments in the cat spinal cord in vivo confirmed this order of susceptibility in the case of the antagonists CNQX and pCB-PzDA. 4) Acromelic acid A was a more AMPA-like than domoate-like agonist. 5) The results suggest that two receptors contribute to the responses induced by several of the agonists, and that quisqualate and kainate are less selective agonists at these receptors than are AMPA and domoate, respectively.

在新生大鼠离体脊髓中，使用一系列非 NMDA 受体激动剂测定了包括 DGG、pCB - PzDA、pBB - PzDA、HDC - QXCA、DNQX 和 CNQX 在内的一系列拮抗剂的 KD 值。2) CNQX 和 DNQX，以及在较小程度上的 DCH - QXCA，是迄今为止最有效的拮抗剂，尽管在所使用的整个拮抗剂范围内选择性程度变化不大。3) AMPA 和海人酸分别是对所有拮抗剂作用最敏感和最不敏感的激动剂。在猫脊髓体内进行的离子电泳实验证实了拮抗剂 CNQX 和 pCB - PzDA 情况下的这种敏感性顺序。4) 肢端酸 A 是一种比海人酸更类似 AMPA 的激动剂。5) 结果表明，两种受体参与了几种激动剂诱导的反应，并且使君子酸盐和红藻氨酸盐在这些受体上分别比 AMPA 和海人酸的选择性更低。

Watkins J C, Pook P C, Sunter D C, Davies J, Honore T

Department of Pharmacology, School of Medical Sciences, Bristol, UK.

Adv Exp Med Biol. 1990;268:49-55. doi: 10.1007/978-1-4684-5769-8_6.

The KD values for a range of antagonists including DGG, pCB-PzDA, pBB-PzDA, HDC-QXCA, DNQX and CNQX have been determined using a series of non-NMDA receptor agonists in the isolated spinal cord of the neonatal rat. 2) CNQX and DNQX, and, to a lesser extent, DCH-QXCA, were by far the most potent antagonists, although the degree of selectivity did not vary much throughout the whole range of antagonists used. 3) AMPA and domoate were the most and least sensitive agonists, respectively, to the action of all the antagonists. Ionophoretic experiments in the cat spinal cord in vivo confirmed this order of susceptibility in the case of the antagonists CNQX and pCB-PzDA. 4) Acromelic acid A was a more AMPA-like than domoate-like agonist. 5) The results suggest that two receptors contribute to the responses induced by several of the agonists, and that quisqualate and kainate are less selective agonists at these receptors than are AMPA and domoate, respectively.

在新生大鼠离体脊髓中，使用一系列非 NMDA 受体激动剂测定了包括 DGG、pCB - PzDA、pBB - PzDA、HDC - QXCA、DNQX 和 CNQX 在内的一系列拮抗剂的 KD 值。2) CNQX 和 DNQX，以及在较小程度上的 DCH - QXCA，是迄今为止最有效的拮抗剂，尽管在所使用的整个拮抗剂范围内选择性程度变化不大。3) AMPA 和海人酸分别是对所有拮抗剂作用最敏感和最不敏感的激动剂。在猫脊髓体内进行的离子电泳实验证实了拮抗剂 CNQX 和 pCB - PzDA 情况下的这种敏感性顺序。4) 肢端酸 A 是一种比海人酸更类似 AMPA 的激动剂。5) 结果表明，两种受体参与了几种激动剂诱导的反应，并且使君子酸盐和红藻氨酸盐在这些受体上分别比 AMPA 和海人酸的选择性更低。