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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

Department of Veterinary Basic Sciences, Royal Veterinary College, London, U.K.

Gen Pharmacol. 1990;21(2):165-70. doi: 10.1016/0306-3623(90)90895-s.

Drugs with phencyclidine (PCP)-like activity in behavioural discrimination and [3H]PCP binding studies share anticonvulsant properties. 2. We have compared the rank order potency of a series of PCP-like compounds as N-methylaspartate (NMA) antagonists, determined from previously published studies from our laboratory, with their rank order anticonvulsant potencies as determined by two independent research groups in three different in vivo models of experimentally-induced epilepsy. 3. Rank order potency for NMA antagonism correlated well with rank order anticonvulsant potency. Furthermore, the systemic doses required for an effective blockade of NMA-evoked excitations were, in most cases, similar to those which produced anticonvulsant activity. 4. The results suggest that functional NMA antagonism may underlie the shared anticonvulsant properties of structurally dissimilar compounds with PCP-like activity.

在行为辨别和[3H]苯环己哌啶结合研究中具有苯环己哌啶（PCP）样活性的药物具有抗惊厥特性。2. 我们将一系列PCP样化合物作为N-甲基-D-天冬氨酸（NMA）拮抗剂的效价排序（根据我们实验室先前发表的研究确定），与两个独立研究小组在三种不同的实验性癫痫体内模型中确定的它们的抗惊厥效价排序进行了比较。3. NMA拮抗的效价排序与抗惊厥效价排序密切相关。此外，在大多数情况下，有效阻断NMA诱发的兴奋所需的全身剂量与产生抗惊厥活性的剂量相似。4. 结果表明，功能性NMA拮抗作用可能是具有PCP样活性的结构不同的化合物共有的抗惊厥特性的基础。

Department of Veterinary Basic Sciences, Royal Veterinary College, London, U.K.

Gen Pharmacol. 1990;21(2):165-70. doi: 10.1016/0306-3623(90)90895-s.

Drugs with phencyclidine (PCP)-like activity in behavioural discrimination and [3H]PCP binding studies share anticonvulsant properties. 2. We have compared the rank order potency of a series of PCP-like compounds as N-methylaspartate (NMA) antagonists, determined from previously published studies from our laboratory, with their rank order anticonvulsant potencies as determined by two independent research groups in three different in vivo models of experimentally-induced epilepsy. 3. Rank order potency for NMA antagonism correlated well with rank order anticonvulsant potency. Furthermore, the systemic doses required for an effective blockade of NMA-evoked excitations were, in most cases, similar to those which produced anticonvulsant activity. 4. The results suggest that functional NMA antagonism may underlie the shared anticonvulsant properties of structurally dissimilar compounds with PCP-like activity.

在行为辨别和[3H]苯环己哌啶结合研究中具有苯环己哌啶（PCP）样活性的药物具有抗惊厥特性。2. 我们将一系列PCP样化合物作为N-甲基-D-天冬氨酸（NMA）拮抗剂的效价排序（根据我们实验室先前发表的研究确定），与两个独立研究小组在三种不同的实验性癫痫体内模型中确定的它们的抗惊厥效价排序进行了比较。3. NMA拮抗的效价排序与抗惊厥效价排序密切相关。此外，在大多数情况下，有效阻断NMA诱发的兴奋所需的全身剂量与产生抗惊厥活性的剂量相似。4. 结果表明，功能性NMA拮抗作用可能是具有PCP样活性的结构不同的化合物共有的抗惊厥特性的基础。