1,4-dibenzylpiperazines possess anticocaine activity

1,4-dibenzylpiperazines possess anticocaine activity
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DOI:
10.1016/s0960-894x(02)01034-x
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发表时间:
2003-02-24
影响因子:
2.7
通讯作者:
Coop, A
Coop, A
中科院分区:
医学4区
文献类型:
--
作者:
Foster, A;Wu, HF;Coop, A

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N,N-二苄基哌嗪对 sigma 受体具有高亲和力,我们旨在通过引入已知可增强其他 sigma 配体中此类活性的取代基来增强其抗可卡因活性。配体对 sigma-1 受体具有高亲和力,但其减弱可卡因诱导的惊厥的活性与 sigma-1 结合亲和力并不相关,并且可能与其 sigma-2 结合亲和力更密切相关。 (C) 2003 Elsevier Science Ltd. 保留所有权利。
N,N-Dibenzylpiperazines have high affinity for sigma receptors, and we aimed to increase their anticocaine activity by introducing substituents known to enhance such activity in other sigma ligands. Ligands with high affinity for sigma-1 receptors resulted, but their activity in attenuating cocaine-induced convulsions did not cot-relate with sigma-l binding affinity, and may be more closely related to their sigma-2 binding affinities. (C) 2003 Elsevier Science Ltd. All rights reserved.