Pharmacological identification of SM-21, the novel sigma(2) antagonist.

Ghelardini C; Galeotti N; Bartolini A

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Pharmacological identification of SM-21, the novel sigma(2) antagonist.

机译：新型sigma（2）拮抗剂SM-21的药理学鉴定。

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SM-21 is a tropane analogue with high affinity and selectivity for sigma(2) receptor subtype. In the absence of highly selective sigma(2) antagonists, the aim of the present study was to determine whether SM-21 is endowed with antagonistic activity. The experiments were conducted in rats by inducing neck dystonia, which is reported to be subsequent to activation of sigma(2) receptors. SM-21 (10 nmol/0.5 microl) was able to prevent torsion of the neck obtained by administration of the sigma(1)-sigma(2) agonist 1,3-di-(2-tolyl)guanidine (DTG, 5 nmol/0.5 microl) in the red nucleus. These data indicate that SM-21 is a potent and selective sigma(2) antagonist.

机译：SM-21是对sigma（2）受体亚型具有高亲和力和选择性的托烷类似物。在没有高度选择性的sigma（2）拮抗剂的情况下，本研究的目的是确定SM-21是否具有拮抗活性。该实验是通过诱导颈部肌张力障碍在大鼠中进行的，据报道这是在激活sigma（2）受体之后进行的。 SM-21（10 nmol / 0.5 microl）能够预防通过施用sigma（1）-sigma（2）激动剂1,3-二-（2-甲苯基）胍（DTG，5 nmol）获得的颈部扭转/0.5微升）在红色核中。这些数据表明SM-21是有效的选择性sigma（2）拮抗剂。

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《Pharmacology, Biochemistry and Behavior》 |2000年第3期|共4页
作者
Ghelardini C; Galeotti N; Bartolini A;
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正文语种 eng
中图分类药理学;
关键词
Analgesics; Butyrates; Receptors; sigma; Red Nucleus; Torticollis; Tropanes; 镇痛药; 丁醋酸盐类; 受体; Σ; 红核; 斜颈; 托烷类;

机译：Analgesics;Butyrates;Receptors;sigma;Red Nucleus;Torticollis;Tropanes;镇痛药;丁醋酸盐类;受体;Σ;红核;斜颈;托烷类;

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Pharmacological identification of SM-21, the novel sigma(2) antagonist.

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