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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >N-methyl-D-aspartate receptor antagonist activity and phencyclidine-like behavioral effects of the pentadecapeptide, (Ser1)histogranin.
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N-methyl-D-aspartate receptor antagonist activity and phencyclidine-like behavioral effects of the pentadecapeptide, (Ser1)histogranin.

机译：五肽（Ser1）组蛋白的N-甲基-D-天冬氨酸受体拮抗剂活性和苯环利定样的行为作用。

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摘要

The behavioral and pharmacologic profiles of [Ser1]histogranin ([Ser1]HN) were assessed by monitoring its ability to displace the binding of the specific N-methyl-D-aspartate (NMDA) receptor ligand, [3H]CGP 39653, to block the convulsant effects of NMDA and other excitatory agents in mice, and to produce phencyclidine (PCP)-like behavioral effects in rats. The peptide potently inhibited [3H]CGP 39653 binding to membrane preparations of rat brain with an IC50 of 198 nM and a maximal inhibition of 34% of the specific binding activity. Saturation binding experiments with [3H]CGP 39653 in the absence and presence of [Ser1]HN (2 microM) indicated that the inhibitory effect of the peptide was noncompetititive, producing a decrease in the maximal number of binding sites (Bmax of 62.5 fmol/mg protein as compared with 91.3 fmol/mg protein in control), but no significant change in the affinity (Kd of 4.5 nM as compared with 5.1 nM in control). Intracerebroventricular (ICV) injection of [Ser1]HN (10-100 nmol) in mice evoked a dose-dependent and selective blockade of NMDA-induced convulsions. In rats, [Ser1]HN (2.5-100 nmol, ICV) produced dose-dependent stereotypy, ataxia, and locomotion similar to those observed with PCP, at doses ranging between 50 and 400 nmol. The data indicate that [Ser1]HN noncompetitively interacts with the NMDA receptor, an action that goes along with its in vivo NMDA receptor antagonist activity and PCP-like behavioral effects.
机译：[Ser1] histogranin（[Ser1] HN）的行为和药理学特征是通过监测其取代特定N-甲基-D-天冬氨酸（NMDA）受体配体[3H] CGP 39653结合的能力来评估的NMDA和其他兴奋剂对小鼠的惊厥作用，并在大鼠中产生苯环利定（PCP）样的行为作用。该肽有效抑制[3H] CGP 39653与大鼠脑膜制剂的结合，IC50为198 nM，最大抑制比结合活性的34％。在[Ser1] HN（2 microM）不存在下使用[3H] CGP 39653进行的饱和结合实验表明，该肽的抑制作用是非竞争性的，从而导致最大结合位点数量减少（Bmax为62.5 fmol /与对照组中的91.3 fmol / mg蛋白相比，该蛋白的蛋白含量更高，但亲和力没有显着变化（与对照组中的5.1 nM相比，Kd为4.5 nM）。小鼠脑室内（ICV）注射[Ser1] HN（10-100 nmol）引起了NMDA诱导的惊厥的剂量依赖性和选择性阻断。在大鼠中，[Ser1] HN（2.5-100 nmol，ICV）在50至400 nmol的剂量范围内产生与PCP相似的剂量依赖性定型，共济失调和运动。数据表明[Ser1] HN与NMDA受体非竞争性相互作用，这一作用与其体内NMDA受体拮抗剂的活性和PCP样的行为效应一起发生。

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