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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >The cannabinoid receptor antagonist SR-141716 does not readily antagonize open-field effects induced by the cannabinoid receptor agonist (R)-methanandamide in rats.
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The cannabinoid receptor antagonist SR-141716 does not readily antagonize open-field effects induced by the cannabinoid receptor agonist (R)-methanandamide in rats.

机译：大麻素受体拮抗剂SR-141716不能轻易拮抗大麻素受体激动剂（R）-甲烷酰胺在大鼠中引起的开放视野效应。

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摘要

This study examined the effects of the cannabinoid CB(1) receptor agonist (R)-methanandamide and the CB(1) receptor antagonist SR-141716 on open-field behaviors in rats. Animals were examined after administration of (R)-methanandamide (dose range 10 to 30 mg/kg) plus vehicle, and the two drugs in combination; the dose range of SR-141716 was 0.3 to 5.6 mg/kg. Injections were given intraperitoneally 20 min prior to initial testing. Additional exposures to the open-field arena occurred for the groups treated with 30 mg/kg (R)-methanandamide at 60 and 120 min post administration. There was a dose-related suppression of ambulation (horizontal activity) and rearing (vertical activity) after (R)-methanandamide administration. Coadministration of SR-141716 did not counteract the suppression induced by 10 and 18 mg/kg (R)-methanandamide but rather tended to augment it, especially with regard to ambulation using SR-141716 doses of 1 mg/kg and up. The latency to leave the starting area in the center of the field was significantly elevated by 30 mg/kg (R)-methanandamide. This effect was completely blocked by SR-141716. With increasing doses of SR-141716, there was an increase in grooming and scratching. Generally, the strongest effects occurred 20 min post administration with the exception of grooming, which reached maximum at 60 min post. Differences in the number of circlings, vocalizations, urination, and defecation generally did not differ clearly among treatments. These results coupled with previous open-field data examining combinations of Delta(9)-tetrahydrocannabinol (Delta(9)-THC) and SR-141716 [Pharmacol. Biochem. Behav. 73 (2002) 911] underscore pharmacological differences between (R)-methanandamide and Delta(9)-THC revealed by their interactions with SR-141716.
机译：这项研究检查了大麻素CB（1）受体激动剂（R）-甲酰胺和CB（1）受体拮抗剂SR-141716对大鼠开放视野行为的影响。给予（R）-甲酰胺（剂量范围10至30 mg / kg）加赋形剂和两种药物合用后检查动物。 SR-141716的剂量范围为0.3至5.6 mg / kg。在初次测试前20分钟腹膜内注射。在给药后60和120分钟，用30 mg / kg（R）-甲烷二胺治疗的组在野外场所有其他暴露。 （R）-甲烷酰胺给药后，有一定剂量相关的活动抑制（水平活动）和饲养（垂直活动）抑制。 SR-141716的共同给药不能抵消10和18 mg / kg（R）-甲酰胺的诱导抑制作用，而是会增强抑制作用，尤其是对于使用1 mg / kg或更高剂量的SR-141716的下床活动。离开田间中心起始区域的潜伏期显着增加了30 mg / kg（R）-甲烷酰胺。 SR-141716完全阻止了此效果。随着SR-141716剂量的增加，修饰和刮擦也有所增加。通常，除修饰外，最强的作用发生在给药后20分钟，在修饰后60分钟达到最大。一般情况下，治疗的循环次数，发声，排尿和排便次数没有明显差异。这些结果与先前的公开数据一起研究了Delta（9）-四氢大麻酚（Delta（9）-THC）和SR-141716的组合[Pharmacol。生化。行为。 73（2002）911]强调了（R）-甲酰胺和Delta（9）-THC在与SR-141716的相互作用中的药理差异。

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