首页> 外文期刊>Life sciences >The delta2-opioid receptor subtype stimulates phosphoinositide metabolism in mouse periaqueductal gray matter.
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The delta2-opioid receptor subtype stimulates phosphoinositide metabolism in mouse periaqueductal gray matter.

机译:delta2-阿片样物质受体亚型刺激小鼠导水管周围灰质中的磷酸肌醇代谢。

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The delta(delta)-opioid agonists [D-Pen2,5]enkephalin (DPDPE) and [D-Ala2]deltorphin II increased the formation of inositol phosphates (IPs) in mice periaqueductal gray matter (PAG) slices pre-labeled with myo-[3H]inositol. Both delta-agonists caused an increase in IP accumulation in a dose-dependent manner (1-100 microM) and which was pertussis toxin (0.5 microg/mouse, i.c.v.) sensitive. This effect was blocked by the delta-antagonist ICI-174.864 (10 microM). The presence of subtypes of the delta-opioid receptor (delta1 and delta2) in PAG has been suggested by pharmacological studies. In this brain structure, naltrindrole 5'-isothiocyanate (5'-NTII), but not 7-benzylidenenaltrexone (BNTX), antagonized the effects of DPDPE and [D-Ala2]deltorphin II, suggesting the involvement of a population of delta receptors sensitive to the delta2-antagonist NT II on this effect. To further investigate the participation of delta-receptor subtypes in the stimulation of IPs formation, mice were injected with antisense oligodeoxynucleotides (ODNs) directed to nucleotides 7-26 or 2946 of the cloned delta-receptor mRNA, and PAG slices from these animals were used in in vitro assays. The results demonstrate that the reported increase of phosphoinositide (PI) hydrolysis depends on the agonist activation of the delta2-opioid receptor subtype in the PAG.
机译:δ(δ)-阿片样物质激动剂[D-Pen2,5]脑啡肽(DPDPE)和[D-Ala2] deltorphin II增加了预先标记有心肌的小鼠导水管周围灰质(PAG)切片中肌醇磷酸酯(IPs)的形成。 -[3H]肌醇。两种δ-激动剂均以剂量依赖的方式(1-100 microM)引起IP积累的增加,并且对百日咳毒素(0.5 microg /小鼠,i.c.v。)敏感。这种作用被δ-拮抗剂ICI-174.864(10 microM)阻断。药理研究表明,PAG中存在δ阿片受体亚型(δ1和δ2)。在这种大脑结构中,萘丁醚5'-异硫氰酸酯(5'-NTII),而不是7-苄基神经烯酮(BNTX)拮抗了DPDPE和[D-Ala2] deltorphin II的作用,表明参与了敏感的δ受体群体对δ2-拮抗剂NT II具有这种作用。为了进一步研究δ受体亚型参与IP形成的刺激,向小鼠注射了针对克隆的δ受体mRNA的7-26位或2946位核苷酸的反义寡脱氧核苷酸(ODN),并使用了来自这些动物的PAG切片在体外测定中。结果表明,所报道的磷酸肌醇(PI)水解的增加取决于PAG中δ2-阿片样物质受体亚型的激动剂活化。

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