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The delta(2)-opioid receptor subtype stimulates phosphoinositide metabolism in mouse periaqueductal gray matter

机译:delta(2)-阿片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-Pen(2,5)]enkephalin (DPDPE) and [D-Ala(2)]deltorphin II increased the formation of inositol phosphates (IPs) in mice periaqueductal gray matter (FAG) slices pre-labeled with myo-[H-3]inositol. Both delta-agonists caused an increase in IP accumulation in a dose-dependent manner (1-100 mu M) and which was pertussis toxin (0.5 mu g/mouse, icy) sensitive. This effect was blocked by the delta-antagonist ICI-174.864 (10 mu M). The presence of subtypes of the delta-opioid receptor (delta(1) and delta(2)) in FAG 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-Ala(2)]deltorphin II, suggesting the involvement of a population of delta receptors sensitive to the delta(2)-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 29-46 of the cloned delta-receptor mRNA, and FAG 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 delta(2)-opioid receptor subtype in the FAG. (C) 1998 Elsevier Science Inc. [References: 20]
机译:δ(δ)-阿片样物质激动剂[D-Pen(2,5)]脑啡肽(DPDPE)和[D-Ala(2)] deltorphin II增加了小鼠导水管周围灰质(FAG)中肌醇磷酸酯(IPs)的形成。标记有肌-[H-3]肌醇的切片。两种δ-激动剂都以剂量依赖的方式(1-100μM)引起IP积累的增加,并且对百日咳毒素(0.5μg /小鼠,冰冷)敏感。该作用被δ-拮抗剂ICI-174.864(10μM)阻断。药理研究表明FAG中存在δ阿片受体亚型(delta(1)和delta(2))。在这种大脑结构中,萘丁醚5'-异硫氰酸酯(5'-NTII),而不是7-苄叉神经内酯(BNTX)拮抗了DPDPE和[D-Ala(2)] deltorphin II的作用,表明该人群参与了对此效应对delta(2)-拮抗剂NT II敏感的delta受体。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或29-46位核苷酸的反义寡脱氧核苷酸(ODN),以及来自这些动物的FAG切片用于体外测定。结果表明,所报道的磷酸肌醇(PI)水解的增加取决于FAG中delta(2)-鸦片受体亚型的激动剂激活。 (C)1998 Elsevier Science Inc. [参考:20]

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