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首页> 外文期刊>Japanese Journal of Pharmacology >Effect of 1DMe, a neuropeptide FF analog, on acetylcholine release from myenteric plexus of guinea pig ileum.
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Effect of 1DMe, a neuropeptide FF analog, on acetylcholine release from myenteric plexus of guinea pig ileum.

机译:1DMe,一种神经肽FF类似物,对豚鼠回肠肌层神经丛乙酰胆碱释放的影响。

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Since neuropeptide FF (NPFF) is a putative neurotransmitter to exert anti-opioid activity, we examined the effects of [D-Tyr', (NMe)Phe3]neuropeptide FF (IDMe), a stable NPFF analog, on acetylcholine (ACh) release from a longitudinal muscle-myenteric plexus (LMMP) preparation of guinea pig ileum in which opioids were known to inhibit ACh release when muscarinic autoinhibition was not fully activated. In the presence of atropine, 1DMe increased spontaneous and electrical field stimulation (EFS)-evoked ACh release in a concentration-dependent manner. Naloxone also increased ACh release. The stimulatory effects of 1DMe and naloxone were not additive. In the absence of atropine, 1DMe did not affect ACh release. Morphine decreased spontaneous and EFS-evoked ACh release in the presence of 1 microM atropine. 1DMe as well as naloxone counteracted the inhibitory effects of morphine on EFS-evoked ACh release. The combination of 1DMe and naloxone was not more inhibitory than either drug alone. 1DMe had no appreciable effect on norepinephrine-induced inhibition of spontaneous and EFS-evoked ACh release. These results first demonstrated the effects of a NPFF analog on neurotransmitter release: 1DMe had a stimulatory effect on spontaneous and EFS-induced ACh release from the LMMP preparation of guinea pig ileum, probably by counteracting the inhibitory effect of endogenous opioids on ACh release.
机译:由于神经肽FF(NPFF)是发挥抗阿片类药物活性的假定神经递质,因此我们研究了稳定的NPFF类似物[D-Tyr',(NMe)Phe3]神经肽FF(IDMe)对乙酰胆碱(ACh)释放的影响来自豚鼠回肠的纵向肌-肠系膜神经丛(LMMP)制剂,其中已知当毒蕈碱自身抑制作用未完全激活时,阿片类药物可抑制ACh释放。在阿托品的存在下,1DMe以浓度依赖性方式增加自发性和电场刺激(EFS)引起的乙酰胆碱释放。纳洛酮还增加了ACh的释放。 1DMe和纳洛酮的刺激作用不是累加的。在没有阿托品的情况下,1DMe不会影响ACh的释放。在1 microM阿托品的存在下,吗啡降低了自发和EFS诱发的ACh释放。 1DMe和纳洛酮抵消了吗啡对EFS诱发的ACh释放的抑制作用。 1DMe和纳洛酮的组合并没有比任何一种单独的药物更具抑制作用。 1DMe对去甲肾上腺素诱导的自发和EFS诱发的ACh释放的抑制作用没有明显的作用。这些结果首先证明了NPFF类似物对神经递质释放的影响:1DMe对豚鼠回肠LMMP制剂中自发和EFS诱导的ACh释放具有刺激作用,可能是通过抵消内源性阿片类药物对ACh释放的抑制作用。

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