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首页> 外文期刊>Life sciences >Characterization of (3H)Met-enkephalin-Arg6-Phe7 binding to multiple sites in rat and guinea pig cerebellum.
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Characterization of (3H)Met-enkephalin-Arg6-Phe7 binding to multiple sites in rat and guinea pig cerebellum.

机译：（3H）Met-脑啡肽-Arg6-Phe7与大鼠和豚鼠小脑多个部位结合的特征。

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[3H]Met-enkephalin-Arg6-Phe7 (MERF) has been shown to label opioid (kappa2 and delta) and sigma2 sites in rat and frog brain membrane preparations, and no specific binding to kappa1 opioid receptors could be established (refs. 6 and 8). In this study the binding was examined in rat cerebellar membranes which are relatively rich in kappa2-sites, and in guinea pig cerebellar preparations where kappa1 opioid receptors are almost exclusively present. In accordance with our previous results, [3H]MERF binding could not be displaced in guinea pig cerebellar membranes neither with U-69,593 nor with naloxone or levorphanol suggesting no interaction with opioid sites, nevertheless a Kd of 2.8 nM was calculated in cold saturation experiments. In rat cerebellar membrane fractions about the half of the specific [3H]MERF binding sites was inhibited by opiate alkaloids such as naloxone, ethylketocyclazocine, or bremazocine. This portion of the heptapeptide binding sites was stereoselective as demonstrated by the difference in the affinities of the enantiomeric compounds levorphanol and dextrorphan, therefore it would represent an opioid site. In both tissues (-)N-allyl-normetazocine (SKF-10,047), which is also considered as sigma2 ligand, displayed the highest affinities. Among opioid peptides beta-endorphin and dynorphin(1-13) showed the highest potencies, displacing [3H]MERF also from its non-opioid sites. It was concluded therefore that [3H]MERF does not bind to kappa1 sites, and besides kappa2-opioid sites substantial binding to peptide preferring non-opioid sites, and/or sigma2 receptors also occurs.
机译：[3H] Met-脑啡肽-Arg6-Phe7（MERF）已显示出可在大鼠和青蛙脑膜制剂中标记阿片样物质（kappa2和δ）和sigma2位点，并且无法建立与kappa1阿片样物质受体的特异性结合（参考文献6）。和8）。在这项研究中，结合是在大鼠小脑膜中进行的，后者相对富含kappa2位点，在豚鼠小脑制剂中几乎仅存在kappa1阿片受体。根据我们之前的结果，[3H] MERF结合不能在豚鼠小脑膜中被U-69,593或与纳洛酮或左啡烷醇取代，表明与阿片样物质位点无相互作用，但是在冷饱和实验中计算得出的Kd为2.8 nM 。在大鼠小脑膜部分中，鸦片生物碱（如纳洛酮，乙基酮基环偶氮星或溴代咪唑胺）抑制特定的[3H] MERF结合位点的一半。七肽结合位点的这一部分是立体选择性的，这由对映体化合物左啡烷和右啡烷的亲和力差异证明，因此它将代表阿片样物质位点。在两个组织中，也被认为是sigma2配体的（-）N-烯丙基-去甲偶氮辛（SKF-10,047）表现出最高的亲和力。在阿片类肽中，β-内啡肽和强啡肽（1-13）表现出最高的效力，也从其非阿片类药物位点取代了[3H] MERF。因此可以得出结论，[3H] MERF不与kappa1位点结合，并且除了kappa2阿片样物质位点以外，还与首选非阿片类药物位点和/或sigma2受体的肽发生了实质性结合。

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