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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Effects of naloxone benzoylhydrazone on native and recombinant nociceptin/orphanin FQ receptors.
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Effects of naloxone benzoylhydrazone on native and recombinant nociceptin/orphanin FQ receptors.

机译：纳洛酮苯甲酰on对天然和重组Nociceptin / Orphanin FQ受体的影响。

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摘要

We have studied the effects of naloxone benzoylhydrazone (NalBzoH) at recombinant human OP4 receptors expressed in Chinese hamster ovary (CHO) cells (CHOhOP4) and native OP4 sites in isolated tissues from various species. In CHOhOP4 membranes, nociceptin (NC) and NalBzoH displaced [125I]Tyr14-NC with pKi values of 10.1 and 7.3. In the presence of 100 microM GDP, NC stimulated GTPgamma35S binding (pEC50 = 8.5). NalBzoH was ineffective but antagonized the effects of NC (pA2 = 6.9). At 5 microM GDP, there was an increase in potency (pEC50 = 9.3) and efficacy (4.3-fold) of NC. NalBzOH was a partial agonist (pEC50 = 7.0, Emax = 13% relative to NC). In CHOhOP4 cells, NC and NalBzoH inhibited cAMP formation with pEC50 and Emax values of 9.8 and 100% and 6.0 and 44%, respectively. In the rat vas deferens, NalBzoH (10 microM) did not modify electrically induced twitches but competitively antagonized the inhibitory action of NC (pA2 = 6.2). In the mouse vas deferens (mVD) and guinea pig ileum (gpI), NalBzoH inhibited twitches with pEC50 and Emax values of 7.6 and 78% and 8.5 and 77%, respectively. The effect of 3 microM NalBzoH was fully inhibited by 3 microM naloxone in mVD and 30 microM in gpI. Under these conditions, NalBzoH antagonized the actions of NC in both preparations with pA2 values of 6.3 and 6.8, respectively. Collectively, these data demonstrate that NalBzoH is a nonselective OP4 ligand with system-dependent behaviour.
机译：我们已经研究了纳洛酮苯甲酰（（NalBzoH）对在中国仓鼠卵巢（CHO）细胞（CHOhOP4）中表达的重组人OP4受体和来自不同物种的分离组织中的天然OP4位点的影响。在CHOhOP4膜中，伤害感受肽（NC）和NalBzoH取代了[125I] Tyr14-NC，pKi值为10.1和7.3。在存在100 microM GDP的情况下，NC刺激了GTPgamma35S结合（pEC50 = 8.5）。 NalBzoH无效，但拮抗NC的作用（pA2 = 6.9）。 GDP为5 microM时，NC的效力（pEC50 = 9.3）和功效（4.3倍）增加。 NalBzOH是部分激动剂（相对于NC，pEC50 = 7.0，Emax = 13％）。在CHOhOP4细胞中，NC和NalBzoH抑制cAMP的形成，pEC50和Emax值分别为9.8、100％，6.0和44％。在大鼠输精管中，NalBzoH（10 microM）不会改变电刺激的抽搐，但竞争性拮抗NC的抑制作用（pA2 = 6.2）。在小鼠输精管（mVD）和豚鼠回肠（gpI）中，NalBzoH抑制抽搐，pEC50和Emax值分别为7.6和78％，8.5和77％。 3 microM NalBzoH的作用被mVD中的3 microM纳洛酮和gpI中的30 microM完全抑制。在这些条件下，NalBzoH分别以6.3和6.8的pA2值拮抗两种制剂中NC的作用。总的来说，这些数据表明NalBzoH是具有系统依赖性行为的非选择性OP4配体。

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