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首页> 外文期刊>Life sciences >Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: research tools and potential therapeutic agents.
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Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: research tools and potential therapeutic agents.

机译：Nociceptin / orphanin FQ受体ORL1的肽和非肽配体：研究工具和潜在的治疗剂。

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The 17-amino acid neuropeptide nociceptin/Orphanin FQ (N/OFQ) was recently identified as the endogenous ligand for the opioid receptor-like (ORL1) receptor, a fourth member of the classical mu, delta, and kappa opioid receptor family. Although ORL1 clearly belongs to the opioid receptor family, it does not bind classical opiates and the ORL1-N/OFQ system has pharmacological actions distinct from the opioid receptor system. This new ligand-receptor system has generated active interest in the opioid community because of its wide distribution and involvement in a myriad of neurological pathways. The past two years have witnessed tremendous advances in the design and discovery of very potent and selective peptide and nonpeptide agonist and antagonist ligands at ORL1. These discoveries have facilitated the understanding of the role of the ORL1-N/OFQ system in a variety of processes such as pain modulation, anxiety, food intake, learning, memory, neurotransmitter release, reward pathways, and tolerance development. The ORL1 receptor therefore represents a new molecular target for the design of novel agents for anxiety, analgesia, and drug addiction. Indeed, there is tremendous interest in the pharmaceutical industry in the development of nonpeptide ligands such as the potent ORL1 agonist, Ro 64-6198, as anxiolytics and the ORL1 antagonist JTC-801 as novel analgesics. This review presents an overview of the various peptide and nonpeptide ORL1 ligands with an emphasis on their potential therapeutic utility in various human disorders.
机译：最近鉴定出17个氨基酸的神经肽痛觉敏/孤儿蛋白FQ（N / OFQ）是类阿片受体样（ORL1）受体的内源性配体，是经典mu，delta和kappa类阿片受体家族的第四个成员。尽管ORL1显然属于阿片受体家族，但它不结合经典鸦片制剂，并且ORL1-N / OFQ系统具有不同于阿片受体系统的药理作用。这种新的配体-受体系统因其广泛分布和参与无数的神经通路而引起了对阿片样物质社区的积极关注。在过去的两年中，在ORL1上非常有效和选择性的肽和非肽激动剂和拮抗剂配体的设计和发现方面取得了巨大进步。这些发现促进了对ORL1-N / OFQ系统在各种过程中的作用的理解，例如疼痛调节，焦虑，食物摄入，学习，记忆，神经递质释放，奖励途径和耐受性发展。因此，ORL1受体代表了用于设计焦虑，镇痛和药物成瘾的新型药物的新分子靶标。确实，制药行业对非肽配体的开发非常感兴趣，例如有效的抗焦虑药ORL1激动剂Ro 64-6198和新型镇痛药ORL1拮抗剂JTC-801。这篇综述对各种肽和非肽ORL1配体进行了概述，重点是它们在各种人类疾病中的潜在治疗作用。

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