- 作者: Lih-Chu Chiou
- 作者服務機構: Department of Pharmacology, College of Medicine, Natonal Taiwan University, Taipei, Taiwan
- 中文摘要: --
- 英文摘要: A novel opioid receptor-like orphan receptor (ORL1) wascloned and identified to be homologous to classicalopioid receptors but insensitive to traditional opioids. Aheptadecapeptide, termed orphanin FQ or nociceptin(OFQ/N), was identified as its endogenous ligand. OFQ/Nshares overlapping distribution sites in pain-processingareas and common cellular mechanisms with opioidsbut exerts diverse effects on nociceptive responses. Ofthe two reported ORL1 antagonists,[PheΨ(CH -NH)-Gly] nociceptin-(1-13)-NH(PheΨ) and naloxone ben-zoylhydrazone (NBZ), antagonisms were validated in theactivation of inward rectifying K channels induced byOFQ/N, using the patch clamp technique in ventrolateralperiaqueductal gray slices. Results showed that PheΨacted as a partial agonist and NBZ was a weak nonselec-tive antagonist of ORL1. It is comparable with most butnot all of the findings from other tissues. Comparing allthe reports supports the above inference for these twoantagonists. The possible causes for the discrepancywere discussed. A brief review on the putative ORL1antagonists, acetyl-RYYRIK-NH2, some σ-ligands andthe functional antagonist, nocistatin, is also included. Itindicates that a potent and selective ORL1 antagonist isexpecting to elucidate the physiological role of OFQ/N.
- 中文關鍵字: --
- 英文關鍵字: --