Nicol B, Lambert D G, Rowbotham D J, Smart D, McKnight A T
University Department of Anaesthesia, Leicester Royal Infirmary.
Br J Pharmacol. 1996 Nov;119(6):1081-3. doi: 10.1111/j.1476-5381.1996.tb16007.x.
Nociceptin, an endogenous ligand for the orphan receptor ORL1, has recently been described. In this study we have shown that nociception inhibits 46 mM K(+)-stimulated glutamate release from rat perfused cerebrocortical slices with an IC50 of 51 nM. At 100 nM the inhibition amounted to 68 +/- 14% and was naloxone (10 microM)-insensitive excluding an activation of mu, delta and kappa opioid receptors. These data demonstrate the functional coupling of ORL1 in glutamatergic neurones and implicates a role for nociceptin in glutamatergic neurotransmission.
痛敏肽，一种孤儿受体ORL1的内源性配体，最近已被描述。在本研究中，我们已表明痛觉抑制作用可抑制46 mM K⁺刺激大鼠灌注大脑皮质切片中谷氨酸的释放，其半数抑制浓度（IC50）为51 nM。在100 nM时，抑制率达68±14%，且对纳洛酮（10 μM）不敏感，排除了μ、δ和κ阿片受体的激活。这些数据证明了ORL1在谷氨酸能神经元中的功能偶联，并表明痛敏肽在谷氨酸能神经传递中发挥作用。
