Chu X, Xu N, Li P, Wang J Q
Department of Physiology, Shanghai Medical University, Shanghai, People's Republic of China.
Neuroreport. 1998 Apr 20;9(6):1081-4. doi: 10.1097/00001756-199804200-00022.
Nociceptin (orphanin FQ), the newly discovered endogenous ligand for the opioid receptor like-1 receptor, profoundly inhibited spontaneous discharges of neurons in the rostral ventrolateral medulla (RVLM) in rat brain slices. This inhibition was concentration-dependent (0.3, 1, 3 and 10 nM) and insensitive to pharmacological blockade of traditional opioid receptors by naloxone. Moreover, nociceptin injected into the RVLM (10 nM, 0.1 microliter) in anesthetized rats decreased arterial blood pressure and heart rate by 31% and 15%, respectively. The data obtained in vitro and in vivo suggest that nociceptin has powerful effects on the RVLM neurons involving central control of cardiovascular activity. The negative regulation of cardiovascular activity by nociceptin is not mediated through typical naloxone-sensitive opioid receptors.
孤啡肽（痛敏肽FQ）是新发现的阿片受体样-1受体的内源性配体，它能显著抑制大鼠脑片延髓头端腹外侧区（RVLM）神经元的自发放电。这种抑制作用呈浓度依赖性（0.3、1、3和10 nM），且对纳洛酮对传统阿片受体的药理阻断不敏感。此外，向麻醉大鼠的RVLM注射孤啡肽（10 nM，0.1微升）可使动脉血压和心率分别降低31%和15%。体外和体内实验获得的数据表明，孤啡肽对RVLM神经元具有强大作用，涉及心血管活动的中枢控制。孤啡肽对心血管活动的负性调节不是通过典型的对纳洛酮敏感的阿片受体介导的。
