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Aim: To study the analgesic effect of endomorphin-1 (EM-1)., Methods: The experiment was performed in rats and mice to study the analgesic effect of intraperitoneal (ip) injection of EM-1 with tail stimulation-vocalization test, writhing test, adjuvant arthritis, and neuropathic pain model and to compare it with the analgesic effects produced by intracerebroventricular (icv) and intrathecal (it) administrations., Results: 1) EM-1 raised the pain threshold dose-dependently in tail stimulation-vocalization test in rats and inhibited the writhing responses induced by ip acetic acid in mice. EM-1 also decreased the hyperalgesia in both adjuvant arthritis and neuropathic pain model. 2) The analgesic effect induced by central (icv and it) administration of EM-1 was faster and more powerful than that induced by peripheral (ip) administration. 3) The analgesic effect of EM-1 was reversed by naloxone (opioid receptor antagonist), as well as by cyprodime (mu-opioid receptor selective antagonist). Repeated administrations of EM-1 induced tolerance., Conclusion: EM-1 had a definite analgesic effect and the analgesic effect of EM-1 was mediated by central mu-opioid receptor.

The effects of hypothalamic arcuate nucleus (ARC) or anterior lobe of pituitary (AL) stimulation on the nociceptive responses of thalamic parafascicular (Pf) neurons were studied in rats with electrophysiological technique. The results showed that ARC stimulation could inhibit the nociceptive discharges of Pf neurons, namely, the immediate inhibition because of its very short latency and duration. AL stimulation could also inhibit the nociceptive discharges of Pf neurons, but this inhibition was a delayed one because of its longer latency and duration. Hypophysectomy diminished the immediate inhibition due to ARC stimulation, while ARC lesion diminished the delayed inhibition due to AL stimulation. Both kinds of inhibition were blocked by dexamethasone pretreatment. The above results suggest that neuroendocrine relationship between ARC and AL is involved in pain modulation.

Previous studies have demonstrated that locus coeruleus (LC)-noradrenergic neuronal system plays an important role in pain modulation and electroacupuncture (EA) analgesia. In the present experiment, the effect of LC stimulation and EA on nociceptive response of spinal dorsal horn neurons was investigated. The main results were: 1) LC stimulation and electroacupuncture produced a significant inhibitory effect on nociceptive response of dorsal horn neurons; 2) The inhibitory effect of LC stimulation was not affected by the lesion of nucleus raphe magnus or by the injection of naloxone; 3) These inhibitory effects of LC stimulation and electroacupuncture could be enhanced by alpha 2-agonist clonidine, and decreased slightly by alpha-antagonist phentolamine. These results suggest that the inhibitory effect of LC stimulation and electroacupuncture on the nociceptive response of dorsal horn neurons might be mediated by alpha 2-receptors.