Sakurada T, Tan-No K, Yamada T, Sakurada S, Kisara K, Ohba M, Terenius L
Department of Pharmacology, Tohoku College of Pharmacy, Sendai, Japan.
Life Sci. 1990;47(20):PL109-13. doi: 10.1016/0024-3205(90)90291-x.
N-terminal fragments of substance P (SP) were tested for antagonism against the aversive responses induced in mice by various tachykinin receptor agonists, somatostatin and bombesin. When co-administered with SP intrathecally, low doses (1.0-4.0 pmol) of SP (1-7) or SP (1-8) reduced the SP-induced behavioural responses of scratching, biting and licking. Aversive responses induced by two other neurokinin (NK) 1 receptor agonists, Septide and physalaemin, were also dose-dependently decreased by the simultaneous injection of small doses of SP (1-7) or SP (1-8). Aversive responses induced by 400 pmol of NK A were also significantly reduced by co-administration of SP (1-7) or SP (1-8). No significant effects of the N-terminal fragments were observed against the aversive responses elicited by NK A (300 pmol), eledoisin, NK B, somatostatin or bombesin. These results suggest that the behavioural antagonism produced by SP (1-7) and SP (1-8) may be limited to the NK 1 receptor at the spinal level in mice.
对P物质（SP）的N端片段进行了测试，以检测其对各种速激肽受体激动剂、生长抑素和蛙皮素在小鼠中诱导的厌恶反应的拮抗作用。当与SP鞘内共同给药时，低剂量（1.0 - 4.0 pmol）的SP（1 - 7）或SP（1 - 8）可降低SP诱导的抓挠、咬和舔等行为反应。另外两种神经激肽（NK）1受体激动剂Septide和 Physalaemin诱导的厌恶反应，也会因同时注射小剂量的SP（1 - 7）或SP（1 - 8）而呈剂量依赖性降低。共同给予SP（1 - 7）或SP（1 - 8）时，400 pmol的NK A诱导的厌恶反应也显著降低。未观察到N端片段对NK A（300 pmol）、eledoisin、NK B、生长抑素或蛙皮素引起的厌恶反应有显著影响。这些结果表明，SP（1 - 7）和SP（1 - 8）产生的行为拮抗作用可能仅限于小鼠脊髓水平的NK 1受体。
