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Intrathecal (Nphe1)nociceptin( 1-13)NH2 selectively reduces the spinal inhibitory effect of nociceptin.

机译:鞘内(Nphe1)nociceptin(1-13)NH2选择性降低Nociceptin的脊髓抑制作用。

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摘要

The effects of intrathecal (i.t.) application of the proposed nociceptin receptor antagonist [Nphe1]nociceptin(1-13)NH2 on the flexor reflex was evaluated in spinalized rats. I.t. [Nphe1]nociceptin (1-13)NH2 dose-dependently facilitated the flexor reflex with no depression. Pretreatment with 16.5 nmol of [Nphe1]nociceptin(1-13)NH2 prevented the development of reflex depression following 0.55 nmol i.t. nociceptin, but strongly enhance the initial excitatory effect of nociceptin. The reflex depressive effect of i.t. endomorphine-2 was not blocked by [Nphe1]nociceptin(1-13)NH2 pretreatment. It is concluded that [Nphe1]nociceptin(1-13)NH2 is a selective antagonist of the spinal receptor mediating the inhibitory action of nociceptin. It can be further suggested that the spinal inhibitory effect of nociceptin may be tonically active.
机译:在脊髓大鼠中评估鞘内(i.t.)拟议的伤害感受器受体拮抗剂[Nphe1] nociceptin(1-13)NH2对屈肌反射的影响。它。 [Nphe1] nociceptin(1-13)NH2剂量依赖性地促进屈肌反射而无抑郁。用16.5 nmol的[Nphe1] nociceptin(1-13)NH2预处理可防止在0.55 nmol i.t后出现反射抑制。伤害感受器,但强烈增强伤害感受器的初始兴奋作用。 i.t.的反射抑制作用[Nphe1] nociceptin(1-13)NH2预处理未阻断endomorphine-2。结论是[Nphe1] nociceptin(1-13)NH2是介导Nociceptin抑制作用的脊髓受体的选择性拮抗剂。可以进一步暗示,伤害感受肽的脊柱抑制作用可能是强直性的。

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