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  • Title: Intrathecal [Nphe1]nociceptin( 1-13)NH2 selectively reduces the spinal inhibitory effect of nociceptin.
    Author: Xu IS, Grass S, Calo G, Guerrini R, Wiesenfeld-Hallin Z, Xu XJ.
    Journal: Life Sci; 2002 Jan 25; 70(10):1151-7. PubMed ID: 11848299.
    Abstract:
    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.
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