Antinociception supraspinal

Raffa RB, Martinez RP, Connelly CD. G-protein antisense oligodeoxyribonu-cleotides and mu-opioid supraspinal antinociception. Eur J Pharmacol 1994 258 R5-R7. 

Nguyen TT, Matsumoto K, Yamasaki K, Watanabe H. (1997). Involvement of supraspinal GABA receptors in majonoside-R2 suppression of clonidine-induced antinociception in mice. Life Sci. 61(4) 427-36. 

Yeung JC, Rudy TA. (1980). Multiplicative interaction between narcotic agonisms expressed at spinal and supraspinal sites of antinociceptive action as... 

Opioid-induced antinociception depends, to some degree, on monoaminergic signaling in the spinal dorsal horn. While opioids can act directly on dorsal horn terminals of primary afferent nociceptive fibers or on excitatory interneurons in lamina II of the dorsal horn to reduce the release of excitatory transmitters (Glaum et al., 1994), the supraspinally mediated analgesic effects of opioids, at least in part, involve interactions with central and spinal serotonergic and noradrenergic transmission. 

Indeed, using the same experimental approach (i.e. i.c.v. administration of KAtp channel openers and blockers) it was shown that supraspinal KAtp channels are also involved in producing antinociceptive effects of several other classes of analgesic substances (Table 1). The KAtp channels involved in supraspinal antinociception are not... 

The i.c.v. injection of apamin or charybdotoxin, specific blockers of the SK and BK type of Ca2+-activated K+ channels, respectively, prevented the antinociception mediated by tricyclic antidepressants and H1 histamine receptor antagonists whereas 0C2 adrenoceptor-mediated supraspinal analgesia did not depend on the activation of these K+ channels (Table 1). 

Again, as is the case for KAtp channels involved in supraspinal analgesia those participating in spinal antinociception are not tonically activated since none of the Katp channel blockers exerted any effect per se. 

Chizh, B. A., Reifimuller, E., Schlutz, H., Scheede, M., Haase, G., Englberger, W. Supraspinal vs. Spinal sites of the antinociceptive action of the subtype-selective NMDA antagonist ifenprodil, Neuropharmacology 2001, 40, 212-220. 

Zurek, J. R., Nadeson, R., and Goodchild, C. S. (2001). Spinal and supraspinal components of opioid antinociception in streptozotocin induced diabetic neuropathy in rats. Pain 90, 57-63. 

Supraspinal DPDPE/ [D-Ala2]-delt II ai3, ai2 Antinociception Antisera 58,59... 

There is considerable evidence that 5r and 2-opioid receptors act at supraspinal sites to modulate nociceptive responses. Direct ICV injection of the putative 5-opioid agonists DPDPE or DPLPE in the mouse produced dose-dependent antinociception that was blocked by ICI 174,864 but not by (5-FNA [87,88]. Furthermore, 5-opioid selective doses of DPDPE given ICV blocked nociception, but not gastrointestinal transit, in mice [99].The ICV administration of DPDPE has been shown to produce dose-dependent antinociception against mechanical nociception (Randall-Selitto paw with-... 

In contrast, direct microinjection into brain parenchyma provided evidence of 6-opioid-mediated antinociception arising from supraspinal sites. In an early study aimed at determining the relative contribution of opioid subtypes to antinociception arising from different brain regions, morphine, DADLE, and ethylketocyclazocine (EKC) were microinjected directly into the PAG, NGC, and the NRM in the rat [109]. It was found that DADLE was more potent than morphine by 1 order of magnitude in the PAG and NRM, and less potent in the NGC [109], Furthermore, the potency of DADLE among these sites was consistent [109], In contrast, EKC was weakly active... 

The fact that 6-opioid receptors act at spinal and supraspinal sites increases the possibility that, like morphine, 6-opioid agonists may exhibit a synergistic interaction between the spinal and supraspinal sites of action. It has been clearly established that the concurrent administration of ICV and ITH morphine results in a multiplicative antinociceptive interaction [130,131]. It is this supraspinal/spinal multiplicative nature of morphine and its clinical analgesic utility at tolerable doses. Early studies with mice indicated only... 

SUPRASPINAL ANTINOCICEPTION MEDIATED BY DELTA OPIOID RECEPTOR AGONIST AND INTERACTION BETWEEN MU AND DELTA OPIOID RECEPTORS IN THE BRAIN... 

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