Hyperalgesic effect

Similar to tobacco, lobelia may also have analgesic effects. However, it depends on the mode of administration (Damaj et al. 1997). Intrathecal lobeline produces analgesia on the tail-flick test, but subcutaneous administration is ineffective. On the other hand, subcutaneous lobeline dose-dependently enhances nicotine analgesia. Tolerance develops to this effect of lobeline after 10 days. Lobeline can also produce hyperalgesic effects when administered into the dorsal posterior mesencephalic tegmentum (Hamann and Martin 1994). However, the relevance of this to peripheral administration of lobelia is questionable because chronic injections (IP) of lobeline in rats induced no changes in tail-flick latencies (Sopranzi et al. 1991). 

Carter, R. B., Vanover, K. E., Wilent, W., Xu, Z., Woodward, R. M., Illyin, V. I. Anti-allodynic and anti-hyperalgesic effects of the novel voltage-dependent sodium channel blocker Co102862 in a rat model of peripheral neuropathy, Adv. Ion Channel Res., San Francisco 1999, Abstract book, P-... 

The heptadecapeptide nociceptin has some structural similarity to dynorphin A (YGGFLRRIRPKLKWDNQ Darland et al., 1998), but bears an N-terminal phenylalanine (F) instead of tyrosine (Y) which is essential for the activation of classical opioid receptors ( n, k, 5). It was named nociceptin (NC) by Meunier et al. (1995) to indicate its initially observed hyperalgesic effect and is the endogenous agonist of ORL1. 

Karlsten, R., Gordh, T., Post, C. Local antinociceptive and hyperalgesic effects in in the formalin test after peripheral administration of adenosine analogues in mice, Pharmacol. Toxicol 1992, 70, 434-438. 

The i.t. administration of (+)-TAN-67 induced pain-like nociceptive behaviors, beyond our expectation [36,44]. This observation implies that (+)-TAN-67 counteracted the analgesic effects produced by (-)-TAN-67. Treatment with (-)-TAN-67 actually reduced the hyperalgesic effects induced by (+)-TAN-67. The weak antinociceptive effect of ( )-TAN-67 in spite of its strong agonistic activities in vitro could result from the fact that both (+)- and (-)-TAN-67 have the opposite effects in vivo. It is worth noting that the pain-like behaviors induced by (+)-TAN-67 were not suppressed by morphine... 

Costa, B., Comelli, F., Bettoni, I., Colleoni, M., and Giagoni, G. (2008). The endogenous fatty acid amide, palmitoylethanolamide, has anti-allodynic and anti-hyperalgesic effects in a murine model of neuropathic pain Involvement of CB(1), TRPV1 and PPARgamma receptors and neurotrophic factors. Pain 139, 541-550. 

The search for hyperalgesic effects is more delicate. Standard drugs which cause hyperalgesia are rare and more difficult to demonstrate, frequently requiring particular conditions of administration required, for example topical administration of capsaicin (Yoshimuraetal. 2000). 

Liu EH, Nishiuchi Y, Kimura T, Tachibana S (2006) Supraspinal nodstatin and its amide derivative antagonize the hyperalgesic effects of nodceptin in mice. Neurosci Lett 397 59-63 Liu HX, Hokfelt T (2002) The participation of galanin in pain processing at the spinal level. Trends Pharmacol Sci 23 468-474... 

The action of lobeline (237) as a nicotinic receptor agonist has continued to generate considerable interest. (-)-Lobeline demonstrated a potent hyperalgesic effect, similar to that of nicotine, when tested in the low intensity thermally evoked tail avoidance response assay [514]. It improved cognition and retention in rats comparably to nicotine [515]. Both 237 and nicotine exhibited anxiolytic effects in mice [516] and partially inhibited iV-methyl-D-aspartate-induced responses in rat cortical neurons in vitro [517]. It was a potent inhibitor of nicotine-induced prostration in rats (ED50 = 10 nM) and antagonized additional actions of nicotine including systolic blood pressure increases, seizure, and death [518]. 

Parthenolide (18) Anti-inflammatory and anti-hyperalgesic effects potential cancer drug... 

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