Antinociceptive activity

Welch SP, Stevens DL. (1992). Antinociceptive activity of intrathecally administered cannabinoids alone, and in combination with morphine, in mice. J Pharmacoi Exp Ther. 262(1) 10-18. 

Martin BR. (1985). Structural requirements for cannabinoid-induced antinociceptive activity in mice. Life Sci. 36(16) 1523-30. 

Taniguchi K, Shinjo K, Mizutani M, et al (1997) Antinociceptive activity of CP-101,606, an NMDA receptor NR2B subunit antagonist. Br J Pharmacol 122 809-812 Tempia F, Alojado ME, Strata P, KnOpfel T (2001) Characterization of the mGlnR(l)-mediated electrical and calcium signaling in Purkinje cells of mouse cerebellar slices. J Neurophysiol 86 1389-1397... 

C-Glycosylflavonoids and General Animal Physiology 14.6.6.1 Antinociceptive Activity... 

There is evidence that in cerebral ischaemia adenosine may have protective effects, since it inhibits the release of many excitatory neurotransmitters, such as glutamate, and it also stabilises the membrane potential. Unfortunately, adenosine has an extremely short half-life, but recently nucleoside (adenosine) transport inhibitors, e.g. draflazine, have been developed that prevent the endothelial uptake and breakdown of adenosine and prolong its beneficial effects. Nucleoside transport inhibitors also have myocardial protective properties and may have a role in organ preservation prior to transplantation. Adenosine also has an antinociceptive function and various adenosine analogues have antinociceptive activity, which correlates with their affinity for the A1 receptors (Lipkowski and co-workers 1996). 

Welch, S. P. and Dunlow, L. D. Antinociceptive activity of intrathecally administered potassium channel openers and opioid agonists a common mechanism of action , The Journal of Pharmacology and Experimental Therapeutics 1993, 267, 390-399. 

Table 1 Antinociceptive activity of L-type Ca2+ channel antagonists in specified pharmacological assays.

Concerning the -conopeptides, SNX-111 (Ziconotide) seems to be one of the proteins with the highest intrinsic antinociceptive activity in the formalin test (Table 4, Malmberg and Yaksh, 1994). This may be the main reason why most of the papers cited deal with this special synthetic peptide. 

Table 4 Antinociceptive activity of N-, P- and/or Q-type VDCC inhibitors in rats.

Coderre, T. J. and Van Empel, I. The utility of excitatory amino acid (EAA) antagonists as analgesic agents. Comparison of the antinociceptive activity of various classes of EAA antagonists in mechanical, thermal and chemical nociceptive tests, Pain 1994, 59, 345-352. 

Antinociceptive activity of CP-101,606, an NMDA receptor NR2B subunit antagonist, Brit. J. Pharmacol. 1997, 122, 809-812. 

Epibatidine was shown to be a very potent and selective agonistic ligand of nicotinic acetylcholine receptors. This natural product is effective in various animal models of pain through a pronounced nAChR agonistic mechanism (Ki <100 pm) which is accompanied by severe and nACh-related side-effects (Corey et al. 1993 Rupniak et al., 1994 Boyce et al., 2000). A clear differentiation between antinociceptive activity in animal models of pain and toxic side-effects cannot be determined. Nevertheless there is some activity directed towards the development of epibatidine as an analgesic (Bai et al., 1997). 

Calignano, A., La Rana, G., Piomelli, D. Antinociceptive activity of the endogenous fatty acid amide, palmitylethanolamide, Eur. J. Pharmacol. 2001, 419,191-198. 

At present, BP 2.94 (36) is under clinical development in Phase II trials for the treatment of asthma, pneumoallergic diseases, and others. Preclinical studies in rodents clearly displayed anti-inflammatory as well as antinociceptive activity of BP 2.94 (36) given orally at low doses. These effects are mediated by inhibitory H3 receptors located on sensory C-fibres in several different tissues. In particular, capsaicin-induced plasma protein extravasation was dose-dependently inhibited in airways, digestive tract, skin, conjunctiva, urinaiy bladder, nasal mucosa, and dura mater of the rat. In the p-phenylbenzoquinone-induced writhing test in mice, BP 2.94 (36) had a pronounced antinociceptive activity similar to that of acetylsalicylic acid. This effect was significantly abolished by the H3 receptor antagonist thioperamide but not by naloxone. Furthermore, BP 2.94 (36) reduced zymosan-induced edema. This antiinflammatory effect was also abolished by thioperamide [6]. 

Aoki KR (2003) Evidence for antinociceptive activity of botulinum toxin type A in pain management. Headache 43 Suppl 1 S9-15... 

Peana, A. T., Marzocco, S., Popolo, A., and Pinto, A. (2006a). (—)-Linalool inhibits in vitro NO formation Probable involvement in the antinociceptive activity of this monoterpene compound. 

Sakurada, T., Katsumata, K., Yogo, H., Tan-No, K., Sakurada, S., Ohba, M., and Kisara, K. (1995). The neurokinin-1 receptor antagonist, sendide, exhibits antinociceptive activity in the formalin... 

Five lignans isolated from the heartwood of T. baccata L. growing in Turkey were evaluated for their anti-inflammatory and antinociceptive activities in vivo. All of the compounds were shown to possess significant antinociceptive activities against p-bcnzoquinone-induccd abdominal contractions and significantly inhibited carrageenan-induced hind paw edema in mice [100]. 

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