Antinociceptive effects

French ED, Dillon K, Wu X Cannabinoids excite dopamine neurons in the ventral tegmentum and substantia nigra. Neuroreport 8 649—632, 1997 Fujinaga M, Maze M Neurobiology of nitrous oxide-induced antinociceptive effects. Mol Neurobiol 25 167-189, 2002... 

Schaddelee MP, Collins SD, DeJongh J, de Boer AG, Ijzerman AP, Danhof M. Pharmacokinetic/pharmacodynamic modelling of the anti-hyperalgesic and antinociceptive effect of adenosine A1 receptor partial agonists in neuropathic pain. Eur J Pharmacol 2005 May 9 514(2-3) 131-40. 

In further support of a pro-nociceptive role of CX3CL1 are data showing that the direct injection of CX3CL1 in the periaqueductal grey, a brain region mostly involved with analgesic responses, albeit un-effective by itself, results in inhibition of the antinociceptive effects induced by p, 5, and k opioid agonists (Chen et al. 2(X)7). 

Chen X, Geller EB, Rogers TJ, Adler MW (2007) The chemokine CX3CLl/fractaUdne interferes with the antinociceptive effect induced by opioid agonists in the periaqueductal grey of rats. Brain Res 1153 52-57... 

Kamei J, Saitoh A, Ohsawa M, Suzuki T, Misawa M, Nagase H, Kasuya Y. Antinociceptive effects of the selective non-peptidic delta-opioid receptor agonist TAN-67 in diabetic mice. Eur J Pharmacol 1995 276 131-135. 

Jiirgensen S, Dalbo S, Angers P, Santos AR, Ribeiro-do-Valle RM. Involvement of 5-HT2 receptors in the antinociceptive effect of Uncaria tomentosa. Pharmacol Biochem Behav 2005 81 466-477. 

Ugarte, S. D., Homanics, G. E Firestone, L. L and Hammond, D. L. (2000) Sensory thresholds and the antinociceptive effects of GABA receptor agonists in mice lacking the P3 subunit of the GABAa receptor. Neuroscience 95,795-806. 

Yaksh, T. L. (1979) Direct evidence that spinal serotonin and noradrenaline terminals mediate the spinal antinociceptive effects of morphine in the central periaqueductal gray. Brain Res.. 160 180-185. 

Costa LG, Murphy SD. 1986. Cholinergic and opiate involvement in the antinociceptive effect of diisopropylfluorophosphate. Pharmacol Biochem Behav 24 733-736. 

Findings continue to accumulate in the field of endogenous opiates, as exemplified by two tetrapeptides isolated from mammalian brain and found to have high affinity and selectivity for p-opioid receptors. These tetrapeptides are endomorphin-1 (Tyr-Pro-Trp-Phe-NH2) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH2). A number of synthetic analogues have been prepared with the view to improve their metabolic stability and, in some cases, to limit their access to peripheral opioid receptors. The three synthetic endomor-phin analogues Tyr-D-Ala-Phe-Phe-NH2 (6.84), Tyr-D-Arg-Phe-Phe-NH2 (6.85), and Tyr-D-Arg-Phe-Ape-NH2 (6.86), to be discussed in the next section, have potent antinociceptive effects in in vivo inflammatory tests but exhibit modest effects in the CNS. However, and despite the presence of a D-amino acid and a protected C-terminus, they remained sensitive to enzymatic hydrolysis [211][212],... 

Alhaider AA. (1991). Antinociceptive effect of ketanserin in mice invoivement of supraspinai 5-HT2 receptors in nociceptive transmission. Brain Res. 543(2) 335-40. 

Ferri S, Cavicchini E, Romualdi P, Speroni E, Murari G. (1986). Possible mediation of catecholaminergic pathways in the antinociceptive effect of an extract of Cannabis sativa L. Psychopharmacology (Berlin). 89(2) 244-47. 

Pugh G Jr, Abood ME, Welch SP. (1995). Antisense oligodeoxynucleotides to the kappa-1 receptor block the antinociceptive effects of delta 9-THC in the spinal cord. Brain Res. 689(1) 157-58. 

Welch SP, Huffman JW, Lowe J. (1998). Differential blockade of the antinociceptive effects of centrally administered cannabinoids by SR141716A. J Pharmacoi Exp Ther. 286(3) 1301-8. 

In contrast, some animal studies have suggested that female rats have an increased sensitivity to nicotine althongh these have assessed acnte antinociceptive effects and decreases in motor activity (e.g. Cronan et al. 1985 Craft and Milholland 1998) or chronic increases in locomotion (Kanyt et al. 1999). However, female mice of three strains were reported to be less sensitive than males to motor depressant effects of nicotine (Hatchell and Collins 1977). Gonadal hormones have been suggested to play a part in stimulus control as responses to nicotine during ethanol withdrawal were lower in intact females compared with ovariectomised females and males (Jung et al. 2000). 

Neuroanatomically both the locus coeruleus and the raphe nuclei project to the spinal cord where they gate sensory pathways from the skeletomuscular areas. As there is evidence that both noradrenaline and 5-HT are dysfunctional in depression, it is perhaps not surprising to find that the pain threshold is often reduced in patients with depression. Conversely, different types of antidepressants have been shown to have an antinociceptive effect in both rodent models of neuropathic pain, and clinically in fibromyalgia, chronic fatigue syndrome, postherpetic neuralgia and diabetic neuropathy. In general, it would appear that the dual action antidepressants (such as the TCAs and SNRIs) are more effective than the SSRIs. 

Wilcox GL, Carlsson KH, Jochim A, Jurna 1 (1987) Mutual potentiation of antinociceptive effects of morphine and clonidine in rat spinal cord. Brain Res 405 84-93... 

The uncompetitive NMDA receptor antagonist ketamine has been available for clinical use as an anaesthetic for 40 years (Domino et al. 1965). Ketamine is effective in various animal models of hyperalgesia and allodynia and has been reported to have antinociceptive effects in some of these models at doses devoid of obvious side-effects. Others, however, have reported that the effects of ketamine are only seen at doses producing ataxia (see Parsons 2001 for review). Ketamine reportedly inhibits the area of secondary hyperalgesia induced by chemical (Park et al. 1995) or thermal stimuli (Ilkjaer et al. 1996 Warncke et al. 1997) and inhibits temporal siunmation of repeated mechanical (Warncke et al. 1997) and electrical stimuli (Arendtnielsen et al. 1995 Andersen et al. 

Fisher K, Lefebvre C, Coderre TJ (2002) Antinociceptive effects following intrathecal pretreatment with selective metabotropic glutamate receptor compounds in a rat model of neuropathic pain. Pharmacol Biochem Behav 73 411-418 Flajolet M, RakhUin S, Wang H, et al (2003) Protein phosphatase 2C binds selectively to and dephosphorylates metabotropic glutamate receptor 3. Proc Natl Acad Sci USA 100 16006-16011... 

A.B. Malmberg, M.F. Rafferty, T.L. Yaksh, Antinociceptive effect of spinally delivered prostaglandin E receptor antagonists in the formalin test on the rat, Neurosci. Lett. 173 (1994) 193. 

Z0199 Kuraishi, Y., T. Nanayama, T. Yamaguchi, T. Hotani, and M. Satoh. Antinociceptive effects of Oriental medicine kei-kyoh-zoh-soh-oh-shin-bu-toh in mice and rats. J PharmacobioDyn 1990 13(1) 49-56. 

The leaves of Aleurites moluccana contain 2"-C-rhamnosylswertisin and swertisin. The antinociceptive effect of both compounds was evaluated by the writhing test in mice. " The results indicated that the first derivative inhibits, dose dependently, the abdominal constrictions caused by acetic acid with an ID50 value of 6.9 to 10.2 pM/kg and maximal inhibition of 92%. When compared with aspirin ID5o= 133 pM/kg, the C-glycosylflavone was about 16-fold more potent. On the other hand, the swertisin alone did not show any effect. 

Meloxicam shows central antinociceptive effects in rats which seem to be independent of the COX-inhibitory activity (Lopez-Garcia and Laird, 1998). 

Courade, J. P., Chassaing, C., Bardin, L., Alloui, A., Eschalier, A. 5-HT receptor subtypes involved in the spinal antinociceptive effect of acetaminophen in rats, Eur. J. Pharmacol. 2001, 432, 1-7. 

Lopez-Garcia, J. A. and Laird, J. M. Central antinociceptive effects of meloxicam on rat spinal cord in vitro, Neuroreport 1998, 9, 647-651. 

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