Antinociceptive properties

Itzhak, Y. Kalir, A. Weissman, B.A. and Cohen, S. Receptor binding and antinociceptive properties of phencyclidine opiatelike derivatives. jjj J. Pharmacol 72 305-311, 1981. 

Another significant cannabinoid activity that is mediated by the nervous system arises from the antinociceptive properties of these agents. Compelling evidence suggests that cannabimimetics are effective in the... 

Goncales CEP, Araldi D, Panatieri R B, Rocha J B T, Zeni G and Nogueira C W (2005), Antinociceptive properties of acetylenic thiophene and furan derivatives Evidence for the mechanism of action , Life Sciences, 76, 2221-2234. 

Rouleau, A., Stark, H., Schunack, W. and Schwartz, J. C. Anti-inflammatory and antinociceptive properties of BP 2-94, a histamine H-3-receptor agonist prodrug./. Pharmacol. Exp. Ther. 295 219-225, 2000. 

A. Rouleau, H. Stark, W. Schunack, J. C. Schwartz, Anti-Inflammatory and Antinociceptive Properties of BP 2-94, a Histamine H3-Receptor Agonist Prodrug , J. Pharmacol. Exp. Ther. 2000, 295, 219 -225. 

During the late 1930s some 4-phenylpiperidine derivatives were examined as potential spasmolytics on the basis of their chemical relationship to atropine. The antinociceptive properties of one member, ethyl 1-methyl-4-phenyl-piperidine-4-carboxylate, was detected in screening tests and the compound was subsequently introduced into clinical use by Eisleb and Schaumann in 1939. The compound, well known as pethidine in Europe and meperidine in North America (proprietary names include Demerol, Dolantin, and Dolosal), was soon in widespread use for the relief of pain, and it is remarkable how pethidine, the original non-opioid-derived opioid analgesic, has retained its popularity for many years in the face of competition from other synthetic analgesics introduced since 1939. 

MRZ-2/576 has been demonstrated to cross the blood -brain barrier rapidly and to function centrally as a glycineB antagonist after systemic administration of doses within the relevant antinociceptive dose range. However, the compound is only short-acting within the CNS because of a relatively short half-life within this compartment (Parsons et al., 1997). The compound has antinociceptive properties and shows exceptionally good efficacy in a visceral pain model (McClean et al., 1998 Olivar et al., 1999). 

Syntheses, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2 -Substituted 5-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Epibatidine-analogues, J. Med. Chem. 

Figure 3 Muscarinic agonists with antinociceptive properties.

Adenosine deaminase catalyzes the hydrolytic deamination of adenosine and 2 -deoxyadenosine to inosine and 2 -deoxyinosine respectively. Inhibition of adenosine deaminase leads to an accumulation of its substrates which results in adenosine receptor-mediated effects. Most inhibitors are not reported to have antinociceptive properties, but 2 -deoxycoformycin was proven to have an inhibitory effect on pain transmission (Poon and Sawynok, 1999), and Fujisawa Pharmaceuticals claim adenosine deaminase inhibitors to be active against chronic pain. 

Antinociceptive properties of On the other hand, NO can also be antinociceptive in that... 

Linalool is a natural compound with anti-inflammatory and antinociceptive properties. The antinociceptive action of Iinalool has been reported in several models of inflammatory pain. However, its effects in neuropathic pain have not been investigated. Here, we used the spinal nerve ligation (SNL) model of... 

Unfortunately, in a series such as this, antagonists have not yet been discovered with the potency to match agonists. Diprenorphine is about 100 x nalorphine as a morphine antagonist, and it exhibits no antinociceptive properties in the MW test. 339 However, in the GPI assay, some agonist actions were... 

Extensive structure-biological activity investigations followed the observation that 49 (R = H or OH R = Me) possessed good antinociceptive properties. Resolution of racemic 49 (R = OH R = Me) with L-(+)-tartaric acid indicated that the (-)-isomer was endowed with all the analgesic properties of the racemate (up to 8x morphine in humans). Subsequently, it was introduced into clinical use as levorphanol or Dromoran. Unfortunately, its capacity for causing physical dependence was no less than that of morphine. 

The (—)-morphinans (i.e., those configurationally related to morphine) are responsible for all the antinociceptive properties of the racemate. In addition, such compounds tend to have parallel respiratory depression levels and PDCs. In (+)-series (e.g., dextromethorphan), clinically useful antitussive properties are encountered, again following the separation of biological activities noted in 4,5-epoxymorphinan optical antipodes. 

BoscM G, DesUes M, Reny V, Rips R, Wrigglesworth S (1983) Antinociceptive properties of thyrotropin releasing hormone in mice - comparison with morphine. Br J Pharmacol 79 85-92 Boucher TJ, Okuse K, Bennett DLH, Munson JB, Wood JN, McMahon SB (2(XX)) Potent analgesic effeds of GDNF in neuropathic pain states. Sdence 290 124—127... 

Jiang Q, Seyedmozaffari A, Archer S, Bidlack JM (1992) Antinociceptive properties of 2 alkylating derivatives of morphinone - 14-beta-(thioglycolamido)-7,8-dihydromorphinone (TAMO) and 14-beta-(bromoacetamido)-7,8-dihydromorphinone (H2BAMO). J Pharmacol Exp Ther 262 526-531... 

Imhof, R., Kyburz, E., Daly, J. J. Design, synthesis, and X-ray data of novel potential antipsychotic agents. Substituted 7-phenylquino-lizidines stereospecific, neuroleptic, and antinociceptive properties. J. Med. Chem. 1984, 27, 165-175. 

Pertwee RG, Gibson TM, Stevenson LA, Ross RA, Banner WK, Saha B, Razdan RK, Martin BR (2000) O-1057, apotent water-soluble cannabinoid receptor agonist with antinociceptive properties. Br J Pharmacol 129 1577-1584... 

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