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Chemical Compound Review

CHEMBL92501     N,N-dimethyl-2-[(2- methylpyrazol-3-yl)...

Synonyms: SureCN290138, AC1L30XJ
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Disease relevance of Cizolirtine

  • Under acute conditions, cizolirtine (30 and 80 mg/kgi.p.) significantly increased paw withdrawal and vocalization thresholds in the paw pressure test in diabetic rats displaying mechanical hyperalgesia [1].
  • These results suggest that cizolirtine may be useful for alleviating some neuropathic somatosensory disorders, in particular cold allodynia, with a reduced risk of undesirable side effects [2].
  • Evidence for adenosine- and serotonin-mediated antihyperalgesic effects of cizolirtine in rats suffering from diabetic neuropathy [3].
  • CONCLUSIONS: Although this limited pilot study did not include an internal measure of sensitivity, relevant pain reduction was shown in the population of patients with suspected renal colic undergoing treatment with cizolirtine, suggesting the presence of analgesic activity [4].

High impact information on Cizolirtine

  • In this study, we investigated the efficacy of a novel non opioid analgesic, cizolirtine, to reduce mechanical hyperalgesia associated with streptozotocin (STZ)-induced diabetes, in the rat [1].
  • Cizolirtine significantly reduced the K(+)-evoked overflow of both the SP-like material (SPLM; -25% at 0.1 microM--0.1 mM) and CGRPLM (-20% at 0.1--1.0 microM) from slices of the dorsal half of the lumbar enlargement of the spinal cord [5].
  • Cizolirtine may be effective in primary allodynia after peripheral nerve injury, and a further trial in a larger number of such subjects is warranted [6].
  • Recent studies have shown that the analgesic effect of cizolirtine could be related, at least partially, to an inhibition of spinal substance P release [7].

Analytical, diagnostic and therapeutic context of Cizolirtine

  • These effects were antagonized by prior injection of the alpha(2)-adrenoceptor antagonist idazoxan (0.5 mg/kg i.v.), but not the opioid receptor antagonist naloxone (0.1 mg/kg i.v.). On the other hand, cizolirtine (10 mg/kg p.o.) produced no motor deficits in animals using the rotarod test [2].
  • Intrathecal perfusion in halothane-anaesthetized rats showed that local application of cizolirtine markedly diminished the spinal outflow of SPLM (up to -50% at 0.1 mM) but only marginally that of CGRPLM [5].
  • Simultaneous separation of the enantiomers of cizolirtine and its degradation products by capillary electrophoresis [8].
  • Cizolirtine was tested in a double-blind, placebo-controlled, two-way crossover study, having previously been shown to have significant analgesic and anti-hyperalgesic action in neuropathic pain models and preliminary human studies [6].
  • Cizolirtine does not produce gastrointestinal lesions or depress respiration [388894], however, it does exhibit antipyretic activity in animal models [260611], [388894] [9].


  1. Antihyperalgesic effects of cizolirtine in diabetic rats: behavioral and biochemical studies. Aubel, B., Kayser, V., Mauborgne, A., Farré, A., Hamon, M., Bourgoin, S. Pain (2004) [Pubmed]
  2. Effects of the novel analgesic, cizolirtine, in a rat model of neuropathic pain. Kayser, V., Farré, A., Hamon, M., Bourgoin, S. Pain (2003) [Pubmed]
  3. Evidence for adenosine- and serotonin-mediated antihyperalgesic effects of cizolirtine in rats suffering from diabetic neuropathy. Aubel, B., Kayser, V., Farré, A., Hamon, M., Bourgoin, S. Neuropharmacology (2007) [Pubmed]
  4. Comparison of cizolirtine citrate and metamizol sodium in the treatment of adult acute renal colic: a randomized, double-blind, clinical pilot study. Pavlik, I., Suchy, J., Pacík, D., Bokr, R., Sust, M., Villoria, J., Abadías, M. Clinical therapeutics. (2004) [Pubmed]
  5. The novel analgesic, cizolirtine, inhibits the spinal release of substance P and CGRP in rats. Ballet, S., Aubel, B., Mauborgne, A., Poliénor, H., Farré, A., Cesselin, F., Hamon, M., Bourgoin, A.S. Neuropharmacology (2001) [Pubmed]
  6. Cizolirtine citrate (E-4018) in the treatment of chronic neuropathic pain. Shembalkar, P., Täubel, J., Abadias, M., Arezina, R., Hammond, K., Anand, P. Current medical research and opinion. (2001) [Pubmed]
  7. Pharmacology of cizolirtine: a new analgesic agent. Alvarez, I., Andreu, F., Buxens, J., Colombo, M., Dordal, A., Fort, M., Gutiérrez, B., Farré, A.J. Methods and findings in experimental and clinical pharmacology. (2000) [Pubmed]
  8. Simultaneous separation of the enantiomers of cizolirtine and its degradation products by capillary electrophoresis. Gómez-Gomar, A., Ortega, E., Calvet, C., Mercé, R., Frigola, J. Journal of chromatography. A. (2002) [Pubmed]
  9. Cizolirtine. Laboratorios Dr Esteve. Monck, N. Current opinion in investigational drugs (London, England : 2000) (2001) [Pubmed]
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