Mirtazapine and its enantiomers differentially modulate acute thermal nociception in rats

Brain Research Bulletin
Rainer FreynhagenUta Muth-Selbach

Abstract

The antidepressant mirtazapine is an optically active drug and currently marketed as a racemic compound consisting of its S(+) and R(-)-enantiomers in a 50:50 mixture. As stereochemistry of antidepressants has become increasingly important to consider for the relevance of their analgesic properties, we investigated the effect of (+/-)-mirtazapine and its enantiomers in an animal model of acute thermal nociception. Wistar rats were injected intrathecal with either (+/-)-mirtazapine, R(-)-mirtazapine, S(+)-mirtazapine from 1 to 0.001 mg/kg and vehicle (0.9% NaCl), respectively. The effects on thermal paw withdrawal thresholds were monitored using the Hargreaves test. (+/-)-Mirtazapine exerted pro- and antinociceptive effects in acute thermal nociception, whereas R(-)-mirtazapine showed solely antinociceptive and S(+)-mirtazapine pronociceptive properties. These results clearly demonstrate a differential effect of (+/-)-mirtazapine and its enantiomers on nociception. As R(-)-mirtazapine exerts the antinociceptive activity of the racemic mixture it may be a putative candidate for an enantioselective use as analgesic.

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Citations

Aug 26, 2014·Psychopharmacology·Michael PaulzenSarah E Groppe
Jul 19, 2008·Anesthesia and Analgesia·Michael J Sheen, Shung-Tai Ho
Oct 30, 2020·Organic & Biomolecular Chemistry·Srinivas ChamakuriDamian W Young

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