Antinociceptive property of intrathecal and intraperitoneal administration of a novel water-soluble isoindolin-1-one derivative, JM 1232 (-) in rats

European Journal of Pharmacology
Tomoki NishiyamaYoshitsugu Yamada

Abstract

Antinociceptive effects of a new water-soluble sedative agent, an isoindolin-1-one derivative, (-)-3-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]-2-phenyl-3,5,6,7-tetrahydrocyclopenta[f]isoindol-1-(2H)-one (JM 1232 (-)) were studied in two different nociceptive models of rats. Sprague-Dawley rats with lumbar intrathecal catheters were tested for their thermal tail withdrawal response and for their paw flinches by formalin injection after intrathecal administration of various doses of JM 1232 (-). The effects of intraperitoneal administration were also investigated. In addition, behavioral side effects were examined. When antinociceptive effects were observed, the effects of pretreatment with flumazenil or naloxone for the maximum effective dose were evaluated. Eight rats were used in each dose of each group. Intrathecal JM 1232 (-) increased the tail flick latency and decreased the number of flinches in both phases 1 and 2 of the formalin test. These changes were antagonized by intrathecal flumazenil but not by naloxone. Intraperitoneal JM 1232 (-) had no effects on the tail flick latency, but decreased the number of flinches in both phases 1 and 2 of the formalin test. The latter was antagonized by intraperitoneal flumazenil and na...Continue Reading

References

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Citations

Jul 24, 2010·British Journal of Anaesthesia·J R Sneyd, A E Rigby-Jones
Jul 6, 2010·Journal of Cardiothoracic and Vascular Anesthesia·Takahiro MoriyamaYuichi Kanmura
May 9, 2013·Surgical Neurology International·Hovig V ChitilianDouglas E Raines
Mar 13, 2019·Chemistry, an Asian Journal·Wei GaoYiyuan Peng
Jan 10, 2012·Anesthesiology·J Robert SneydKaren Grimsehl
Aug 18, 2020·Expert Opinion on Therapeutic Patents·Xuqing Zhang, Mark J Macielag
Oct 2, 2009·Peptides·Richard J Bodnar
Jan 27, 2010·Current Opinion in Supportive and Palliative Care

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