Antinociceptive Effects of Tetrahydrophthalimides and Related Compounds

Abstract

This paper describes the antinociceptive effects of tetrahydrophthalimides and related compounds in mice. Twenty compounds were obtained by the reaction of cis-1,2,3,6-tetrahydrophthalic anhydride with appropriate amines, dehydration, and addition to the imidic double bond. They were analyzed in the writhing test at 10 mg/kg given intraperitoneally. The most active compound 2-benzyl-5-morpholin-4-yl-hexahydroisoindole-1,3-dione (19) was studied on formalin, capsaicin, glutamate and hot plate models. The antinociceptive activity demonstrated by some studied compounds is promising, and some of them were more active than acetylsalicylic acid and paracetamol used as reference drugs in writhing tests in mice. Compound 19 was about 5-fold more potent than the reference drugs, being also effective by oral route and against the inflammatory response in the formalin test. The results suggest that compound 19 could be used as a model to obtain new and more potent antinociceptive agents. It exhibits an interesting antinociceptive profile, and does not interact with opioid systems.

Analyses of chemical composition and gastroprotective and antinociceptive properties of Eugenia involucrate DC. leaves

“…The results of the evaluation of CME-Jul, CLF-Jul, and EAF-Jul at a dose of 10 mg/kg indicated that all the samples tested significantly reduced the nociception, but a greater result was observed for the non-polar fraction, CLF-Jul (64.4%) (Figure 3). Common drugs used in clinical treatments, such as aspirin and paracetamol, show inhibition around 35% in same conditions (Costa et al, 2007). After this trial result, it was determined the DI 50 (minimal dose able to inhibit 50% of writhings compared to the control group) of CLF-Jul (Figure 4).…”

“…Since many years ago, plants have been employed with success to cure the more distinct ailments. Currently, modern medicinal chemistry is using new approaches and technologies that confirm the scientific evidence on the therapeutic efficacy of various medicinal plants, their isolated substances and derivatives (Filho, 2015;Alves, 2013;Cragg and Newman, 2013).…”