Annual Activities Report 2011 - INCT-Inofar - UFRJ

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Annual Report 2011 | INCT-INOFAR 46 Highlights Figure 1: Antinociceptive effects of tadalafil in zymosan-induced arthritis (A) and experimental osteoarthritis, where was evaluated the effect of the guanylyl cyclase inhibitor (ODQ) on the antiinflammatory activity of tadalafil (B). Table 1: Effect of the guanylyl cyclase inhibitor (ODQ) on the anti-inflammatory activity of tadalafil in zymosan-induced arthritis. In zymosan-induced arthritis, tadalafil significantly decreased the cell influx and TNF-α release to the articular cavity, but did not alter IL-1 or CINC-1 levels (Fig.3). Figure 2: Effects of tadalafil on the acute cell influx and cytokine (TNF-α) release in zymosan arthritis.
Annual Report 2011 | INCT-INOFAR 47 Highlights The present data suggest that tadalafil has in vivotherapeutic anti-inflammatory effects by promoting antinociception and reducing the leukocyte influx into the synovial cavity in zymosan arthritis. Moreover, tadalafil was effective when given per os, indicating a therapeutic potential in humans. The analgesic effect is probably secondary to the activation of cGMP in nociceptive neurons and did not appear to depend on the release of endogenous opioids. In addition to the specific direct effect via cGMP modulation, we propose that the antinociceptive effect of tadalafil is also linked to a decreased release of TNF-a associated with the reduction of neutrophil migration into the joints. Usually, the patients prescribed PDE-5 inhibitors to treat erectile dysfunction are those also affected by osteoarthritis. The possibility of relief of joint pain provided by these compounds, as a side effect, could possibly increase patient compliance with the therapy. Pharmacological activity of novel 2-hydroxyacetophenone isatin derivatives on cardiac and vascular smooth muscle in rats Daniele Gabriel; Luana Braga Pontes; Jaqueline Soares da Silva; Roberto Takashi Sudo; Marilza Baptista Corrêa; Ângelo da Cunha Pinto; Simon John Garden; Gisele Zapata-Sudo. J. Cardiovasc. Pharmacol. 57 (2011) 20-27. Isatin (1H-indole-2,3 dione) is an endogenous compound with biological activities. Many of its derivatives have pharmacological effects, including inhibition of cyclic guanosine monophosphate levels in cardiac tissue; sedative-hypnotic profiles; anticonvulsant, analgesic, antithermic and anti-inflammatory activities; and anxyolitic, antimicrobial and proapoptotic effects. This work investigated the effects on the cardiovascular system of two novel 2-hydroxyacetophenone derivatives of isatin. The MB101 and MB130 compounds were synthesized by introducing a carboethoxy group on isatin, resulting in novel molecules of unknown pharmacological profile.
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Annual Activities Report 2011 - INCT-Inofar - UFRJ

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