Annual Activities Report 2011 - INCT-Inofar - UFRJ
Annual Activities Report 2011 - INCT-Inofar - UFRJ
Annual Activities Report 2011 - INCT-Inofar - UFRJ
You also want an ePaper? Increase the reach of your titles
YUMPU automatically turns print PDFs into web optimized ePapers that Google loves.
<strong>Annual</strong> <strong>Report</strong> <strong>2011</strong> | <strong>INCT</strong>-INOFAR<br />
47<br />
Highlights<br />
The present data suggest that tadalafil has in vivotherapeutic anti-inflammatory effects by promoting<br />
antinociception and reducing the leukocyte influx into the synovial cavity in zymosan arthritis.<br />
Moreover, tadalafil was effective when given per os, indicating a therapeutic potential in humans. The<br />
analgesic effect is probably secondary to the activation of cGMP in nociceptive neurons and did not<br />
appear to depend on the release of endogenous opioids. In addition to the specific direct effect via cGMP<br />
modulation, we propose that the antinociceptive effect of tadalafil is also linked to a decreased release<br />
of TNF-a associated with the reduction of neutrophil migration into the joints. Usually, the patients<br />
prescribed PDE-5 inhibitors to treat erectile dysfunction are those also affected by osteoarthritis. The<br />
possibility of relief of joint pain provided by these compounds, as a side effect, could possibly increase<br />
patient compliance with the therapy.<br />
Pharmacological activity of novel<br />
2-hydroxyacetophenone isatin<br />
derivatives on cardiac and vascular<br />
smooth muscle in rats<br />
Daniele Gabriel; Luana Braga Pontes; Jaqueline Soares da Silva; Roberto Takashi Sudo; Marilza Baptista<br />
Corrêa; Ângelo da Cunha Pinto; Simon John Garden; Gisele Zapata-Sudo. J. Cardiovasc. Pharmacol. 57<br />
(<strong>2011</strong>) 20-27.<br />
Isatin (1H-indole-2,3 dione) is an endogenous compound with biological activities. Many of its<br />
derivatives have pharmacological effects, including inhibition of cyclic guanosine monophosphate levels<br />
in cardiac tissue; sedative-hypnotic profiles; anticonvulsant, analgesic, antithermic and anti-inflammatory<br />
activities; and anxyolitic, antimicrobial and proapoptotic effects. This work investigated the effects on the<br />
cardiovascular system of two novel 2-hydroxyacetophenone derivatives of isatin. The MB101 and MB130<br />
compounds were synthesized by introducing a carboethoxy group on isatin, resulting in novel molecules of<br />
unknown pharmacological profile.
Change language