Atividade analgésica, anti-inflamatóriae vasorelaxante de dois derivados pirazólicos: 5-[1-(4- fluorfenil)-1H-pirazol-4-IL]-2H-tetrazola(LQFM 020) e 5- [1-(2-fluorofenil)-1H-pirazol-4-IL]-2H-tetrazola (LQFM 039)
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2014-10-31
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Universidade Federal de Goiás
Resumo
Inflammation is a complex process that aims to protect the body
eliminating the harmful agent and to promote tissue repair is characterized by
classic signs: pain, heat, redness and swelling as a result of failure to resolve
the inflammatory process may occur loss of function. Control of pain and
inflammation leads to the search for new drugs both analgesic and antiinflammatory
drugs with good efficacy to aid in the treatment of these deseases.
The aim of this study was to evaluate the pharmacological effects of two
pyrazole derivatives. In acute nociception tests LQFM 020 (9, 17.5 and 35
mg/kg) and LQFM 039 (17.5, 35 and 70 mg/kg) reduced the number of writhing
dose dependent manner to 53, 48 and 35; and 57, 52, 42, respectively, while
the control group the number of writhes was 88. In the formalin test this
antinociceptive effect was confirmed by the reduction in time reactivity to pain in
both test phases, the time in the control group was 78 and 72s in the first phase
and 150 and 128s in the second phase, with LQFM for 020 and 039 LQFM in
the first phase was to reduce 50 and 47s and the second phase to 97 and 74s
respectively. In bending the tail the groups of mice treated with LQFM 020 and
LQFM 039 test were not able to increase the latency to thermal stimulus
demonstrated that the analgesic effect does not involve central mechanisms.
Furthermore, the results of the enzymatic activity of cyclooxygenase (COX) and
phospholipase (PLA2) in vitro tests indicated no part of the mechanism of
action involved in the activity of these compounds. In vascular reactivity tests
LQFM 020 promoted vasorelaxant effect presenting maximum effect (Emax) of
93% in aortic preparations with endothelium and maximum effect (Emax) of 91%
without endothelium . LQFM 039 also promoted vasorelaxant effect with
maximum effect (Emax) of 80% when tested in preparations with endothelium
and maximum effect (Emax) of 76% without endothelium, given this result, we
investigated the mechanism of action of these compounds. Our results showed
that LQFM 020 and LQFM 039 demonstrated the involvement of NO/cGMP
pathway and suggest also the involvement of sensitive Ca2+ channels in the
plasma membrane voltage.
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OLIVEIRA, L. P. Atividade analgésica, anti-inflamatóriae vasorelaxante de dois derivados pirazólicos: 5-[1-(4- fluorfenil)-1H-pirazol-4-IL]-2H-tetrazola(LQFM 020) e 5- [1-(2-fluorofenil)-1H-pirazol-4-IL]-2H-tetrazola (LQFM 039). 2014. 62 f. Dissertação (Mestrado em Biologia) - Universidade Federal de Goiás, Goiânia, 2014.