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Molecular modification of compounds remains important strategy towards the discovery of new drugs. In this sense, this study presents a new pyrazole derivative 5-(1-(2-fluorophenyl)-1 H -pyrazol-4-yl)-1 H -tetrazole (LQFM039) and evaluated the anti-inflammatory, analgesic, and vasorelaxant effects of this compound as well the mechanisms of action involved in the pharmacological effects. For this, mice were orally treated with LQFM039 (17.5, 35, or 70 mg/kg) prior acetic acid-induced abdominal writhing, formalin, tail flick, and carrageenan-induced paw edema protocols. In addition, vascular reactivity protocols were made with aortic rings contraction with phenylephrine and stimulated with graded concentrations of LQFM039. Abdominal writhing and licking time in both neurogenic and inflammatory phases of formalin were reduced with LQFM039 without altering latency to nociceptive response in the tail flick test. Carrageenan-induced paw edema showed that LQFM039 reduces edema and cell migration. In addition, the mechanism of action of LQFM039 involves NO/cGMP pathway and calcium channels, since this new pyrazole derivate elicited concentration-dependent relaxation attenuated by Nω-nitro-l-arginine methyl ester and 1 H -[1,2,4] oxadiazolo [4,3-alpha]quinoxalin-1-one, and blockade of CaCl 2 -induced contraction. Altogether, our finding suggests anti-inflammatory, antinociceptive, and vasorelaxant effect of this new pyrazole derivative with involvement of NO/cGMP pathway and calcium channels.

The purpose of this study was to determine the validity of using the electromyography (EMG) signal as a noninvasive method of estimating the lactate threshold (LT) power output in recreational cyclists. Using an electromagnetic bicycle ergometer and constant pedaling cadence of 80 rpm, 24 recreational cyclists performed an incremental exercise protocol that consisted of stepwise increases in power output of 25 W every 3 min until exhaustion. The EMG signal was recorded from the right vastus lateralis (VL) and right rectus femoris (RF) throughout the test. Blood samples were taken from the fingertip every 3 min. The LT was determined by examining the relation between the lactate concentration and the power output using a log-log transformation model. The root mean square (RMS) value from the EMG signal was calculated for every 1-second non-superimposing window. Sets of pairs of straight regression lines were plotted and the corresponding determination coefficients (R(2)) were calculated. The intersection point of the pair of lines with the highest R(2) product was chosen to represent the EMG threshold (EMGT). The results showed that the correlation coefficients (r) between EMGT and LT were significant (p < 0.01) and high for the VL (r = 0.826) and RF (r = 0.872). The RF and VL muscles showed similar behavior during the maximal incremental test and the EMGT and LT power output were equivalent for both muscles. The validity of using EMG to estimate the LT power output in recreational cyclists was confirmed.