Anti-inflammatory, antinociceptive, and vasorelaxant effects of a new pyrazole compound 5-(1-(2-fluorophenyl)-1-pyrazol-4-yl)-1-tetrazole: role of NO/cGMP pathway and calcium channels.

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-pyrazol-4-yl)-1-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.

Acute toxicity, antinociceptive, and anti-inflammatory activities of the orally administered crotamine in mice.

Crotamine is a polypeptide toxin isolated from rattlesnake venom. Although several studies have been developed identifying many biological effects of isolated crotamine, none of them evaluated its acute toxicity, antinociceptive, and anti-inflammatory activities through oral administration. All in vivo experiments from this study were performed in mice.

Food-Effect on (-) - Hydroxycitric Acid Absorption After Oral Administration of Garcinia cambogia Extract Formulation: a Phase I, Randomized, Cross-Over Study.

Garcinia cambogia extract (GCE)/(-) - hydroxycitric acid (HCA) has been identified as a potential antiobesity agent. However, controversial clinical trial results have been published on its biological effect and poor pharmacokinetic (PK) information increases its dubious efficacy. The aim of this study was to determine the main PK parameters of GCE/HCA in healthy women, and to evaluate food effects on HCA absorption.

Activation of PI3K/Akt pathway mediated by estrogen receptors accounts for estrone-induced vascular activation of cGMP signaling.

Estrone (E1) produces remarkable vascular effects, including relaxation, modulation of proliferation, apoptosis and cell adhesion. This study investigated the role of estrogen receptors and endothelial signaling pathways in the vascular relaxation promoted by E1. Aortic rings from male Wistar rats (250-300 g) were contracted with phenylephrine and stimulated with graded concentrations of E1.

Preclinical Assessment of Cardiovascular Alterations Induced by Birch Polypore Mushroom, Piptoporus betulinus (Agaricomycetes).

Piptoporus betulinus has been used in folk medicine for millennia. However, no data currently exist regarding its potential cardiovascular activity. In this work, the crude ethanolic extract and fractions (hexane, ethyl acetate, and water) with increased polarity from the partitioning process, as well as stigmasterol (the major metabolite isolated from P.

Essential Oil Composition, Antimicrobial and Pharmacological Activities of Cham. (Verbenaceae) From São Gonçalo do Abaeté, Minas Gerais, Brazil.

Background: (Verbenaceae) is used in Brazilian folk medicine as an antiseptic, and it is usually applied topically on skin, mucous membranes, mouth, and throat, or used for vaginal washings.

Objectives: To analyze the chemical composition of the essential oil from collected in São Gonçalo do Abaeté, Minas Gerais and grown in Hidrolândia, Goiás; to evaluate the antimicrobial activity of the essential oil, crude ethanol extract, and hexane, dichloromethane, ethyl-acetate, and aqueous fractions (AFs); to study the antinociceptive, anti-inflammatory, and central nervous system activities of the crude ethanol extract.

Materials And Methods: The essential oils were obtained by hydro-distillation using a Clevenger-type apparatus and analyzed by GC/MS.

New pyrazole derivative 5-[1-(4-fluorophenyl)-1H-pyrazol-4-yl]-2H-tetrazole: synthesis and assessment of some biological activities.

The molecular modification and synthesis of compounds is vital to discovering drugs with desirable pharmacological and toxicity profiles. In response to pyrazole compounds' antipyretic, analgesic, and anti-inflammatory effects, this study sought to evaluate the analgesic, anti-inflammatory, and vasorelaxant effects, as well as the mechanisms of action, of a new pyrazole derivative, 5-[1-(4-fluorophenyl)-1H-pyrazol-4-yl]-2H-tetrazole. During the acetic acid-induced abdominal writhing test, treatments with 5-[1-(4-fluorophenyl)-1H-pyrazol-4-yl]-2H-tetrazole reduced abdominal writhing, while during the formalin test, 5-[1-(4-fluorophenyl)-1H-pyrazol-4-yl]-2H-tetrazole reduced licking times in response to both neurogenic pain and inflammatory pain, all without demonstrating any antinociceptive effects, as revealed during the tail flick test.

Anti-nociceptive and anti-inflammatory activities of 4-[(1-phenyl-1H-pyrazol-4-yl) methyl] 1-piperazine carboxylic acid ethyl ester: A new piperazine derivative.

Piperazine compounds possess anti-infective, anti-carcinogenic, anxiolytic, hypotensive, anti-hypertensive and vasorelaxant properties and are attractive candidates for the development of new analgesic and anti-inflammatory drugs. This study investigates the anti-nociceptive and anti-inflammatory effects of piperazine derivative 4-[(1-phenyl-1H-pyrazol-4-yl) methyl]1-piperazine carboxylic acid ethyl ester (LQFM-008) and the involvement of the serotonergic pathway. In the formalin test, treatments with LQFM-008 (15 and 30mg/kg p.

Involvement of the NO/cGMP/KATP pathway in the antinociceptive effect of the new pyrazole 5-(1-(3-fluorophenyl)-1H-pyrazol-4-yl)-2H-tetrazole (LQFM-021).

The pyrazol compounds are known to possess antipyretic, analgesic and anti-inflammatory activities. This study was conducted to investigate the peripheral antinociceptive effect of the pyrazole compound 5-(1-(3-Fluorophenyl)-1H-pyrazol-4-yl)-2H-tetrazole (LQFM-021) and involvement of opioid receptors and of the NO/cGMP/K(ATP) pathway. The oral treatments in mice with LQFM-021 (17, 75 or 300 mg/kg) decreased the number of writhing.

Hypotensive and vasorelaxant effects of (E) - methyl isoeugenol: a naturally occurring food flavour.

Application of naturally occurring (E) - methyl isoeugenol (MIE) as food flavour has been widely accepted despite the growing concerns over cardiovascular issue. Hence, we sought to investigate hypotensive property of MIE and the involvement of central and/or peripheral mechanism (s). Variation in mean arterial pressure (MAP), heart rate (HR), systolic blood pressure (SBP), baroreflex sensitivity of normotensive rats and vascular reactivity were recorded.