Acute and subacute antidiabetic studies of ENP-9, a new 1,5-diarylpyrazole derivative

The Journal of Pharmacy and Pharmacology
Eduardo Hernández-VázquezSamuel Estrada-Soto

Abstract

To explore the antihyperglycaemic and antidiabetic effects and to determine the acute toxicity of 5-(4-chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide (ENP-9). The antihyperglycaemic effect of ENP-9 (50 mg/kg) was determined by oral glucose tolerance test (OGTT). Also, the acute (16, 50 and 160 mg/kg) and subacute (50 mg/kg/day for 10 days) antidiabetic effects of ENP-9 were determined. After subacute treatment, blood samples were analysed to determine glucose and lipid profiles. Also, an acute toxicity determination of ENP-9 was conducted followed the OECD recommendation. Molecular docking was performed using AutoDock 4.2.6 at human cannabinoid receptor 1 (PDB code 5TGZ). Acute Administration of ENP-9 showed significant antidiabetic effect and decreased the maximum OGTT peak, compared to the control group (P < 0.05). Moreover, the 10 days treatment induced a decrease in plasma glucose levels, being significant at the end of the experiments (P < 0.05); however, triacylglycerols and cholesterol were not modified. Finally, LD50 of ENP-9 was estimated to be greater than 2000 mg/kg. Molecular docking suggests that ENP-9 may act as rimonabant does. ENP-9 showed significant antihyperglycaem...Continue Reading

References

Jul 27, 2002·Planta medica·E J Verspohl
Apr 28, 2005·Nature Neuroscience·Vincenzo Di Marzo, Isabel Matias
Jun 7, 2006·Biological & Pharmaceutical Bulletin·Koji HayashiMikio Ito
Jan 9, 2007·Lancet·Raj S Padwal, Sumit R Majumdar
Jun 11, 2008·Current Opinion in Clinical Nutrition and Metabolic Care·André J Scheen, Nicolas Paquot
Jul 8, 2008·Journal of Neuroendocrinology·L BellocchioU Pagotto
Oct 28, 2008·Bioorganic & Medicinal Chemistry·Mario AlvaradoFernando Rodríguez de Fonseca
Apr 29, 2009·Journal of Computational Chemistry·Garrett M MorrisArthur J Olson
Jul 29, 2010·The Journal of Clinical Investigation·Joseph TamGeorge Kunos
Oct 12, 2010·Bioorganic & Medicinal Chemistry Letters·Ho Yin LoStéphane De Lombaert
Mar 8, 2011·Bioorganic & Medicinal Chemistry Letters·Hamid R HoveydaGraeme Fraser
Aug 13, 2011·Bioorganic & Medicinal Chemistry Letters·Michael S MalamasMenelas N Pangalos
Jun 15, 2012·Bioorganic & Medicinal Chemistry Letters·Ravindra B PathakH H Parekh
Jul 5, 2012·American Journal of Physiology. Endocrinology and Metabolism·Vidya VaidyanathanElizabeth J Parks
Apr 3, 2013·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·S A Al-AbriK R Olson
Jun 12, 2013·European Journal of Medicinal Chemistry·J Ashok KumarB China Raju
Sep 3, 2013·European Journal of Medicinal Chemistry·Eduardo Hernández-VázquezFrancisco Hernández-Luis
Dec 9, 2010·ACS Medicinal Chemistry Letters·Katrin Stierand, Matthias Rarey
Dec 2, 2014·Bioorganic & Medicinal Chemistry Letters·Ellen KickRaju Mohan
Jun 17, 2015·European Journal of Medicinal Chemistry·Eduardo Hernández-VázquezSamuel Estrada-Soto
Nov 26, 2015·Journal of Pharmacological and Toxicological Methods·Miroslav RadenkovićMilica Prostran
Mar 11, 2016·Bioorganic & Medicinal Chemistry Letters·Litzia Cerón-RomeroSamuel Estrada-Soto
May 18, 2016·Expert Opinion on Drug Discovery·Aeri LeeDongsup Kim
May 19, 2016·European Journal of Medicinal Chemistry·Mohemmed Faraz KhanMohammad Shaquiquzzaman
Mar 23, 2017·European Journal of Pharmacology·Eduardo Hernández-VázquezSamuel Estrada-Soto
Jul 5, 2017·Chemical Biology & Drug Design·Battistina AsproniGérard A Pinna

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

© 2022 Meta ULC. All rights reserved