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

Objectives 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). Methods The antihyperglycaemic effect of ENP‐9 (50 mg/kg) was determined by oral gluc...

Full description

Saved in:
Bibliographic Details
Published in:Journal of pharmacy and pharmacology 2018-08, Vol.70 (8), p.1031-1039
Main Authors: Hernández‐Vázquez, Eduardo, Young‐Peralta, Sandra, Cerón‐Romero, Litzia, García‐Jiménez, Sara, Estrada‐Soto, Samuel
Format: Article
Language:English
Subjects:
Acute toxicity
acute toxicological studies
antidiabetic effect
Antidiabetics
cannabinoid receptor 1 antagonist
Cannabinoid receptors
Cholesterol
Diabetes mellitus
ENP‐9
Glucose
Glucose tolerance
Molecular chains
rimonabant analogue
Triglycerides
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Objectives 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). Methods 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). Key findings Acute Administration of ENP‐9 showed significant antidiabetic effect and decreased the maximum OGTT peak, compared to the control group (P 
ISSN:0022-3573
2042-7158
DOI:10.1111/jphp.12933