Metabolic benefits of novel histamine H
Adipose Tissue
/ drug effects
Animals
Body Weight
/ drug effects
C-Peptide
/ blood
Carrier Proteins
/ blood
Cholesterol
/ blood
Energy Intake
/ drug effects
Feeding Behavior
/ drug effects
Female
Glucose Tolerance Test
Histamine Agonists
/ administration & dosage
Histamine Antagonists
/ administration & dosage
Injections, Intraperitoneal
Insulin
/ blood
Insulin Resistance
Leptin
/ blood
Ligands
Metformin
/ administration & dosage
Models, Animal
Obesity
/ drug therapy
Rats, Wistar
Receptors, Histamine H3
/ metabolism
Triglycerides
/ blood
Histamine H3 receptor ligands
Model of excessive eating
Journal
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
ISSN: 1950-6007
Titre abrégé: Biomed Pharmacother
Pays: France
ID NLM: 8213295
Informations de publication
Date de publication:
Oct 2021
Oct 2021
Historique:
received:
21
05
2021
revised:
16
07
2021
accepted:
20
07
2021
pubmed:
30
7
2021
medline:
5
1
2022
entrez:
29
7
2021
Statut:
ppublish
Résumé
One of the therapeutic approaches in the treatment of obesity is the use of histamine H Histamine ligands were selected based on the preliminary studies which included determination of intrinsic activity and selected pharmacokinetic parameters. Female Wistar rats were fed palatable feed for 28 days and simultaneously the tested compounds were administered intraperitoneally at a dose of 10 mg/kg b.w./day. Rats' weight was evaluated daily and calories intake was evaluated once per week. At the end of experiment insulin and glucose tolerance tests was performed. Plasma levels of cholesterol, triglycerides, leptin, insulin, glucose, C-peptide and CRP were also determined. In order to rule out false-positive results the influence of tested compounds on spontaneous activity of rats was monitored. Animals fed palatable feed and treated with KSK-61 or KSK-63 compounds showed the slowest weight gain which was comparable to the one observed in control animals. Both compounds with the highest pharmacological activity have also similar pharmacokinetic properties with quite long half-life and high volume of distribution indicating that they can freely cross most biological barriers. Some compounds, especially KSK-63, compensated for metabolic disorders. The presented study proves that search among the active histamine H
Identifiants
pubmed: 34325303
pii: S0753-3322(21)00734-4
doi: 10.1016/j.biopha.2021.111952
pii:
doi:
Substances chimiques
C-Peptide
0
Carrier Proteins
0
Crp protein, rat
0
Histamine Agonists
0
Histamine Antagonists
0
Insulin
0
Leptin
0
Ligands
0
Receptors, Histamine H3
0
Triglycerides
0
Metformin
9100L32L2N
Cholesterol
97C5T2UQ7J
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
111952Informations de copyright
Copyright © 2021 The Authors. Published by Elsevier Masson SAS.. All rights reserved.