Metabolic benefits of novel histamine H


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
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

111952

Informations de copyright

Copyright © 2021 The Authors. Published by Elsevier Masson SAS.. All rights reserved.

Auteurs

Kamil Mika (K)

Department of Pharmacological Screening, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Cracow, Poland.

Małgorzata Szafarz (M)

Department of Pharmacokinetics and Physical Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.

Marek Bednarski (M)

Department of Pharmacological Screening, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Cracow, Poland.

Kamil Kuder (K)

Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.

Katarzyna Szczepańska (K)

Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland; Department of Medicinal Chemistry, Maj Institute of Pharmacology Polish Academy of Sciences, 12 Smętna Street, 31-343 Kraków, Poland.

Krzysztof Pociecha (K)

Department of Pharmacokinetics and Physical Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.

Bartosz Pomierny (B)

Department of Biochemical Toxicology, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.

Katarzyna Kieć-Kononowicz (K)

Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.

Jacek Sapa (J)

Department of Pharmacological Screening, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Cracow, Poland.

Magdalena Kotańska (M)

Department of Pharmacological Screening, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Cracow, Poland. Electronic address: magda.dudek@uj.edu.pl.

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Classifications MeSH