Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases.
Allergic diseases
Histamine H1 receptor antagonists
Muscarinic M3 receptor
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Mar 2024
15 Mar 2024
Historique:
received:
23
11
2023
revised:
27
01
2024
accepted:
28
01
2024
medline:
18
3
2024
pubmed:
19
2
2024
entrez:
18
2
2024
Statut:
ppublish
Résumé
Desloratadine, a second-generation histamine H1 receptor antagonist, has established itself as a first-line drug for the treatment of allergic diseases. Despite its effectiveness, desloratadine exhibits an antagonistic effect on muscarinic M3 receptor, which can cause side effects such as dry mouth and urinary retention, ultimately limiting its clinical application. Herein, we describe the discovery of compound Ⅲ-4, a novel H1 receptor antagonist with significant H1 receptor antagonistic activity (IC
Identifiants
pubmed: 38368709
pii: S0223-5234(24)00077-1
doi: 10.1016/j.ejmech.2024.116197
pii:
doi:
Substances chimiques
Histamine H1 Antagonists
0
desloratadine
FVF865388R
Receptors, Histamine H1
0
Loratadine
7AJO3BO7QN
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
116197Informations de copyright
Copyright © 2024. Published by Elsevier Masson SAS.
Déclaration de conflit d'intérêts
Declaration of competing interest We declare that we have no financial and personal relationships with other people or organizations that can inappropriately influence our work, there is no professional or other personal interest of any nature or kind in any product, service and company that could be construed as influencing the position presented in, or the review of, the manuscript entitle.