Pharmacological profile of upacicalcet, a novel positive allosteric modulator of calcium-sensing receptor, in vitro and in vivo.
Calcimimetics
Calcium-sensing receptor
Gastric emptying
Parathyroid hormone
Secondary hyperparathyroidism
Upacicalcet
Journal
European journal of pharmacology
ISSN: 1879-0712
Titre abrégé: Eur J Pharmacol
Pays: Netherlands
ID NLM: 1254354
Informations de publication
Date de publication:
05 Oct 2023
05 Oct 2023
Historique:
received:
31
03
2022
revised:
10
07
2023
accepted:
31
07
2023
medline:
31
8
2023
pubmed:
5
8
2023
entrez:
4
8
2023
Statut:
ppublish
Résumé
Upacicalcet (formerly SK-1403/AJT240) is a novel non-peptide calcimimetic agent that acts as a calcium-sensing receptor (CaSR) agonist for the treatment of secondary hyperparathyroidism (SHPT) in chronic kidney disease (CKD). We compared upacicalcet with other calcimimetics (etelcalcetide or cinacalcet) and examined its in vitro and in vivo characteristics in terms of its human CaSR agonistic activity, its efficacy in normal and CKD rats after a single administration, and its effect on gastric emptying in rats. Upacicalcet activated human CaSR depending on the extracellular calcium (Ca
Identifiants
pubmed: 37541363
pii: S0014-2999(23)00448-X
doi: 10.1016/j.ejphar.2023.175936
pii:
doi:
Substances chimiques
Cinacalcet
UAZ6V7728S
Receptors, Calcium-Sensing
0
upacicalcet
5C1222PBE2
Parathyroid Hormone
0
Calcium
SY7Q814VUP
Calcimimetic Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
175936Informations de copyright
Copyright © 2023 The Authors. Published by Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper