Abstract
From a series of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides derived from 4-methyl-4'-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]-1,2,3-thiadiazole-5-carboxanilide, one inhibited thapsigargin-induced Ca2+ influx in Jurkat T cells (IC(50)=77 nM) and exhibited high selectivity for the CRAC channel over the VOC channel (index: >130). Another acted as an inhibitor for both T lymphocyte activation-induced diseases and ovalbumin-induced airway eosinophilia in rats (ED(50)=1.3 mg/kg) p.o.
MeSH terms
-
Anilides / chemical synthesis
-
Anilides / chemistry
-
Anilides / pharmacology*
-
Animals
-
Calcium / metabolism*
-
Calcium Channel Blockers / chemical synthesis
-
Calcium Channel Blockers / chemistry
-
Calcium Channel Blockers / pharmacology*
-
Calcium Channels / drug effects*
-
Calcium Signaling / drug effects
-
Enzyme Inhibitors / pharmacology
-
Female
-
Humans
-
Hypersensitivity / drug therapy
-
Interleukin-2 / metabolism
-
Jurkat Cells
-
Lymphocyte Activation / drug effects
-
Male
-
Mice
-
Pulmonary Eosinophilia / chemically induced
-
Pulmonary Eosinophilia / drug therapy
-
Pyrazoles / chemical synthesis
-
Pyrazoles / chemistry
-
Pyrazoles / pharmacology*
-
Rats
-
Rats, Inbred BN
-
Structure-Activity Relationship
-
T-Lymphocytes / drug effects
-
T-Lymphocytes / metabolism
-
Thapsigargin / pharmacology
Substances
-
Anilides
-
Calcium Channel Blockers
-
Calcium Channels
-
Enzyme Inhibitors
-
Interleukin-2
-
Pyrazoles
-
Thapsigargin
-
Calcium