Journal
BIOLOGICAL & PHARMACEUTICAL BULLETIN
Volume 33, Issue 6, Pages 1067-1069Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.33.1067
Keywords
CC chemokine receptor 4; RS-1748; airway inflammation
Categories
Ask authors/readers for more resources
CC chemokine receptor 4 (CCR4) is generally recognized as a preferential marker for T helper 2 cells, and we have previously reported morpholine-derivative CCR4 antagonists, RS-1154 and RS-1269. Here, we investigate the pharmacological profiles of a novel pyrimidine-derivative CCR4 antagonist, 2-{4-[2-(diethylamino)ethoxy]phenyl}-N-(2,4-difluorobenzyl)-5-fluoropyrimidin-4-amine (RS-1748), which showed potency to inhibit the bindings of [I-125]CCL17 and [S-35]GTP gamma S to human CCR4-expressing Chinese hamster ovary (CHO) cells with IC50 values of 59.9 nm and 18.4 nm, respectively. Furthermore, RS-1748 inhibited ovalbumin-induced airway inflammation in guinea pigs at a dose of 10 mg/kg. These results indicate that RS-1748 would be a promising lead compound for developing a therapeutic agent against asthma.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available