JNJ-31020028 Size:Solid 10 mg AZD1981 displaced radio-labelled PGD2 from

AZD1981 displaced radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8

N-[4-({3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}amino)quinazolin-6-yl]prop-2-enamide

CAS Number: 125494-59-9

PMID: 25928480

Hashikawa K

JNJ-31020028 Size:Solid 10 mg AZD1981 displaced radio-labelled PGD2 fromJNJ 31020028 is a selective brain penetrant small molecule antagonist of the neuropeptide Y Y(2) receptor. JNJ 31020028 bound with high affinity (pIC(50) = 8. 07 + 0. 05, human, and pIC(50) = 8. 22 + 0. 06, rat) and was >100 fold selective versus human Y(1), Y(4), and Y(5) receptors. JNJ 31020028 was demonstrated to be an antagonist (pK(B) = 8. 04 + 0. 13) in functional assays. JNJ 31020028 occupied Y(2) receptor binding sites (approximately 90% at 10