Itadani Satoshi, Takahashi Shinya, Ima Masaki, Sekiguchi Tetsuya, Fujita Manabu, Nakayama Yoshisuke, Takeuchi Jun
Medicinal Chemistry Research Laboratories and Department of Biology & Pharmacology, Ono Pharmaceutical Co., Ltd. , 3-1-1 Sakurai, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.
ACS Med Chem Lett. 2014 Oct 6;5(11):1230-4. doi: 10.1021/ml500298y. eCollection 2014 Nov 13.
The benzoxazine derivative, (2S)-4-(3-carboxypropyl)-8-{[4-(4-phenylbutoxy)benzoyl]amino}-3,4-dihydro-2H-1,4-benzoxazine-2-carboxylic acid (19, ONO-2050297), was identified as the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.
苯并恶嗪衍生物,(2S)-4-(3-羧丙基)-8-{[4-(4-苯基丁氧基)苯甲酰基]氨基}-3,4-二氢-2H-1,4-苯并恶嗪-2-羧酸(19,ONO-2050297),被鉴定为首个强效的半胱氨酰白三烯1(CysLT1)和半胱氨酰白三烯2(CysLT2)双重拮抗剂,其对CysLT1和CysLT2的半数抑制浓度(IC50)值分别为0.017 μM和0.00087 μM。