中文名富马酸福莫特罗英文名Formoterol Fumarate别名富马酸福莫特罗半富马酸福莫特罗福美特罗富马酸盐富马酸福莫特罗无水物富马酸福莫特罗(无水)福莫特罗杂质I鉴别 EP标准品富马酸福莫特罗系统适应性 EP标准品N-[2-羟基-5[(RS)-1-羟基-2-[(RS)-2-(4-甲氧基苯基)-1-甲基乙基胺]乙基]苯基]甲酰胺半富马酸英文别名AtockBD 40AForadilYM-08316Oxis pMDiNSC 299587CGP 25827AAformoterolPerforomistUNII-P3T5QA5J9NForadil AerolizerForadil acrolizerForadil CertihalerFormoterol FumarateFORMATEROL FUMATATEFormoterol fumarate JP13Formoterol fumarate 50 gramformamide,n-(2-hydroxy-5-(1-hydroxy-2-((2-(4-methoxyphenyl)-1-methylethyl)aminN-{2-hydroxy-5-[(1S)-1-hydroxy-2-{[(1S)-2-(4-methoxyphenyl)-1-methylethyl]amino}ethyl]phenyl}formamide(R*,R*)-N-[2-HYDROXY-5-[1-HYDROXY-2-[[2-(4-METHOXYPHENYL)-1-METHYLETHYL]AMINO]ETHYL]PHENYL]FORMAMIDE FUMARATE(R*,R*)-(+)-N-[2-HYDROXY-5-[1-HYDROXY-2-[[2-(4-METHOXYPHENYL)-1-METHYLETHYL]AMINO]ETHYL]-PHENYL]FORMAMIDE FUMARATEN-[2-hydroxy-5-(1-hydroxy-2-{[2-(4-methoxyphenyl)-1-methylethyl]amino}ethyl)phenyl]formamide (2E)-but-2-enedioate (salt)N-{2-hydroxy-5-[(1S)-1-hydroxy-2-{[(1S)-2-(4-methoxyphenyl)-1-methylethyl]amino}ethyl]phenyl}formamide (2E)-but-2-enedioate (salt)N-{2-hydroxy-5-[(1R)-1-hydroxy-2-{[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino}ethyl]phenyl}formamide (2E)-but-2-enedioate (salt)CAS43229-80-7EINECS1308068-626-2化学式C42H52N4O12分子量804.88InChIInChI=1/C19H24N2O4.C4H4O4/c1-13(9-14-3-6-16(25-2)7-4-14)20-11-19(24)15-5-8-18(23)17(10-15)21-12-22;5-3(6)1-2-4(7)8/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22);1-2H,(H,5,6)(H,7,8)/b;2-1+熔点138-140°C沸点603.2°C at 760 mmHg闪点318.6°C蒸汽压2.12E-15mmHg at 25°C溶解度Slightly soluble in water, soluble in methanol, slightly soluble in 2-propanol, practically insoluble in acetonitrile.酸度系数pKa1 7.9; pKa2 9.2(at 25℃)存储条件Room temperature稳定性Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.外观neat颜色White to off-white最大波长(λmax)['284nm(lit.)']Merck14,4245体外研究Formoterol是一种有效的气道平滑肌松弛剂,对β2肾上腺素受体具有高效,高亲和力和选择性。Formoterol似乎在气道平滑肌中保留一段时间,由于其对人气道平滑肌的松弛作用能够耐反复冲洗,冲去β肾上腺素受体拮抗剂后,formoterol表现出“重新确认”的松弛作用。在实验测试系统中,Formoterol被证明能够有效抑制这些细胞和过程。 Formoterol,如salbutamol和salmeterol,在离体准备中松弛豚鼠气管和人支气管,并浓度依赖性抑制抗原诱导的炎症介质从人肺片中释放。体内研究在有意识的豚鼠体内,Formoterol剂量相关性抑制组胺诱导的支气管收缩。在豚鼠体内,Formoterol抑制组胺诱导的血浆蛋白质渗出(PPE),10 mg /mL和100 mg /mL剂量时,能够观察到显著的抑制作用。在豚鼠肺中,Formoterol (100 mg /mL)抑制PPE 2-4小时,作用时间介于之前得到的salbutamol (1小时)和salmeterol (> 6 小时)之间。在豚鼠肺中,Formoterol抑制中性粒细胞聚集(脂多糖诱导的),但是比抑制粒细胞不依赖性PPE(组胺诱导的)需要更高的剂量。在豚鼠肺中,Formoterol (100 mg /mL)抑制PAF诱导的嗜酸性粒细胞聚集。