2,4-噻唑烷二酮类作为强效且选择性的人β3激动剂。
2,4-Thiazolidinediones as potent and selective human beta3 agonists.
作者信息
Hu B, Ellingboe J, Gunawan I, Han S, Largis E, Li Z, Malamas M, Mulvey R, Oliphant A, Sum F W, Tillett J, Wong V
机构信息
Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2001 Mar 26;11(6):757-60. doi: 10.1016/s0960-894x(01)00063-4.
Abstract
Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50=0.01 microM, IA=1.19) and selective (more than 110-fold over beta1 and beta2 agonist activity) beta3 agonist. This compound has also been proven to be active and selective in an in vivo mode.
摘要
甲基磺酰胺取代的2,4-噻唑烷二酮22c是一种强效（EC50 = 0.01微摩尔，内在活性= 1.19）且具有选择性（对β1和β2激动剂活性的选择性超过110倍）的β3激动剂。该化合物在体内模式下也已被证明具有活性和选择性。
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