前列腺素D2受体CRTH2的选择性拮抗剂及相应放射性配体的合成与体外评价
Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2.
作者信息
Ulven Trond, Gallen Michael J, Nielsen Mads C, Merten Nicole, Schmidt Carola, Mohr Klaus, Tränkle Christian, Kostenis Evi
机构信息
Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
出版信息
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5924-7. doi: 10.1016/j.bmcl.2007.07.080. Epub 2007 Aug 22.
Synthesis and preliminary in vitro biological evaluation of a selective high-affinity CRTH2 antagonist is described. The stability of an N-benzyl group facilitated synthesis of the corresponding radioligand by tritiation of a brominated precursor. The compound [(3)H]TRQ11238 represents the first selective CRTH2 antagonist radioligand and exhibited a specific radioactivity of 52 Ci/mmol and a pK(d) of 9.0.
本文描述了一种选择性高亲和力CRTH2拮抗剂的合成及其初步体外生物学评价。N-苄基的稳定性有助于通过溴化前体的氚化合成相应的放射性配体。化合物[(3)H]TRQ11238是首个选择性CRTH2拮抗剂放射性配体，其比活度为52 Ci/mmol，解离常数pK(d)为9.0。
Zotero 插件