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α-第二丁基对羟基苄醇(简称天-018)是中枢苯二氮革受体的新型配基。作者以天-018为先导化合物,设计并合成了17个目标化合物,其中13个未见文献报道。通过体外竞争性放射配基受体结合分析,对所合成的化合物进行筛选,发现有7个化合物选择性地作用于脑苯二氮(艹卓)受体,其亲和力与结构相关。以α-苄基对碘苄醇竞争抑制作用最强,IC_(50)为3.4×10~(-8)mol/L,表明其对该受体的亲和力最高。
α-2-Butyl p-hydroxybenzyl alcohol (abbreviated as day-018) is a new ligand for central benzodiazepine receptors. The authors designed and synthesized 17 target compounds using Sky-018 as the lead compound, 13 of which have not been reported in the literature. Through in vitro competitive radioligand receptor binding analysis, the synthesized compounds were screened and found that seven compounds selectively act on the brain benzodiazepine receptor, and its affinity is structurally related. The competitive inhibition with α-benzyl-iodobenzyl alcohol was the strongest. IC 50 was 3.4 × 10 -8 mol / L, indicating that it had the highest affinity to this receptor.