Barrow C J, Sedlock D M, Sun H H, Cooper R, Gillum A M
Sterling Winthrop Pharmaceuticals Research Division, Malvern, PA 19355.
J Antibiot (Tokyo). 1994 Nov;47(11):1182-7. doi: 10.7164/antibiotics.47.1182.
WIN 66306 (1a), a cyclic peptide containing a novel amino acid, was isolated as a neurokinin antagonist from an Aspergillus species, labelled SC230. Conditions that maximized the production of 1a were developed, leading also to production of the related compound WIN 68577 (2) and rosellichalasin (3). Both 2 and 3 were more active in the rat NK1 than in the human NK1 receptor binding assay, while 1a was more active at the human receptor with an inhibitor affinity constant of 7 microM.
WIN 66306（1a）是一种含有新型氨基酸的环肽，从一种曲霉属菌株中分离得到，标记为SC230，作为一种神经激肽拮抗剂。已开发出使1a产量最大化的条件，同时也导致了相关化合物WIN 68577（2）和罗塞尔拉辛（3）的产生。在大鼠NK1受体结合试验中，2和3的活性均高于人NK1受体，而1a在人受体上活性更高，其抑制剂亲和常数为7微摩尔。
