A bastadin with potent and selective delta-opioid receptor binding affinity from the Australian sponge Ianthella flabelliformis.
A bastadin with potent and selective delta-opioid receptor binding affinity from the Australian sponge Ianthella flabelliformis.
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来自澳大利亚海绵 Ianthella fllabelliformis 的巴斯塔丁，具有有效和选择性的 δ-阿片受体结合亲和力。
DOI：
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发表时间：
2010
影响因子：
5.1
通讯作者：
R. Quinn
中科院分区：
文献类型：
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作者：
A. Carroll;Sonya M Kaiser;Rohan A. Davis;R. Moni;J. Hooper;R. Quinn
从澳大利亚海绵黄斑Ianthella flabelliformis的MeOH提取物中分离到3个新的basadin 25(1)、15- o - sulfonatbasadin 11(2)和basadin 26(3)。通过一维和二维核磁共振谱和质谱分析确定了它们的结构。Bastadin 26(3)对豚鼠δ阿片受体表现出强亲和力，K(i)值为100 nM。另外两个私生子的亲合力要低100倍。这三种化合物还测试了它们对豚鼠微阿片受体和kappa-阿片受体的亲和力，结果表明它们对这两种阿片受体没有亲和力或只有非常弱的亲和力。
Three new bastadins, bastadin 25 (1), 15-O-sulfonatobastadin 11 (2), and bastadin 26 (3), were isolated from a MeOH extract of the Australian marine sponge Ianthella flabelliformis. Their structures were determined by interpretation of 1D and 2D NMR spectra and mass spectrometry. Bastadin 26 (3) showed potent affinity for the guinea pig delta-opioid receptors with a K(i) value of 100 nM. The other two bastadins had a 100-fold lower affinity. The three compounds were also tested for their affinity to guinea pig micro- and kappa-opioid receptors and shown to have either no affinity or only very weak affinity toward both of these opioid receptors.