伊辛内酰胺：来自澳大利亚伊辛尼科科海绵的亚基选择性甘氨酸受体调节剂。
Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae.
机构信息
Institute for Molecular Bioscience, The University of Queensland, St. Lucia, QLD 4072, Australia.
出版信息
Bioorg Med Chem. 2010 Apr 15;18(8):2912-9. doi: 10.1016/j.bmc.2010.03.002. Epub 2010 Mar 6.
Screening an extract library of >2500 southern Australian and Antarctic marine invertebrates and algae for modulators of glycine receptor (GlyR) chloride channels identified three Irciniidae sponges that yielded new examples of a rare class of glycinyl lactam sesterterpene, ircinialactam A, 8-hydroxyircinialactam A, 8-hydroxyircinialactam B, ircinialactam C, ent-ircinialactam C and ircinialactam D. Structure-activity relationship (SAR) investigations revealed a new pharmacophore with potent and subunit selective modulatory properties against alpha1 and alpha3 GlyR isoforms. Such GlyR modulators have potential application as pharmacological tools, and as leads for the development of GlyR targeting therapeutics to treat chronic inflammatory pain, epilepsy, spasticity and hyperekplexia.
从超过 2500 种南澳大利亚和南极海洋无脊椎动物和藻类的提取物文库中筛选甘氨酸受体（GlyR）氯离子通道调节剂，发现了三种 Irciniidae 海绵，它们产生了一种罕见的甘氨酰内酰胺甾体萜烯类的新实例，即 ircinialactam A、8-羟基 ircinialactam A、8-羟基 ircinialactam B、ircinialactam C、ent-ircinialactam C 和 ircinialactam D。结构-活性关系（SAR）研究揭示了一种新的药效团，对 alpha1 和 alpha3 GlyR 同工型具有强效和亚基选择性的调节作用。这种 GlyR 调节剂具有作为药理学工具的潜在应用，以及作为开发靶向 GlyR 的治疗药物的先导，以治疗慢性炎症性疼痛、癫痫、痉挛和高张力。
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