CAS: 23509-16-2; [3H]Batrachotoxin

上下游产品

箭毒蛙毒素a Batrachotoxinin A 19457-37-5

📜2,4-Dimethyl-Pyrrole-3-Carboxylic O-Ethyl-Carbonic Anhydride,箭毒蛙毒素a置于sodium Hydroxide体系中,用 氯仿 用作溶剂,化学反应生成箭毒蛙毒素
参考文献:芽孢毒素的结构,一种来自哥伦比亚箭毒蛙的类固醇生物碱,毛状毛虫,以及芽孢毒素及其类似物和同源物的部分合成.
标题:芽孢毒素的结构,一种来自哥伦比亚箭毒蛙的类固醇生物碱,毛状毛虫,以及芽孢毒素及其类似物和同源物的部分合成.
摘要:
Doi:10.1021/ja01042A042

专利信息

专利号:US-3962217-A
优先权日:1969-10-24
标 题 :Process for the manufacture of Δ16 -steroid-14β,18,20-triols and -14β,20-diol-18-ols of the pregnane series
发明人：WEHRLI HANSULI; JEGER OSKAR
权利人:CIBA GEIGY CORP
摘要:The invention is for a selective reduction of the 20- oxo group in Δ 16 -steroid-14β,18-diol-20-ones of the pregnane series to form the two epimeric 20-alcohols having the 20 S and 20 R configuration. The process is especially intended for the manufacture of alkaloids of the batrachotoxin type, particularly for batrachotoxinine A, which is a pregnane derivative having a 20 S alcohol grouping, and epimers and derivatives, such as epi-batrachotixinine A or 7,8-dihydrobatrachotoxinine A. The process is characterized by reducing the said Δ 16 -steroid-14β,18-diol-20-ones in form of their 14,18-ketals, for instance the 14,18 acetonides and using appropriate complex light metal hydrides and operating at appropriate temperatures. The separation of the two isomers is easy and can be effected by the usual physical operations, such as crystallization or chromatography. In the 14β,18,20-triols obtained the 18-hydroxy group can be dehydrogenated to the corresponding 18-aldehydes, which are intermediates necessary in the synthesis of the said pharmacological interesting substances, such as batrachotoxin, by treatment with a sulphoxide in the presence of a carboxylic acid anhydride.

专利号:US-8816095-B2
优先权日:2008-08-15
标题:Na channels, disease, and related assays and compositions
发明人：BROWN MILTON L; GRINDROD SCOTT; WALLS THOMAS H; HANSEN TODD; SUY SIMENG; PAIGE MIKELL A
权利人:BROWN MILTON L; GRINDROD SCOTT; WALLS THOMAS H; HANSEN TODD; SUY SIMENG; PAIGE MIKELL A; UNIV GEORGETOWN
摘要:Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [ 3 H]-Batrachotoxin-B ([ 3 H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.