Templeton J F, Kumar V P, Bose D, Smyth D D, Kim R S, LaBella F S
Faculty of Pharmacy, University of Manitoba, Winnipeg, Canada.
Can J Physiol Pharmacol. 1988 Nov;66(11):1420-4. doi: 10.1139/y88-231.
The synthesis of the glucoside, 3 beta-[(beta-D-glucopyranosyl)oxy]-14-hydroxy-14 beta-pregn-4-en-20-one, a 14 beta-hydroxyprogesterone glucoside (14 beta-OHP-glu), is described. This compound has an IC50 of 1 microM in a [3H]ouabain binding assay, and is about 10 times more potent than the aglycone. Like 14 beta-hydroxyprogesterone, the glucoside enhances contractility of isolated cardiac muscle. 14 beta-OHP-glu or ouabain, when infused at comparable doses into the renal artery of the anesthetized rat, markedly increases urine volume. Whereas ouabain significantly enhances urinary potassium excretion with little or no effect on sodium excretion, 14 beta-OHP-glu promotes a marked natriuresis with no significant effect on potassium excretion.
本文描述了一种14β-羟基孕酮葡萄糖苷（14β-OHP-glu），即3β-[(β-D-吡喃葡萄糖基)氧基]-14-羟基-14β-孕-4-烯-20-酮葡萄糖苷的合成。该化合物在[3H]哇巴因结合试验中的IC50为1微摩尔，其活性约为苷元的10倍。与14β-羟基孕酮一样，该葡萄糖苷可增强离体心肌的收缩力。当以相当剂量注入麻醉大鼠的肾动脉时，14β-OHP-glu或哇巴因可显著增加尿量。哇巴因可显著增强尿钾排泄，对钠排泄几乎没有影响，而14β-OHP-glu则促进明显的利钠作用，对钾排泄没有显著影响。
