Taché Y, Taché J, Selye H
Arzneimittelforschung. 1975 Oct;25(10):1603-6.
In rats, the sleeping time induced by overdosage with eight steroid anesthetics--alfathesin, 3-(3-oxo-17beta-hydroxy-19-nor-4-androsten-17alpha-yl)-propionic acid-lactone (SC-8109), 21-hydroxy=5alpha-pregnane-3,20-dione (P-234), 4-pregnene-3,11,20-trione (Bio.66), 17-hydroxy-3-oxo-4-androstene-17alpha-propionic acid-gamma-lactone(SC-5233),3alpha-hydroxy-5beta-pregnane-11,20-dione, 5beta-pregnane-3,11,20-trione (U-1373), and hydroxydione--was abolished or considerably reduced by a variety of catatoxic compounds, particularly 3beta-hydroxy-20-oxo-5-pregnene-16alpha-carbonitrile (PCN), 9alpha-fluoro-11beta,17-dihydroxy-3-oxo-4-androstene-17alpha-propionic acid potassium salt (CS-1), prednisolone, ethylestrenol and spironolactone. Phenobarbital and diphenylhydantoin, two non-steroidal stimulators of hepatic microsomal drug metabolism, were also highly effective. In contrast, triamcinolone, estradiol,progesterone, desoxycorticosterone and hydroxydione, which exert little or no catatoxic activity, failed to significantly diminish anesthesia or sedation.
在大鼠中，多种具有抗麻醉毒性的化合物，特别是3β-羟基-20-氧代-5-孕烯-16α-腈（PCN）、9α-氟-11β,17-二羟基-3-氧代-4-雄烯-17α-丙酸钾盐（CS-1）、泼尼松龙、乙基去甲睾酮和螺内酯，可消除或显著缩短由八种甾体麻醉剂——阿法西辛、3-(3-氧代-17β-羟基-19-去甲-4-雄烯-17α-基)-丙酸内酯（SC-8109）、21-羟基-5α-孕烷-3,20-二酮（P-234）、4-孕烯-3,11,20-三酮（Bio.66）、17-羟基-3-氧代-4-雄烯-17α-丙酸-γ-内酯（SC-5233）、3α-羟基-5β-孕烷-11,20-二酮、5β-孕烷-3,11,20-三酮（U-1373）和羟二酮——过量给药所诱导的睡眠时间。两种非甾体类肝微粒体药物代谢刺激剂苯巴比妥和苯妥英钠也非常有效。相比之下，几乎没有或没有抗麻醉毒性活性的曲安西龙、雌二醇、孕酮、脱氧皮质酮和羟二酮未能显著减轻麻醉或镇静作用。
