Messiha F S
J Appl Toxicol. 1981 Dec;1(6):297-9. doi: 10.1002/jat.2550010605.
The in vitro and in vivo effects of selected pharmacologic agents on cytosolic aldehyde dehydrogenase in the adult rat testicles were studied. Naltrexone, a narcotic antagonist, significantly inhibited epididymal but not testicular aldehyde dehydrogenase in vitro. Greater in vitro inhibition of aldehyde dehydrogenase in the epididymal preparation was determined in the presence of diphenhydramine, a histamine H1-receptor antagonist and by amantadine hydrochloride, an antiviral/antiparkinsonian agent. The latter drug also inhibited testicular aldehyde dehydrogenase from corresponding controls. The in vitro inhibition was noncompetitive as evaluated by reciprocal plots of the velocity of the reaction as a function of substrate concentrations. Short-term oral administration of a biologically active metabolite of flutamide, a nonsteroidal antiandrogen, significantly induced testicular aldehyde dehydrogenase without concomitant changes in epididymal aldehyde dehydrogenase from respective controls. Conversely, administration of ethinylestradiol, an estrogenic steroid, inhibited testicular but not epididymal aldehyde hydrogenase in the rat.
研究了选定药物制剂对成年大鼠睾丸胞质醛脱氢酶的体外和体内作用。纳曲酮是一种麻醉拮抗剂，在体外可显著抑制附睾而非睾丸的醛脱氢酶。组胺H1受体拮抗剂苯海拉明和抗病毒/抗帕金森病药物盐酸金刚烷胺可增强对附睾制剂中醛脱氢酶的体外抑制作用。后一种药物也抑制了相应对照组的睾丸醛脱氢酶。通过反应速度与底物浓度的倒数作图评估，体外抑制作用为非竞争性。短期口服氟他胺（一种非甾体抗雄激素）的生物活性代谢物可显著诱导睾丸醛脱氢酶，而相应对照组的附睾醛脱氢酶无伴随变化。相反，给予雌激素类固醇炔雌醇可抑制大鼠睾丸而非附睾的醛脱氢酶。
