Perrot D, Pugeat M, Bonneton A, Mounier-Kuhn A, Motin J, Forest M G
Eur J Clin Pharmacol. 1985;29(2):181-5. doi: 10.1007/BF00547419.
The binding affinities of two steroid anaesthetics, alphaxalone (Alfx) and alphadolone acetate (Alfd), for testosterone-oestradiol-binding globulin (TeBG) and corticosteroid-binding globulin (CBG) were measured in human serum. In 8 male patients, the effect of i.v. administration of Althesin (a mixture of Alfx and Alfd) on the transport of testosterone (T) and cortisol (F) was studied. Both Alfx and Alfd bind to TeBG and CBG with a relatively high affinity (10(6)M-1). A significant change in the percentage of unbound T was observed during Althesin infusion, with no change in total T concentration or in the TeBG binding parameters. The results suggest that by interaction with TeBG binding sites Alfx and/or Alfd displaced T bound to TeBG, and transiently increased the percentage of unbound T. A significant increase in the concentration of F was observed during althesin infusion, while the percentage of unbound F and the CBG binding parameters were unchanged. The dose of Alfx and Alfd used was not sufficient to alter the transport of F during brief althesin anaesthesia in men.
在人血清中测量了两种甾体麻醉剂α-羟孕酮（Alfx）和醋酸α-孕甾二酮（Alfd）与睾酮-雌二醇结合球蛋白（TeBG）和皮质类固醇结合球蛋白（CBG）的结合亲和力。在8名男性患者中，研究了静脉注射Althesin（Alfx和Alfd的混合物）对睾酮（T）和皮质醇（F）转运的影响。Alfx和Alfd均以相对较高的亲和力（10⁶M⁻¹）与TeBG和CBG结合。在输注Althesin期间观察到未结合T的百分比有显著变化，而总T浓度或TeBG结合参数没有变化。结果表明，通过与TeBG结合位点相互作用，Alfx和/或Alfd取代了与TeBG结合的T，并短暂增加了未结合T的百分比。在输注Althesin期间观察到F浓度显著增加，而未结合F的百分比和CBG结合参数没有变化。在男性短暂的Althesin麻醉期间，所用的Alfx和Alfd剂量不足以改变F的转运。
