Rohrer S P, Evans D V
Department of Biochemical Parasitology, Merck Sharp and Dohme Research Laboratories, Rahway, New Jersey 07065.
Vet Res Commun. 1990;14(2):157-65. doi: 10.1007/BF00346556.
Two types of experiments were performed in an effort to demonstrate a role for plasma proteins in determining the amount of ivermectin available for transport across the blood-brain barrier of collie dogs sensitive to the effects of the compound. The solubility of ivermectin in plasma from non-sensitive and sensitive collies was measured and found to be identical at 100 micrograms/ml. An assay for measuring the low affinity binding interaction of ivermectin with plasma components was developed. The amount of ivermectin bound per unit of plasma was the same for samples from sensitive and non-sensitive dogs. Dog serum albumin and the high density lipoprotein portion of the plasma were both capable of binding ivermectin. No differences in the binding characteristics of ivermectin in plasma from ivermectin sensitive and non-sensitive collies were found.
为了证明血浆蛋白在决定伊维菌素通过对该化合物敏感的柯利犬血脑屏障进行转运的可用量方面所起的作用,进行了两种类型的实验。测量了伊维菌素在非敏感和敏感柯利犬血浆中的溶解度,发现其在100微克/毫升时相同。开发了一种用于测量伊维菌素与血浆成分低亲和力结合相互作用的测定方法。来自敏感和非敏感犬的样本中,每单位血浆结合的伊维菌素量相同。犬血清白蛋白和血浆中的高密度脂蛋白部分都能够结合伊维菌素。未发现伊维菌素敏感和非敏感柯利犬血浆中伊维菌素结合特性的差异。