Yakovleva T V, Nikitina L A, Korobov N V, Vinogradov V A, Titov M I
Biochem Biophys Res Commun. 1983 Dec 28;117(3):718-24. doi: 10.1016/0006-291x(83)91656-x.
Binding sites with high affinity for [3H]naloxone, but not for [3H]morphine and [3H] (D-Ala2, D-Leu5) enkephalin, have been found in membranes of Bufo viridis oocytes. The binding is reversible and saturable. Bound [3H]naloxone is easily displaced both by unlabeled naloxone and bremazocine, much worse by morphine and SKF 10,047; (D-Ala2, D-Leu5) enkephalin and beta-endorphin practically fail to displace [3H]naloxone. Scatchard analysis is consistent with the existence of two classes of binding sites with Kd 15 nM and 10(3) nM. The number of binding sites with high affinity for naloxone is 16 pmol/mg protein of homogenized oocytes which is 20-50-fold higher than in, toad or rat brain. Oocyte extract displaces [3H]naloxone bound with oocytes' membranes and inhibits electrically evoked contractions of the rabbit vas deferens. This inhibition is reversed by naloxone. It is suggested that compounds similar to opiate kappa-agonists exist in oocytes. It cannot be ruled out that they participate via specific receptors in the regulation of oocyte maturation and egg development.
在绿蟾蜍卵母细胞膜中发现了对[3H]纳洛酮具有高亲和力的结合位点,但对[3H]吗啡和[3H](D - Ala2,D - Leu5)脑啡肽没有高亲和力。这种结合是可逆的且具有饱和性。结合的[3H]纳洛酮很容易被未标记的纳洛酮和布马佐辛取代,被吗啡和SKF 10,047取代的程度要差得多;(D - Ala2,D - Leu5)脑啡肽和β - 内啡肽实际上无法取代[3H]纳洛酮。Scatchard分析与存在两类结合位点一致,其解离常数(Kd)分别为15 nM和10³ nM。对纳洛酮具有高亲和力的结合位点数量为16 pmol/mg匀浆卵母细胞蛋白,这比蟾蜍或大鼠脑内的数量高20 - 50倍。卵母细胞提取物能取代与卵母细胞膜结合的[3H]纳洛酮,并抑制兔输精管的电诱发收缩。这种抑制作用可被纳洛酮逆转。提示卵母细胞中存在类似于阿片κ - 激动剂的化合物。不能排除它们通过特异性受体参与卵母细胞成熟和卵子发育的调节。