Buznikov G A, Zagorevskiĭ V A, Rakić L, Rogac L, Sharkova L M
Zh Evol Biokhim Fiziol. 1988 Sep-Oct;24(5):611-20.
Unfertilized eggs and early embryos of the sea urchin Arbacia lixula incubated for 60 min in a medium containing the antagonists of prenervous serotonin, i.e. inmecarb (21 microM) or imipramine (40 microM), bind up to 5 microM of these drugs per 1 ml of cells. At high cell concentrations (more than 10,000 eggs or embryos per 1 ml), this binding is not followed by inhibition of cleavage divisions or by increase in the sensitivity to cytostatic effects of these drugs, which is taken as an indication that this binding is a nonreceptive one. The decrease in concentration of eggs or embryos does not affect total binding of the drugs, although their antiserotonin effects become evident indicating the existence of the receptor sites of binding. In experiments with 3H-imipramine, two binding pools were found (Bmax being correspondingly equal to about 20 and 0.75 microM/ml of embryos; the values of Kd amount to 200 and 15 microM). One of them is a nonreceptive pool, whereas the other presumably coincides with receptor binding sites of prenervous serotonin antagonists.
将海胆光棘球海胆的未受精卵和早期胚胎在含有神经前血清素拮抗剂的培养基中孵育60分钟,即因灭卡(21微摩尔)或丙咪嗪(40微摩尔),每1毫升细胞可结合高达5微摩尔的这些药物。在高细胞浓度下(每1毫升超过10,000个卵或胚胎),这种结合之后不会出现卵裂抑制或对这些药物细胞毒性作用敏感性增加的情况,这表明这种结合是无受体的。卵或胚胎浓度的降低并不影响药物的总结合量,尽管它们的抗血清素作用变得明显,表明存在结合的受体位点。在用3H-丙咪嗪进行的实验中,发现了两个结合池(Bmax分别约等于20和0.75微摩尔/毫升胚胎;Kd值分别为200和15微摩尔)。其中一个是无受体池,而另一个可能与神经前血清素拮抗剂的受体结合位点一致。