[Reception and extrareceptor binding of cytostatic serotonin antagonists by early embryos of the sea urchin Arbacia lixula].
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.
Buznikov
G A
GA
Zagorevskiĭ
V A
VA
Rakić
L
L
Rogac
L
L
Sharkova
L M
LM
D000818:Animals; D001593:Benzyl Compounds / Q000493:pharmacokinetics / Q000494:pharmacology; D002970:Cleavage Stage, Ovum / Q000187:drug effects / Q000378:metabolism; D007099:Imipramine / Q000493:pharmacokinetics / Q000494:pharmacology; D007211:Indoles / Q000493:pharmacokinetics* / Q000494:pharmacology; D010063:Ovum / Q000187:drug effects / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D012617:Sea Urchins / Q000187:drug effects / Q000196:embryology / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000493:pharmacokinetics* / Q000494:pharmacology
D001593:Benzyl Compounds; D007211:Indoles; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C055071:inmecarb; D007099:Imipramine
Retseptsiia i vneretseptornoe sviazyvanie tsitostaticheskikh antagonistov serotonina rannimi zarodyshami morskogo ezha Arbacia lixula.