[The effect of antihistaminic preparations on the binding of labelled mepyramine, ketanserin and quinuclidinyl benzilate in the rat brain].
The effects of some antiallergic drugs on H1-histamine, 5-HT2-serotonin, and M-cholinoreceptors ligand binding in the rat brain were studied in vitro. Dimedrol, dimebon, and phencarol bonded to H1-receptors: IC50 were 76 +/- 10, 153 +/- 15, 320 +/- 60 nM, respectively. Diazoline and dimebon had some affinity for 5-HT2-receptors, its IC50 was 880 +/- 90 nM. Dimedrol, phencarol and diazoline were found to be active against M-cholinoceptors, but when given in the maximal concentration (10 microM) it acted nonspecifically. In contrast to the other drugs, bicarphen had no effects on the binding of [3H]-mepyramine, [3H]-ketanserine, and [3H]-quinuclidinyl benzylate in the rat brain.
Gankina
E M
EM
Porodenko
N V
NV
Kondratenko
T I
TI
Severin
E S
ES
Kaminka
M E
ME
Mashkovskiĭ
M D
MD
D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D004347:Drug Interactions; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D007650:Ketanserin / Q000493:pharmacokinetics*; D008024:Ligands; D008297:Male; D011738:Pyrilamine / Q000493:pharmacokinetics*; D011813:Quinuclidinyl Benzilate / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011969:Receptors, Histamine H1 / Q000187:drug effects / Q000378:metabolism; D011970:Receptors, Histamine H2 / Q000187:drug effects / Q000378:metabolism; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000378:metabolism; D014316:Tritium
D006634:Histamine H1 Antagonists; D006635:Histamine H2 Antagonists; D008024:Ligands; D011969:Receptors, Histamine H1; D011970:Receptors, Histamine H2; D011976:Receptors, Muscarinic; D014316:Tritium; D011813:Quinuclidinyl Benzilate; D007650:Ketanserin; D011738:Pyrilamine
Vliianie antigistaminnykh preparatov na sviazyvanie mechennykh mepiramina, ketanserina i khinuklidinilbenzilata v mozge krysy.