[4-[Benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds with selective antagonistic activity against H1-histamine receptors].
This paper describes the synthesis of 2- and 4-[benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds and their antihistaminic properties studied on isolated guinea-pig ileum. Calculated pA2 values show that the antihistaminic activity of 4-[p.methoxybenzyl-(2-dimethylaminoethyl)amino]pyrimidine is specific and potent (8-10 times higher than that of thonzylamine).
D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis*; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology
D006634:Histamine H1 Antagonists; D011743:Pyrimidines; D000109:Acetylcholine
Composti 4-[benzil-(2-dimetilaminoetil)amino]-pirimidinici antagonisti selettivi dei recettori H1-istaminici.