[Antihistamine and antiserotonin action of 2 aminotetralin derivatives].
The authors performs studies under the conditions of whole organism in vivo and on isolatid organs in vitro and examined antihistamine and antiserotonine activity of two derivatives of 2-aminotetraline, synthesized by D. Dancev and Iv. Ivanov, namely: N-(trans-e-hydroxy-1, 2, 3, 4-tetrahydro-2-naphtyl (-N-) 3-oxo-3-phenylpropyl) piperasine dichloride and N-(trans-3-hydroxy-1, 2, 3, 4-tetrahydro-2-naphtyl (-N-) 3-oxo-3-3phenyl-2-methylpropyl (piperasine dichloride) indicated respectively as P10 and P11. The experiments on isolated ileum of a guinea pig showed that the compound P11 (in concentration of 1.10(-7), 1.10(-6), and 1.10(-5) gm/ml) and P11 (in concentration of 1.10(-6) and 1.10(-5) gm/ml) inhibited the spasomogenic effect of histamine (1.10(-8) and 1.10(-7) gm/ml) as better antihistaminev effect revealed P10. Both compounds inconcentrations of 1.10(-6) and 1.10(-5) gm/ml inhibited the spasmogenic effect of serotonine (1.10(-7) gm/ml), as more significant changes occurred under the influence of the compound P11. The compound P10, administered subcutaneously in a guinea pig in a dose of 0.5 mg/kg of body weight 30 minutes before the occurrence of histamine shock, prevented its development. The same compound inhibited also the development of enterocolitis in mice, induced by serotonine (in a dose of 1 mg/kg of body weight). Both examined compounds inhibited the development of serotonine oedema of the hind paw of a rat as better effect showed the compound P11. The established facts are discussed.
D015081:2-Naphthylamine / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D004487:Edema / Q000139:chemically induced; D006168:Guinea Pigs; D006632:Histamine / Q000008:administration & dosage; D006634:Histamine H1 Antagonists; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D051379:Mice; D009281:Naphthalenes / Q000494:pharmacology*; D012701:Serotonin / Q000008:administration & dosage; D012702:Serotonin Antagonists; D012769:Shock / Q000139:chemically induced; D013035:Spasm / Q000139:chemically induced; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*
D006634:Histamine H1 Antagonists; D009281:Naphthalenes; D012702:Serotonin Antagonists; D013764:Tetrahydronaphthalenes; D012701:Serotonin; D006632:Histamine; D015081:2-Naphthylamine
Vurkhu antikhistaminovoto i antiserotoninovoto deĭstvie na dve proizvodni na 2-aminotetralina.