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[2-氨基四氢萘衍生物的抗组胺和抗血清素作用]

[Antihistamine and antiserotonin action of 2 aminotetralin derivatives].

作者信息

Staneva-Stoĭcheva D, Chakurova L, Raĭnova L, Ilarĭonov I

出版信息

Eksp Med Morfol. 1979;18(3):154-9.

PMID:40787
Abstract

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.

摘要

作者在整体动物体内和离体器官体外条件下进行研究,检测了由D. Dancev和Iv. Ivanov合成的2-氨基四氢萘两种衍生物的抗组胺和抗血清素活性,即:N-(反式-e-羟基-1,2,3,4-四氢-2-萘基(-N-)3-氧代-3-苯基丙基)哌嗪二氯化物和N-(反式-3-羟基-1,2,3,4-四氢-2-萘基(-N-)3-氧代-3-3苯基-2-甲基丙基(哌嗪二氯化物),分别表示为P10和P11。豚鼠离体回肠实验表明,化合物P11(浓度为1.10(-7)、1.10(-6)和1.10(-5)克/毫升)和P10(浓度为1.10(-6)和1.10(-5)克/毫升)抑制组胺(1.10(-8)和1.10(-7)克/毫升)的致痉挛作用,P10显示出更好的抗组胺作用。两种化合物浓度为1.10(-6)和1.10(-5)克/毫升时抑制血清素(1.10(-7)克/毫升)的致痉挛作用,在化合物P11影响下变化更显著。在组胺休克发生前30分钟,以0.5毫克/千克体重的剂量给豚鼠皮下注射化合物P10,可预防其发生。同一化合物还抑制血清素(剂量为1毫克/千克体重)诱导的小鼠小肠结肠炎的发展。两种受试化合物均抑制大鼠后爪血清素性水肿的发展,化合物P11显示出更好的效果。对已确定的事实进行了讨论。

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