Pinelli A, Trivulzio S, Malvezzi L, Rossoni G, Berti F
Department of Pharmacology, Chemotherapy and Medical Toxicology, University of Milan, Italy.
Arzneimittelforschung. 1989 Mar;39(3):361-5.
Administration of 6-aminoindazole (6-AIN) and 5-aminoindazole (5-AIN) to rats depressed gastric acid secretion, both basal and carbachol-stimulated. 6-AIN proved to be more active than 5-AIN in decreasing the stimulated secretory process. The antisecretory activity of 6-AIN appears to be partially an antihistamine effect, since this compound antagonized the stimulatory action of betazole on isolated guinea pig auricle. The antisecretory activity of 6-AIN is probably associated with an antimuscarinic effect, since the molecule decreased carbachol-stimulated gastric acid secretion in rats and depressed neostigmine-stimulated motility of duodenum and colon in the anaesthetized cat. It also lessened the hypertonus of isolated guinea-pig trachea caused by pilocarpine. The antisecretory effects of 6-AIN also appear to be associated with myolytic activity, since it decreased the spontaneous motility of duodenum and colon in anaesthetized cats and the spontaneous myoactivity of isolated jejunum of the rabbit. It depressed the contractions of isolated guinea-pig ileum caused by histamine and decreased the spasmogenic effects of barium chloride on isolated guinea-pig gall bladder. These results suggest that 6-AIN probably depresses gastric acid secretion by interfering with both histamine and acetylcholine receptors and with other receptors involved in the secretory process.
给大鼠注射6-氨基吲唑（6-AIN）和5-氨基吲唑（5-AIN）可抑制胃酸分泌，包括基础胃酸分泌和卡巴胆碱刺激的胃酸分泌。在降低刺激的分泌过程方面，6-AIN比5-AIN更具活性。6-AIN的抗分泌活性似乎部分是一种抗组胺作用，因为该化合物可拮抗倍他唑对离体豚鼠耳廓的刺激作用。6-AIN的抗分泌活性可能与抗毒蕈碱作用有关，因为该分子可降低大鼠中卡巴胆碱刺激的胃酸分泌，并抑制麻醉猫中新斯的明刺激的十二指肠和结肠运动。它还减轻了毛果芸香碱引起的离体豚鼠气管的高张力。6-AIN的抗分泌作用似乎还与溶肌活性有关，因为它降低了麻醉猫中十二指肠和结肠的自发运动以及兔离体空肠的自发肌活性。它抑制了组胺引起的离体豚鼠回肠的收缩，并降低了氯化钡对离体豚鼠胆囊的致痉挛作用。这些结果表明，6-AIN可能通过干扰组胺和乙酰胆碱受体以及参与分泌过程的其他受体来抑制胃酸分泌。
