Todorov D, Paskov D
Eksp Med Morfol. 1973;12(2):100-6.
Tetrazolo-(5,4-a)-6-METHyl-uracil (compound VMI-502) and tetrazolo (5,4-a)-6-propyl-uracil (compound VMI-510) posses a marked sedative-hypnotic and analgesic action and a slightly expressed central skeletal muscles relaxant and anticonvulsant action. The analgesic (antinociceptive) action has been demonstrated by meens of 5 algesimetric methods. The compounds depress the pain reactions in case of stimulation of the superficial as well as of the deep nociceptors, too. Its analgesic action is about 3 times more intense then the action of codeine, about 20 times more intense then the action of amidopyrin and maetamizole, and about 2 times slighter then the action of morphine. The obtained results give the possibility of excluding the so called "false positive reaction". The studied compounds potentiate the analgesic action of the morphine and amidopyrine, applied in subanalgesic dose. It is assumed that by the mechanisme of his analgesic action the compounds VMI-502 and VMI-510 probably approach the non-narcotic analgesics.
四唑并-(5,4-a)-6-甲基尿嘧啶(化合物VMI-502)和四唑并(5,4-a)-6-丙基尿嘧啶(化合物VMI-510)具有显著的镇静催眠和镇痛作用,以及轻微的中枢性骨骼肌松弛和抗惊厥作用。通过5种痛觉测量方法证明了其镇痛(抗伤害感受)作用。这些化合物在刺激浅表和深部伤害感受器时也能抑制疼痛反应。其镇痛作用比可待因的作用强约3倍,比氨基比林和安乃近的作用强约20倍,比吗啡的作用弱约2倍。所获得的结果排除了所谓“假阳性反应”的可能性。所研究的化合物能增强以亚镇痛剂量应用的吗啡和氨基比林的镇痛作用。据推测,就其镇痛作用机制而言,化合物VMI-502和VMI-510可能与非麻醉性镇痛药相近。