Beaven M A, Shaff R E
Agents Actions. 1979 Dec;9(5-6):455-60. doi: 10.1007/BF01968110.
The Dimaprit analog, S-[4-(N,N-dimethylamino)-butyl]isothiurea (SKF Compound 91488), which is a noncompetitive inhibitor (Ki, 0.9 microM) of histamine-N-methyltransferase in vitro, inhibited the methylation of labeled histamine in mice. When administered in combination with the diamine oxidase inhibitor, aminoguanidine, an almost complete block of histamine metabolism was observed. The inhibition was dependent on dose of drug and was apparent with doses of 50 mg/kg and greater. Since Compound 91488 is reported to have no agonist activity of its own, the drug may help to identify the actions of histamine released from endogenous stores in response to physiological and pathological stimuli.
地马普明类似物S-[4-(N,N-二甲基氨基)-丁基]异硫脲（SKF化合物91488）在体外是组胺-N-甲基转移酶的非竞争性抑制剂（Ki，0.9微摩尔），它能抑制小鼠体内标记组胺的甲基化。当与二胺氧化酶抑制剂氨基胍联合给药时，观察到组胺代谢几乎完全受阻。这种抑制作用取决于药物剂量，50毫克/千克及以上剂量时作用明显。由于据报道化合物91488自身没有激动剂活性，该药物可能有助于确定内源性储存的组胺在生理和病理刺激下释放后的作用。
