Jacob P, Shulgin A T
J Med Chem. 1983 May;26(5):746-52. doi: 10.1021/jm00359a021.
The two thio analogues of each of the well-known psychotomimetic drugs DOM [(2,5-dimethoxy-4-methylphenyl)isopropylamine] and DOET [(2,5-dimethoxy-4-ethylphenyl)isopropylamine] have been synthesized and pharmacologically evaluated in man. The 5-thio isomers are more potent as psychotomimetic agents than the 2-thio isomers but still represent a drop of an order of magnitude in potency from the sulfur-free counterparts. The dithio analogue of DOM was synthesized and found to be without central activity at a dosage of approximately 50 times the mean effective dose of DOM.
已合成了两种著名的拟精神病药物DOM[(2,5-二甲氧基-4-甲基苯基)异丙胺]和DOET[(2,5-二甲氧基-4-乙基苯基)异丙胺]各自的硫代类似物,并在人体上进行了药理学评估。5-硫代异构体作为拟精神病药物比2-硫代异构体更有效,但与无硫对应物相比,其效力仍下降了一个数量级。合成了DOM的二硫代类似物,发现其在剂量约为DOM平均有效剂量的50倍时无中枢活性。