Girard Y, Atkinson J G, Haubrich D R, Williams M, Yarbrough G G
J Med Chem. 1982 Feb;25(2):113-6. doi: 10.1021/jm00344a004.
A series of 6- and 8-(aminomethyl)-4H-1,2,4-benzothiadiazine 1,1-dioxides has been synthesized and tested for interaction with various GABA systems. None of the compounds showed significant GABA-mimetic properties, but unexpectedly, compound 7 [6-(aminomethyl)-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide] possessed the properties of a selective antagonist of taurine, as measured by the antagonism of taurine-induced inhibition of rat cerebellar Purkinje firing.
已经合成了一系列6-和8-（氨甲基）-4H-1,2,4-苯并噻二嗪1,1-二氧化物，并测试了它们与各种GABA系统的相互作用。这些化合物均未表现出显著的拟GABA特性，但出乎意料的是，化合物7 [6-（氨甲基）-3-甲基-4H-1,2,4-苯并噻二嗪1,1-二氧化物]具有牛磺酸选择性拮抗剂的特性，这是通过其对牛磺酸诱导的大鼠小脑浦肯野细胞放电抑制的拮抗作用来测定的。
