Kozikowski A P, Saiah M K, Bergmann J S, Johnson K M
Trophix Pharmaceuticals, Inc., South Plainfield, New Jersey 07080.
J Med Chem. 1994 Sep 30;37(20):3440-2. doi: 10.1021/jm00046a029.
Six new N-sulfonylated analogs of cocaine have been prepared, and these compounds have been evaluated for their ability to inhibit [3H]mazindol binding and [3H]dopamine uptake into striatal synaptosomes. The N-sulfonyl compounds still inhibited binding and uptake at low micromolar concentrations despite the neutral character of the tropane nitrogen, thus suggesting that the binding of cocaine to the dopamine transporter may not require protonation of its nitrogen and ionic interaction with its recognition site.
已制备出六种新的可卡因N-磺酰化类似物，并对这些化合物抑制[3H]吗吲哚结合以及[3H]多巴胺摄取到纹状体突触体中的能力进行了评估。尽管托烷氮具有中性特征，但N-磺酰化合物在低微摩尔浓度下仍能抑制结合和摄取，这表明可卡因与多巴胺转运体的结合可能不需要其氮的质子化以及与识别位点的离子相互作用。
