Johansson A M, Nilsson J L, Karlén A, Hacksell U, Sanchez D, Svensson K, Hjorth S, Carlsson A, Sundell S, Kenne L
Department of Organic Pharmaceutical Chemistry, Biomedical Center, University of Uppsala, Sweden.
J Med Chem. 1987 Oct;30(10):1827-37. doi: 10.1021/jm00393a025.
C1- and C3-methyl-substituted derivatives of the potent dopamine (DA) receptor agonist 7-hydroxy-2-(di-n-propylamino)tetralin (7-OH-DPAT) have been synthesized, and their conformational preferences have been studied by use of NMR spectroscopy, X-ray crystallography, and molecular mechanics (MMP2) calculations. The compounds were tested for activity at central DA receptors, by use of biochemical and behavioral tests in rats. (1S,2R)-7-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin [(+)-10] was demonstrated to be sevenfold less potent than (2R)-7-OH-DPAT as a DA receptor agonist. The other new compounds were of lower potency or inactive.
强效多巴胺（DA）受体激动剂7-羟基-2-（二正丙基氨基）四氢萘（7-OH-DPAT）的C1-和C3-甲基取代衍生物已被合成，并通过核磁共振光谱、X射线晶体学和分子力学（MMP2）计算研究了它们的构象偏好。通过对大鼠进行生化和行为测试，检测了这些化合物对中枢DA受体的活性。（1S，2R）-7-羟基-1-甲基-2-（二正丙基氨基）四氢萘[（+）-10]作为DA受体激动剂的效力比（2R）-7-OH-DPAT低七倍。其他新化合物效力较低或无活性。
