Pong S F, Pelosi S S, Wessels F L, Yu C N, Burns R H, White R E, Anthony D R, Ellis K O, Wright G C, White R L
Arzneimittelforschung. 1983;33(10):1411-6.
A series of 5-phenyl-2-furamidines has been synthesized and evaluated for antidepressant activities. Substitution in the phenyl ring with a nitro (4) or an amino (12) group in the ortho-position resulted in an increase in antidepressant activity. Both 4 and 12 antagonized tetrabenazine-induced ptosis in rodents and inhibited norepinephrine (noradrenaline) uptake into crude synaptosomes of whole mouse brain at doses or concentrations comparable to those of the tricyclic antidepressants. However, these compounds did not possess the anticholinergic and antihistaminic activities common to tricyclic antidepressants. In addition, they lacked monoamine oxidase inhibitory activity. The 5-phenyl-2-furamidines represent a new chemical class of antidepressants and may be useful for depressive patients who cannot tolerate the compromising side effects of the tricyclic antidepressants and monoamine oxidase inhibitors.
已合成了一系列5-苯基-2-呋喃脒，并对其抗抑郁活性进行了评估。苯环邻位被硝基（4）或氨基（12）取代后，抗抑郁活性增强。化合物4和12在啮齿动物中均能拮抗丁苯那嗪诱导的眼睑下垂，且在与三环类抗抑郁药相当的剂量或浓度下，能抑制去甲肾上腺素（NA）摄取到全小鼠脑的粗突触体中。然而，这些化合物不具有三环类抗抑郁药常见的抗胆碱能和抗组胺活性。此外，它们缺乏单胺氧化酶抑制活性。5-苯基-2-呋喃脒代表了一类新型抗抑郁化学物质，可能对无法耐受三环类抗抑郁药和单胺氧化酶抑制剂副作用的抑郁症患者有用。
