Özdemir Ahmet, Altıntop Mehlika Dilek, Kaplancıklı Zafer Asım, Can Özgür Devrim, Demir Özkay Ümide, Turan-Zitouni Gülhan
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
Graduate School of Health Sciences, Anadolu University, 26470 Eskişehir, Turkey.
Molecules. 2015 Feb 4;20(2):2668-84. doi: 10.3390/molecules20022668.
In an effort to develop potent antidepressant agents, new pyrazoline derivatives 2a-s were synthesized and evaluated for their antidepressant-like activity by tail suspension test (TST) and modified forced swimming test (MFST). The effects of the compounds on spontaneous locomotor activity were also investigated using an activity cage apparatus. Among these derivatives, compounds 2b, 2d, 2f, 2o, and 2r decreased both horizontal and vertical activity number of the mice. On the other hand, compounds 2a, 2h, 2j, 2k, 2l, 2m, and 2n, which did not induce any significant change in the locomotor activity, significantly shortened the immobility time of mice in TST and MFST, representing the presence of the antidepressant-like effect. Additionally, the same compounds increased the swimming time of mice in MFST without any change in climbing duration, similar to the reference drug fluoxetine (10 mg/kg). In the light of previous papers examining the effects of pyrazolines on central nervous system, this study, once more, pointed out remarkable antidepressant activity potential of pyrazoline derivatives.
为了开发强效抗抑郁药，合成了新型吡唑啉衍生物2a - s，并通过悬尾试验（TST）和改良强迫游泳试验（MFST）评估其抗抑郁样活性。还使用活动笼装置研究了这些化合物对自发运动活性的影响。在这些衍生物中，化合物2b、2d、2f、2o和2r降低了小鼠的水平和垂直活动次数。另一方面，化合物2a、2h、2j、2k、2l、2m和2n在运动活性上未引起任何显著变化，但显著缩短了小鼠在TST和MFST中的不动时间，表明存在抗抑郁样效应。此外，与参比药物氟西汀（10 mg/kg）类似，相同的化合物增加了小鼠在MFST中的游泳时间，而攀爬持续时间没有任何变化。鉴于先前研究吡唑啉对中枢神经系统影响的论文，本研究再次指出了吡唑啉衍生物具有显著的抗抑郁活性潜力。
