Whitton P S, Sarna G S, O'Connell M T, Curzon G
Department of Neurochemistry, Institute of Neurology, London, U.K.
Neuropharmacology. 1991 Jan;30(1):1-4. doi: 10.1016/0028-3908(91)90035-a.
Tianeptine is a novel tricyclic antidepressant which, in marked contrast to other antidepressants, increases the uptake of 5-HT in brain tissue and blood platelet preparations ex vivo. In the present study it was shown, by microdialysis, that tianeptine (10 mg/kg i.p.), whether given as a single dose or as daily doses for 14 days, attenuated the K(+)-evoked rise of extracellular 5-HT in the hippocampus in vivo. Tianeptine (10 mg/kg i.p.), given acutely, did not reduce basal levels of 5-HT in hippocampal dialysates in the presence of the 5-HT reuptake inhibitor, citalopram. These results suggest mutually opposing effects of tianeptine and citalopram on neuronal uptake of 5-HT. Their significance in relation to the role of 5-HT in the action of antidepressants is discussed.
噻奈普汀是一种新型三环类抗抑郁药,与其他抗抑郁药形成显著对比的是,它能在体外增加脑组织和血小板制剂中5-羟色胺(5-HT)的摄取。在本研究中,通过微透析表明,噻奈普汀(腹腔注射10毫克/千克),无论是单次给药还是连续14天每日给药,均可在体内减弱海马体中钾离子(K(+))诱发的细胞外5-HT升高。急性给予噻奈普汀(腹腔注射10毫克/千克),在存在5-HT再摄取抑制剂西酞普兰的情况下,并未降低海马体透析液中5-HT的基础水平。这些结果表明噻奈普汀和西酞普兰对神经元摄取5-HT具有相互对立的作用。文中讨论了它们与5-HT在抗抑郁药作用中的作用的相关性。