First pharmacophoric hypothesis for 5-HT 7 antagonism
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چکیده
منابع مشابه
The rapid recovery of 5-HT cell firing induced by the antidepressant vortioxetine involves 5-HT(3) receptor antagonism.
The therapeutic effect of current antidepressant drugs appears after several weeks of treatment and a significant number of patients do not respond to treatment. Here, we report the effects of the multi-modal antidepressant vortioxetine (Lu AA21004), a 5-HT(3) and 5-HT(7) receptor antagonist, 5-HT(1B) receptor partial agonist, 5-HT(1A) receptor agonist and 5-HT transporter (SERT) inhibitor, on ...
متن کاملSerotonin (5-HT)3-receptor antagonism of 4,5,6,7-tetrahydrobenzimidazole derivatives against 5-HT-induced bradycardia in anesthetized rats.
We investigated the mode of the 5-HT3-receptor antagonism of 4,5,6,7-tetrahydrobenzimidazole derivatives, YM060, YM114 (KAE-393), YM-26103-2 and YM-26308-2, against 5-HT-induced transient bradycardia in anesthetized rats. Results were compared with those of ondansetron and granisetron. YM060 (0.03-0.1 microgram/kg, i.v.), YM114 (0.03-0.3 microgram/kg, i.v.), YM-26103-2 (0.01-0.03 microgram/kg, ...
متن کاملviewpoint 5 - HT and motor control : a hypothesis
The activity of 5-HT-containing neurons in the brain is activated preferentially m association with motor output in cats. This is especially apparent during changes in muscle tone and during responses mediated by central pattern generators, such as chewing, locomotion and respiration. These and other data support the hypothesis that the primary functions of the 5-HT system in the brain are to f...
متن کاملComparison of 4 radiolabeled antagonists for serotonin 5-HT(7) receptor neuroimaging: toward the first PET radiotracer.
UNLABELLED Brain serotonin 7 (5-hydroxytryptamine 7, or 5-HT(7)) is the most recently identified serotonin receptor. It is involved in mood disorders and is studied as a target for antidepressants. Because no radioligand has yet been successfully used to study this receptor by PET neuroimaging, the objective of the present study was to develop a 5-HT(7) (18)F-labeled radiotracer. METHODS Four...
متن کاملEffects of serotonin (5-hydroxytryptamine, 5-HT) reuptake inhibition plus 5-HT(2A) receptor antagonism on the firing activity of norepinephrine neurons.
YM992 [(S)-2-[[(7-fluoro-4-indanyl)oxy]methyl]morpholine monohydrochloride] is a selective serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitor (SSRI) and a potent 5-HT(2A) antagonist. The aim of the present study was to assess, using in vivo extracellular unitary recordings, the effect of acute and sustained administration of YM992 (40 mg kg(-1) day(-1) s.c., using osmotic minipumps) on th...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2000
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(00)00166-9