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Novel 5-HT7R antagonists, arylsulfonamide derivatives of (aryloxy)propyl piperidines: Add-on effect to the antidepressant activity of SSRI and DRI, and pro-cognitive profile.

Abstract：

:A novel series of arylsulfonamide derivatives of (aryloxy)propyl piperidines was designed to obtain potent 5-HT7R antagonists. Among the compounds evaluated herein, 3-chloro-N-{1-[3-(1,1-biphenyl-2-yloxy)2-hydroxypropyl]piperidin-4-yl}benzenesulfonamide (25) exhibited antagonistic properties at 5-HT7R and showed selectivity over selected serotoninergic and dopaminergic receptors, as well as over serotonin, noradrenaline and dopamine transporters. Compound 25 demonstrated significant antidepressant-like activity in the forced swim test (0.625-2.5mg/kg, i.p.) and in the tail suspension test (1.25mg/kg, i.p.), augmented the antidepressant effect of inactive doses of escitalopram (selective serotonin reuptake inhibitor) and bupropion (dopamine reuptake inhibitor) in the FST in mice, and similarly to SB-269970, exerted pro-cognitive properties in the novel object recognition task in cognitively unimpaired conditions in rats (0.3mg/kg, i.p.). Such an extended pharmacological profile, especially the augmentation effect of the identified 5-HT7R antagonist on SSRI activity, seems promising regarding the complexity of affective disorders and potentially improved outcomes, including mnemonic performance.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Canale V,Partyka A,Kurczab R,Krawczyk M,Kos T,Satała G,Kubica B,Jastrzębska-Więsek M,Wesołowska A,Bojarski AJ,Popik P,Zajdel P

doi

10.1016/j.bmc.2017.03.057

subject

Has Abstract

pub_date

2017-05-15 00:00:00

pages

2789-2799

issue

10

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(17)30359-0

journal_volume

25

pub_type

杂志文章

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