Nomifensine efficiency in the improvement of memory trace restoration impaired by spontaneous forgetting or amnesic influence was demonstrated in experiments on BALB/c mice by using the passive avoidance technique. Doses of 10-20 mg/kg proved to be the most efficient. The presented results suggest that the antiamnesic effect of nomifensine is due to the activation of dopaminergic and noradrenergic systems.
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Bioorg Med Chem
January 2025
Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy.
The imidazo[1,5-a]quinoline scaffold of central benzodiazepine receptor (CBR) ligands was used as the pharmacophore in the design of bivalent ligands bearing spacers showing variable length and different physicochemical features. The newly designed compounds were synthesized along with the corresponding reference monovalent compounds bearing the corresponding spacers terminated with a tert-butoxycarbonyl group. The novel compounds were tested in binding assays with different CBR preparations such as the cerebral cortex from male CD-1 albino mice or the human recombinant α1β3γ2 and α2β3γ2 γ-aminobutyric acid type A receptors (GABARs) stably expressed in mouse L(tk-) cells.
View Article and Find Full Text PDFActa Pharm Sin B
October 2024
Department of Neurochemistry, Cuban Center for Neurosciences, Cubanacan, Playa, Havana CP 11600, Cuba.
The aggregation of Amyloid- (A) peptides is associated with neurodegeneration in Alzheimer's disease (AD). We previously identified novel naphtalene derivatives, including the lead compound Amylovis-201, able to form thermodynamically stable complexes with A species, peptides and fibrils. As the drug showed a chemical scaffold coherent for an effective interaction with the receptor chaperone and as agonists are currently developed as potent neuroprotectants in AD, we investigated the pharmacological action of Amylovis-201 on the receptor.
View Article and Find Full Text PDFEur J Pharmacol
December 2024
Department of Biology, Faculty of Biology, Alexandru Ioan Cuza University of Iasi, 700506 Iasi, Romania. Electronic address:
J Alzheimers Dis
September 2024
Department of Drug and Health Sciences, University of Catania, Catania, Italy.
Background: Sigma-1 receptors are highly expressed in brain areas related to cognitive function and are a promising target for anti-amnesic treatments. We previously showed that activation of sigma-1 receptors by the selective agonist compound methyl(1 R,2 S/1 S,2 R)-2-[4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl) cyclopropane carboxylate [(±)-PPCC] promotes a remarkable recovery in rat models of memory loss associated to cholinergic dysfunction.
Objective: In this study, we sought to assess the role of (±)-PPCC on working memory deficits caused by noradrenergic depletion.
Metab Brain Dis
April 2024
Programa de Pós-Graduação em Bioquímica e Bioprospecção, Laboratório de Pesquisa em Farmacologia Bioquímica (LaFarBio), Grupo de Pesquisa em Neurobiotecnologia (GPN), Centro de Ciências Químicas, Farmacêuticas e de Alimentos, Universidade Federal de Pelotas (UFPel), Pelotas, RS, CEP 96010-900, Brazil.
This study aimed to investigate the action of two different formulations of curcumin (Cur)-loaded nanocapsules (Nc) (Eudragit [EUD] and poly (ɛ-caprolactone) [PCL]) in an amnesia mice model. We also investigated the formulations' effects on scopolamine-induced (SCO) depressive- and anxiety-like comorbidities, the cholinergic system, oxidative parameters, and inflammatory markers. Male Swiss mice were randomly divided into five groups (n = 8): group I (control), group II (Cur PCL Nc 10 mg/kg), group III (Cur EUD Nc 10 mg/kg), group IV (free Cur 10 mg/kg), and group V (SCO).
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