Neuroprotective and antiamnesic effects of human nerve growth factor (HNGF) synthetic dipeptide mimetic bis-(N-monosuccinyl-glycyl-lysine)hexamethylenediamide (GK-2h) has been studied on a model of bilateral photochemically induced focal ischemical brain injury in prefrontal cortex of rats. It is established that a single intraperitoneal injection of GK-2h (0.1 mg/kg) 1 h or 4 h after operation, followed by injections on the 2nd, 4th and 8th days after operation, results (on the 9th day) in reduction of the cortical infarction volume by 47 or 65%, and leads to restoration of the passive avoidance reflex (acquired before experimental ischemic insult) by 42 and 60%, respectively. It is concluded that GK-2h possesses significant neuroprotective properties.
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Behav Neurol
January 2025
Department of Animal Biology and Physiology, University of Yaoundé I, Yaoundé, Cameroon.
Amnesia is a memory disorder marked by the inability to recall or acquire information. Hence, drugs that also target the neurogenesis process constitute a hope to discover a cure against memory disorders. This study is aimed at evaluating the antiamnesic and neurotrophic effects of the aqueous extract of () on in vivo and in vitro models of excitotoxicity.
View Article and Find Full Text PDFBioorg 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 PDFHeliyon
November 2024
Department of Animal Biology and Physiology, University of Yaoundé I, P.O. Box 812, Yaoundé, Cameroon.
Mesiotemporal lobe epilepsy is the most refractory form of epilepsy. The management of this condition relies on the use of antiepileptic drugs known to provide symptomatic relief. Herbal remedies are therefore an alternative to finding a cure for epilepsy.
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:
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