PRE-084, a σ selective PCP derivative, attenuates MK-801-induced impairment of learning in mice
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Synthesis of tropane-based σ<inf>1</inf> receptor antagonists with antiallodynic activity
2022, European Journal of Medicinal ChemistryFenfluramine modulates the anti-amnesic effects induced by sigma-1 receptor agonists and neuro(active)steroids in vivo
2022, Epilepsy and BehaviorCitation Excerpt :Moreover, neither the racemate of Norfenfluramine, nor the (+)- or (−)-isomer attenuated dizocilpine-induced deficits in the dose range tested (Fig. 1g–l). As previously described [37], the reference S1R agonist PRE-084 showed an anti-amnesic effect at 0.3 and 1 mg/kg in both tests (Fig. 2a and b). Both (+)- and (−)-Norfenfluramine prevented the anti-amnesic effects of PRE-084 (Fig. 2c and d), and therefore acted likely as S1R antagonists.
Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (σ<inf>1</inf>) receptor ligands with potent anti-amnesic effect
2022, European Journal of Medicinal ChemistryCitation Excerpt :Administration of the σ1 receptor antagonist NE-100 completely reverted the effect of the most active dose for each ligand, demonstrating that their anti-amnesic action occurred via σ1 receptors (Fig. 2E and F). Altogether, compound 1b is as potent as the reference compound PRE-084, [45] while 1a is around 30-fold more potent than PRE-084 (Fig. 1), deserving further investigation in other in vivo models of pathologies for which σ1 receptor agonists are beneficial. Molecular modeling.
Revisiting the sigma-1 receptor as a biological target to treat affective and cognitive disorders
2022, Neuroscience and Biobehavioral Reviews