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 :Two behavioral tests were systematically used in parallel which address complementary memory processes. Spontaneous alternation performance in the Y-maze is an index of spatial working memory [34,37,38], while the step-through latency measured in the passive avoidance test is a non-spatial long-term memory parameter [34,37,39]. Drugs were tested in the 0.1–3 mg/kg dose range and we observed that Fenfluramine racemate and (+)-Fenfluramine significantly attenuated dizocilpine-induced learning deficits at the doses of 0.3 and 1 mg/kg (Fig. 1a–d). (
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 :In general, σ1 receptor ligands referred to as agonists are devoid of cytotoxic activity in cancer cells, and neither of the two compounds tested were cytotoxic, indicating that they function as σ1 receptor agonists. Accordingly, we expected that our σ1 receptor agonists should produce anti-amnesic effects when evaluated by using two complementary behavioral tests, namely spontaneous alternation in the Y-maze (measuring spatial working memory) and a step-through-type passive avoidance response (measuring non-spatial long-term memory) [43–45]. Learning deficits were induced in mice (12 per group) by administering the noncompetitive NMDA receptor antagonist dizocilpine ((+)-MK-801 maleate) at a dose of 0.15 mg/kg intraperitoneally (ip) 20 min before the Y-maze test session or the acquisition session in the passive avoidance test [43,45].
Revisiting the sigma-1 receptor as a biological target to treat affective and cognitive disorders
2022, Neuroscience and Biobehavioral Reviews