Ameliorating effect of SA4503, a novel sigma 1 receptor agonist, on memory impairments induced by cholinergic dysfunction in rats

European Journal of Pharmacology
T SendaS Mita

Abstract

We found a potent and selective sigma 1 receptor agonist, SA4503 (1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydro-chloride), with high affinity for the sigma 1 receptor subtype (IC50 = 17 nM), but low affinity for the sigma 2 receptor subtype (IC50 = 1800 nM). The binding activity and selectivity of SA4503 resembled those of (+)-pentazocine, a prototype sigma 1 receptor agonist. We have previously shown that the sigma 1 receptor agonist activated central cholinergic functions. Therefore, we examined the effects of SA4503 on the cholinergic dysfunction-induced memory impairments in a passive avoidance task. Scopolamine, a muscarinic acetylcholine receptor antagonist, produced memory impairment, when it was administered 30 min before the training session of the passive avoidance task in rats. Single administration of SA4503 significantly reduced the scopolamine-induced memory impairment. In addition, the lesioning by injection of alpha-amino-3-hydroxy-5-isoxazole acetic acid (ibotenic acid) into the basal forebrain area produced memory impairment in rats. Repeated administration of SA4503 after lesioning of the basal forebrain area ameliorated the basal forebrain lesion-induced memory impairment. Moreover, the ame...Continue Reading

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Citations

May 24, 2008·Annals of Nuclear Medicine·Masahiro MishinaKiichi Ishiwata
Nov 5, 1998·Pharmacology, Biochemistry, and Behavior·T KobayashiS Mita
Feb 11, 1999·Pharmacology, Biochemistry, and Behavior·M NakazawaS Mita
Nov 1, 2002·Behavioural Pharmacology·G Skuza, Z Rogóz
Mar 19, 2003·British Journal of Pharmacology·Hui-Hung WangChieh-Fu Chen
Jun 10, 2015·Journal of Receptor and Signal Transduction Research·Colin G Rousseaux, Stephanie F Greene
Dec 3, 2014·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Nisha K RamakrishnanAren van Waarde
Jan 24, 2015·Journal of Neuroscience Research·Daisuke YamashitaTatsuo Matsunaga
Apr 8, 2010·Human Psychopharmacology·Ian Hindmarch, Kenji Hashimoto
Dec 15, 2005·International Journal of Clinical Practice·J L Carrasco, C Sandner
Sep 22, 2006·The Journal of Pharmacology and Experimental Therapeutics·Christopher KatnikJavier Cuevas
Jan 1, 2007·International Journal of Psychiatry in Clinical Practice·Stefano Pallanti, Cláudio Sandner
Jul 3, 2021·International Journal of Molecular Sciences·Francesca Serena AbatematteoCarmen Abate
Aug 24, 2007·European Journal of Pharmacology·Dong Hyun KimJong Hoon Ryu

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