SA4503, a novel cognitive enhancer, with σ1 receptor agonistic properties

  title={SA4503, a novel cognitive enhancer, with $\sigma$1 receptor agonistic properties},
  author={Kiyoshi Matsuno and Toshihiko Senda and Tetsuya Kobayashi and Kazuyoshi Okamoto and Katsuhiko Nakata and Shiro Mita},
  journal={Behavioural Brain Research},
Regional differences of the effect of σ receptor ligands on the acetylcholine release in the rat brain
It is found that a receptor ligands differentially regulated the acetylcholine (ACh) neurotransmission in the rat brain and was more potent than that elicited by DTG.
Involvement of the sigma 1 ( r 1 ) receptor in the anti-amnesic , but not antidepressant-like , effects of the aminotetrahydrofuran derivative ANAVEX 1-41
ANAVEX1-41 is a potent anti-amnesic drug, acting through muscarinic and s1 receptors, and the latter component may be involved in the enhancing effects of the drug on long-term memory processes.
Anti-amnesic and neuroprotective potentials of the mixed muscarinic receptor/sigma1 (σ1) ligand ANAVEX2-73, a novel aminotetrahydrofuran derivative
The neuroprotective activity of ANAVEX2-73, its mixed cholinergic/σ1 activity, its low active dose range and its long duration of action together reinforce its therapeutic potential in Alzheimer’s disease.


Sigma receptors. Putative links between nervous, endocrine and immune systems.
  • T. Su
  • Biology
    European journal of biochemistry
  • 1991
The sigma receptor is a neuronal substrate that binds several psychoactive compounds. These include cocaine, some steroids, dextromethorphan, phencyclidine (PCP), and benzomorphans such as
Increase in extracellular acetylcholine level by sigma ligands in rat frontal cortex.
None of the sigma ligands tested in this study had any effects on acetylcholinesterase or choline acetyltransferase activity and sodium-dependent high affinity choline uptake site in the rat frontal cortex.
σ Receptors: From Molecule to Man
One of the initial difficulties in developing mixed agonist/antagonist opiates was the fact that conventional animal models often failed to demonstrate their analgesic actions, so it was hoped that one could design selective agents which lack such dysphoric effects, but retain the ability to elicit analgesia with minimal addictive propensity.
Alzheimer's disease: a disorder of cortical cholinergic innervation.
Advances in neurotransmitter systems involved in the symptomatic manifestations of neurological and psychiatric disorders reflect a close interaction between experimental and clinical neuroscientists in which information derived from basic neurobiology is rapidly utilized to analyze disorders of the human brain.
A proposal for the classification of sigma binding sites.
Exacerbation of parkinsonism by tacrine.
A patient with Alzheimer's disease and mild features of parkinsonism was treated with tacrine. Tremor and gait dysfunction worsened but responded to the addition of levodopa without adversely