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Early Development of Sigma-Receptor Ligands

Future Medicinal Chemistry, 2010
Sigma receptors (σ-1 and σ-2) are non-opioid proteins implicated in the pathophysiology of various neurological disorders and cancer. The σ-1 subtype is a chaperon protein widely distributed in the CNS and peripheral tissues. These receptors are involved in the modulation of K(+)- and Ca(2+)-dependent signaling cascades at the endoplasmic reticulum and
Sanju, Narayanan   +4 more
openaire   +2 more sources

Sigma Receptors in Oncology

Current Pharmaceutical Design, 2010
Sigma receptors (subtypes sigma-1 and sigma-2) are a unique class of binding sites expressed throughout the mammalian body. The endogenous ligand for these sites has not been identified, but steroid hormones (particularly progesterone), sphingolipid-derived amines and N,N-dimethyltryptamine can bind with fairly high affinity.
van Waarde, Aren   +5 more
openaire   +1 more source

Sigma-1 Receptor in Motoneuron Disease

2017
Amyotrophic Lateral Sclerosis (ALS ) is a neurodegenerative disease affecting spinal cord and brain motoneurons , leading to paralysis and early death. Multiple etiopathogenic mechanisms appear to contribute in the development of ALS , including glutamate excitotoxicity, oxidative stress , protein misfolding, mitochondrial defects, impaired axonal ...
Mancuso, Renzo, Navarro, Xavier
openaire   +3 more sources

Sigma-1 Receptor and Neuronal Excitability

2017
The sigma-1 receptor (Sig-1R), via interaction with various proteins, including voltage-gated and ligand-gated ion channels (VGICs and LGICs), is involved in a plethora of neuronal functions. This capability to regulate a variety of ion channel targets endows the Sig-1R with a powerful capability to fine tune neuronal excitability, and thereby the ...
openaire   +2 more sources

Sigma Receptor Ligands Are Potent Antiprion Compounds that Act Independently of Sigma Receptor Binding

ACS Chemical Neuroscience
Prion diseases are invariably fatal neurodegenerative diseases of humans and other animals for which there are no effective treatment options. Previous work from our laboratory identified phenethylpiperidines as a novel class of anti-prion compounds. While working to identify the molecular target(s) of these molecules, we unexpectedly discovered ten ...
Robert C. C. Mercer   +5 more
openaire   +2 more sources

Sigma Receptors and Sigma Ligands: Background to a Pharmacological Enigma

Pharmacopsychiatry, 2004
Although it is now well established that the sigma receptors are distinct from neurotransmitter, neuropeptide and steroid receptors, their precise physiological role, and possible involvement in the pathology of neurological and psychiatric disorders, remains an enigma.
openaire   +2 more sources

Sigma-1 Receptors Modulate NMDA Receptor Function

2013
The sigma-1 receptor (σ-1R) is an endoplasmic reticulum (ER) protein that modulates a number of ion channels. It is hypothesized that σ-1Rs activated with agonist translocate to the plasma membrane. The σ-1R potentiates N-methyl-D-aspartate Receptors (NMDARs), important constituents of synaptic plasticity.
openaire   +2 more sources

Flag manifold sigma models

Physics Reports, 2022
Dmitri V Bykov
exaly  

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