σ1 Receptors

σ1 receptors are members of the σ family of receptors that also includes σ2 receptors. They are distinguished from σ2 receptors as they have high affinity and stereoselectivity for the (+)-isomers of pentazocine, SK&F 10047 and cyclazocine, and different subcellular localizations.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
3870 (±)-PPCC oxalate
Selective sigma (σ) agonist (σ1> σ2)
0589 PRE-084 hydrochloride
Highly selective σ1 agonist
4951 SA 4503 dihydrochloride
Selective σ1 receptor agonist
1079 (+)-SK&F 10047 hydrochloride
σ1 selective agonist

Antagonists

Cat No Product Name / Activity
0956 BD 1047 dihydrobromide
σ1 selective antagonist
3133 NE 100 hydrochloride
Selective σ1 antagonist

Ligands

Cat No Product Name / Activity
0883 BD 1063 dihydrochloride
Selective σ1 ligand, putative antagonist
0454 Carbetapentane citrate
High affinity σ1 ligand
3428 DMT
Endogenous σ1 ligand. Also 5-HT2A agonist
2195 Eliprodil
σ ligand (σ1 > σ2). Also polyamine site NMDA antagonist and Ca2+ channel blocker. Neuroprotective
1033 Fluvoxamine maleate
High affinity σ1 ligand
0931 Haloperidol hydrochloride
High affinity σ ligand (σ1 > σ2). Also D2 antagonist
0748 4-IBP
σ ligand, σ1> σ2
2332 (+)-Igmesine hydrochloride
Selective σ1 ligand; antidepressant
2606 PD 144418 oxalate
High affinity, selective σ1 ligand
0763 N-[2-(Piperidinylamino)ethyl]-4-iodobenzamide
σ1 selective ligand
2669 TC 1
High affinity σ1 ligand

Other

Cat No Product Name / Activity
2074 SKF 83959 hydrobromide
Potentiates agonist binding of the σ1 receptor. Also D1-like agonist

Related Targets

    σ1 receptors are members of the σ family of receptors that also includes σ2 receptors. Originally thought to be opioid receptors or the phencyclidine binding site on the NMDA receptor, they are now known to be distinct targets. These receptors are distinguished from σ2 receptors as they exhibit high affinity and stereoselectivity for the (+)-isomers of pentazocine, SK&F 10047 and cyclazocine, as well as having different tissue distribution patterns and subcellular localizations.

    σ1 receptors are distributed throughout the central nervous system (especially the hippocampal formation and other limbic areas) and in various peripheral tissues, including the liver, kidneys, lungs and muscles. These single transmembrane receptors are found on the plasma, mitochondrial and endoplasmic reticular membranes and are primarily associated with neuronal perikarya and dendrites.

    There has been extensive study of σ receptors since their discovery over twenty years ago. σ ligands are thought to have potential as pharmacological agents in modulation of mood disorders, amnesic and cognitive deficits, the effects produced by drug abuse, tardive dyskinesia and the potentiation of analgesia.

    Literature for σ1 Receptors

    New Product Guide

    New Product Guide (Spring/Summer 2017)

    Our new product guide highlights over 130 new products added to the Tocris Bioscience range during the first half of 2017.

    • 7-TM Receptors
    • Enzymes
    • Enzyme-Linked Receptors
    • Ion Channels
    • Nuclear Receptors
    • Transporters
    • Apoptosis
    • Cell Metabolism
    • Epigenetics
    • Fluorescent Imaging
    • Signal Transduction
    • Stem Cells

    σ1 Receptor Gene Data

    Species Gene Symbol Gene Accession No. Protein Accession No.
    Human SIGMAR1 NM_005866 Q8N7H3
    Mouse Sigmar1 NM_011014 O55242
    Rat Oprs1 NM_030996 Q9R0C9