σ1 Receptors

Supporting information

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.

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

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