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.
σ1 Receptor Agonists |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 3870 | (±)-PPCC oxalate |
| Selective sigma (σ) agonist (σ1> σ2) | |
| 0589 | PRE-084 hydrochloride |
| Highly selective σ1 agonist | |
| 7630 | Pridopidine |
| Highly selective σ1 agonist | |
| 4951 | SA 4503 dihydrochloride |
| Selective σ1 receptor agonist | |
| 1079 | (+)-SK&F 10047 hydrochloride |
| σ1 selective agonist | |
σ1 Receptor Antagonists |
|
| Cat. No. | Product Name / Activity |
| 0956 | BD 1047 dihydrobromide |
| σ1 selective antagonist | |
| 3133 | NE 100 hydrochloride |
| Selective σ1 antagonist | |
| 7156 | WQ 1 |
| Potent and selective σ1 receptor antagonist; active in vivo | |
Ligands |
|
| Cat. No. | Product Name / Activity |
| 0883 | BD 1063 dihydrochloride |
| Selective σ1 ligand, putative antagonist | |
| 1033 | Fluvoxamine maleate |
| High affinity σ1 ligand | |
| 0931 | Haloperidol hydrochloride |
| High affinity σ ligand (σ1 > σ2); also D2 antagonist | |
| 2332 | (+)-Igmesine hydrochloride |
| Selective σ1 ligand; antidepressant | |
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.