σ2 Receptors
σ2 receptors are members of the sigma (σ) family of receptors that also includes σ1 receptors. Originally thought to be opioid receptors or the phencyclidine binding site on the NMDA receptor, more recently σ2 receptors have been identified as the endoplasmic reticulum transmembrane protein, TMEM97.
σ2 Receptor Agonists |
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|---|---|
| Cat. No. | Product Name / Activity |
| 2562 | PB 28 dihydrochloride |
| High affinity σ2 agonist | |
σ2 Receptor Antagonists |
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| Cat. No. | Product Name / Activity |
| 1497 | Rimcazole dihydrochloride |
| σ2 antagonist. Also DAT inhibitor | |
| 0751 | SM-21 maleate |
| Selective σ2 antagonist. Centrally active | |
Ligands |
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| Cat. No. | Product Name / Activity |
| 0545 | Ifenprodil hemitartrate |
| σ ligand (σ2 > σ1). Also α1 antagonist and NMDA antagonist acting at polyamine site | |
σ2 receptors are members of the sigma (σ) family of receptors that also includes σ1 receptors. Originally thought to be opioid receptors or the phencyclidine binding site on the NMDA receptor, more recently σ2 receptors have been identified as the endoplasmic reticulum transmembrane protein, TMEM97.
This protein regulates the sterol transporter Niemann-Pick disease protein (NPC1), and is involved in cholesterol homeostasis. An inherited mutation in the gene for NPC1 causes Niemann-Pick disease, a fatal lysosomal storage disorder. σ2 receptors are highly expressed in the CNS, lungs, liver and kidneys, and compounds targeting the receptors have been evaluated in schizophrenia and Alzheimer's disease. In addition σ2 receptors are overexpressed in several cancer cell lines and are therefore of interest to cancer researchers.