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.

Products
Background
Gene Data

σ2 Receptor Agonists

Cat. No. Product Name / Activity
2562 PB 28 dihydrochloride
High affinity σ2 agonist
6740 Siramesine hydrochloride
High affinity σ agonist (σ2 > σ1)

σ2 Receptor Antagonists

Cat. No. Product Name / Activity
1497 Rimcazole dihydrochloride
σ2 antagonist. Also DAT inhibitor
0751 SM-21 maleate
Selective σ2 antagonist. Centrally active

Ligands

Cat. No. Product Name / Activity
0545 Ifenprodil hemitartrate
σ ligand (σ2 > σ1). Also α1 antagonist and NMDA antagonist acting at polyamine site

Related Targets

    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.

    Sigma2 receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    TMEM97 Human TMEM97 NM_014573 Q5BJF2
    Mouse Tmem97 NM_133706 Q8VD00
    Rat Tmem97 NM_001008334 NP_001008335