σ2

Target id: 2553

Nomenclature: σ2

Family: Sigma receptors

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for σ2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 176 17q11.2 TMEM97 transmembrane protein 97 1
Mouse 4 176 11 B5 Tmem97 transmembrane protein 97
Rat 4 176 10q25 Tmem97 transmembrane protein 97
Previous and Unofficial Names
MAC30 | Meningioma-associated protein 30
Database Links
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
PB-28 Hs Agonist 8.3 pKi 2
pKi 8.3 [2]
1,3-ditolylguanidine Cp Full agonist 7.4 pKi 3
pKi 7.4 (Ki 3.987x10-8 M) [3]
[3H]-di-o-tolylguanidine Hs Agonist - -
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
SM 21 Hs Antagonist 7.2 pIC50 4
pIC50 7.2 [4]
General Comments
The sigma2 receptor has been reported to be TMEM97 [1], a 4TM protein partner of NPC1, the Niemann-Pick C1 protein, a 13TM cholesterol-binding protein.

References

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1. Alon A, Schmidt HR, Wood MD, Sahn JJ, Martin SF, Kruse AC. (2017) Identification of the gene that codes for the σ2 receptor. Proc. Natl. Acad. Sci. U.S.A.114 (27): 7160-7165. [PMID:28559337]

2. Berardi F, Colabufo NA, Giudice G, Perrone R, Tortorella V, Govoni S, Lucchi L. (1996) New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. J. Med. Chem.39 (1): 176-82. [PMID:8568804]

3. Lever JR, Gustafson JL, Xu R, Allmon RL, Lever SZ. (2006) Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse59 (6): 350-8. [PMID:16463398]

4. Mach RH, Wu L, West T, Whirrett BR, Childers SR. (1999) The analgesic tropane analogue (+/-)-SM 21 has a high affinity for sigma2 receptors. Life Sci.64 (10): PL131-7. [PMID:10096443]

How to cite this page

Sigma receptors: σ2. Last modified on 22/08/2017. Accessed on 13/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2553.