σ2 | Sigma receptors | IUPHAR Guide to IMMUNOPHARMACOLOGY

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σ2

Target not currently curated in GtoImmuPdb

Target id: 2553

Nomenclature: σ2

Family: Sigma receptors

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 176 17q11.2 TMEM97 transmembrane protein 97 2
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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
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 Value Parameter Reference
PB-28 Hs Agonist 8.3 pKi 3
pKi 8.3 [3]
1,3-ditolylguanidine Cp Full agonist 7.4 pKi 5
pKi 7.4 (Ki 3.987x10-8 M) [5]
[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 Value Parameter Reference
PD-144418 Mm Antagonist 5.9 pKi 1
pKi 5.9 (Ki 1.377x10-6 M) [1]
Description: Displacement of [3H]DTG from sigma2 sites on membranes from NG 108-15 neuroblastoma X glioma rat/mouse hybrid cells
SM 21 Hs Antagonist 7.2 pIC50 6
pIC50 7.2 [6]
View species-specific antagonist tables
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
vanoxerine Rn Binding 7.3 pIC50 4
pIC50 7.3 (IC50 4.8x10-8 M) [4]
General Comments
The sigma2 receptor has been reported to be TMEM97 [2], a 4TM protein partner of NPC1, the Niemann-Pick C1 protein, a 13TM cholesterol-binding protein.

References

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1. Akunne HC, Whetzel SZ, Wiley JN, Corbin AE, Ninteman FW, Tecle H, Pei Y, Pugsley TA, Heffner TG. (1997) The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology, 36 (1): 51-62. [PMID:9144641]

2. 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]

3. 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]

4. Contreras PC, Bremer ME, Rao TS. (1990) GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain. Life Sci., 47 (22): PL133-7. [PMID:1980329]

5. Lever JR, Gustafson JL, Xu R, Allmon RL, Lever SZ. (2006) Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse, 59 (6): 350-8. [PMID:16463398]

6. 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 27/03/2020. Accessed on 20/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2553.