sigma non-opioid intracellular receptor 1

Target id: 2552

Nomenclature: sigma non-opioid intracellular receptor 1

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 sigma non-opioid intracellular receptor 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 2 223 9p13.3 SIGMAR1 sigma non-opioid intracellular receptor 1
Mouse 2 223 4 Sigmar1 sigma non-opioid intracellular receptor 1
Rat 2 223 5q22 Sigmar1 sigma non-opioid intracellular receptor 1
Previous and Unofficial Names
σ1 | opioid receptor, sigma 1 | OPRS1 | SIG-1R | sigma 1-type opioid receptor | Sigma1R
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
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
(RS)-PPCC Hs Agonist 8.8 pKi 5
pKi 8.8 [5]
1,3-ditolylguanidine Cp Full agonist 7.4 pKi 2
pKi 7.4 (Ki 3.545x10-8 M) [2]
dextromethorphan Hs Agonist 6.3 pKi 1
pKi 6.3 (Ki 5.21x10-7 M) [1]
Description: Sigma receptor cloned from Jurkat cells, identified as SIGMAR1.
PRE-084 Hs Agonist 7.4 pIC50 6
pIC50 7.4 [6]
(+)-SKF 10.047 Hs Agonist - -
[3H]pentazocine 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
NE-100 Hs Antagonist 8.4 pIC50 4
pIC50 8.4 [4]
BD-1047 Hs Antagonist 7.4 pIC50 3
pIC50 7.4 [3]
(-)-pentazocine Hs Antagonist - -
Antagonist Comments
The σ receptor is the likely primary target of the approved drug pentazocine (racemic mixture), although the interaction is shown in the antagonist table above with (-)-pentazocine.
Clinically-Relevant Mutations and Pathophysiology
Disease:  Amyotrophic lateral sclerosis 16, juvenile; ALS16
Synonyms: Juvenile amyotrophic lateral sclerosis [Orphanet: ORPHA300605]
OMIM: 614373
Orphanet: ORPHA300605

References

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1. Ganapathy ME, Prasad PD, Huang W, Seth P, Leibach FH, Ganapathy V. (1999) Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat human T lymphocyte cell line. J. Pharmacol. Exp. Ther.289 (1): 251-60. [PMID:10087012]

2. 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]

3. Matsumoto RR, Bowen WD, Tom MA, Vo VN, Truong DD, De Costa BR. (1995) Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism. Eur. J. Pharmacol.280 (3): 301-10. [PMID:8566098]

4. Okuyama S, Imagawa Y, Ogawa S, Araki H, Ajima A, Tanaka M, Muramatsu M, Nakazato A, Yamaguchi K, Yoshida M et al.. (1993) NE-100, a novel sigma receptor ligand: in vivo tests. Life Sci.53 (18): PL285-90. [PMID:7901723]

5. Prezzavento O, Campisi A, Ronsisvalle S, Li Volti G, Marrazzo A, Bramanti V, Cannavò G, Vanella L, Cagnotto A, Mennini T et al.. (2007) Novel sigma receptor ligands: synthesis and biological profile. J. Med. Chem.50 (5): 951-61. [PMID:17328523]

6. Su TP, Wu XZ, Cone EJ, Shukla K, Gund TM, Dodge AL, Parish DW. (1991) Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand. J. Pharmacol. Exp. Ther.259 (2): 543-50. [PMID:1658302]

How to cite this page

Sigma receptors: sigma non-opioid intracellular receptor 1. Last modified on 13/08/2015. Accessed on 17/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2552.