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
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 6
pKi 8.8 [6]
1,3-ditolylguanidine Cp Full agonist 7.4 pKi 3
pKi 7.4 (Ki 3.545x10-8 M) [3]
dextromethorphan Hs Agonist 6.3 pKi 2
pKi 6.3 (Ki 5.21x10-7 M) [2]
Description: Sigma receptor cloned from Jurkat cells, identified as SIGMAR1.
PRE-084 Hs Agonist 7.4 pIC50 7
pIC50 7.4 [7]
(+)-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 5
pIC50 8.4 [5]
BD-1047 Hs Antagonist 7.4 pIC50 4
pIC50 7.4 [4]
(-)-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.
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
vanoxerine Rn Binding 7.3 pIC50 1
pIC50 7.3 (IC50 4.8x10-8 M) [1]
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. 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]

2. 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]

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. Synapse, 59 (6): 350-8. [PMID:16463398]

4. 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]

5. 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]

6. 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]

7. 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 26/06/2018. Accessed on 17/07/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2552.