Biological Information
Background Information:
Sigma receptor-mediated transduction mechanisms have not as yet been fully elucidated, but require neither G-protein activation nor phosphorylation. Sigma receptors, located primarily in the central nervous system but also in endocrine and immune systems, have been implicated in psychosis, depression, cognition, neuroprotection, and locomotion in the central nervous system and regulation of cell proliferation. Sigma s1 receptors, at least in part, are intracellular amplifiers of glutaminergic NMDA, dopaminergic, IP3-related metabotropic, nerve growth factor-related systems, voltage-gated K+ channels as well as Ca2+influx and intracellular mobilization. Sigma s1 receptor agonist may be antidepressant, facilitate learning and addiction, and reduce opiate analgesia. Sigma s1 receptor antagonist may be antipsychotic.
Family:
Transmembrane (Other)
Sub Family:
Sigma
Protein Name:
sigma1
Uniprot Number:
Q99720
Gene Name:
SIGMAR1
Gene ID:
10280
Gene Aliases:
SR-BP1
Accession Number:
NM_005866
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H](+)pentazocine
Ligand Kd (nM):
16
Ligand Concentration:
15 nM
Non Specific:
10 µM Haloperidol
Incubation:
120 min at 37°C
Control Inhibitor:
haloperidol
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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