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

PubChem ID

3559

Name

Haloperidol

Measurement

4.5nM - ic50

PubChem ID

55445

Name

3-PPP

Measurement

253nM - ic50

PubChem ID

9817231

Name

PD-144418

Measurement

18.9nM - IC50

PubChem ID

11957449

Name

(+)-SK&F 10047

Measurement

4868nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: P426