OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
PAF receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. PAF receptors are found in a diverse array of cells, including neutrophilic polymorphonuclear leukocytes (PMN), platelets, mast cells, monocytes/macrophages, vascular endothelial cells and lymphocytes. PAF receptor stimulation is involved in intracrine, autocrine, paracrine and juxtacrine cell activation. PAF receptor agonism may exacerbate inflammation, allergic asthma, atherosclerosis, psoriasis and neurotoxicity. PAF receptor antagonism may be useful as an adjunct in the treatment of hemorrhagic and septic shock; receptor antagonism may also impair memory.
Family:
GPCR
Sub Family:
Platelet-Activating Factor
Class:
Class A
Protein Name:
PAF
Uniprot Number:
P25105
Protein Aliases:
PAFr
Gene Name:
PTAFR
Gene ID:
5724
Accession Number:
NM_000952
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant PAF receptors are prepared in modified HEPES buffer pH 7.4. A 20 μgó aliquot is incubated with 1 nM [³H]PAF for 180 minutes at 25℃. Non-specific binding is estimated in the presence of 10 μM C16-PAF. Membranes are filtered and washed, the filters are then counted to determine [³H]PAF specifically bound. Compounds are screened at 10 μM.
Ligand:
[³H] PAF
Ligand Kd (nM):
1.5
Ligand Concentration:
1 nM
Non Specific:
10 µM C16-PAF
Incubation:
180 min at 25°C
Control Inhibitor:
C16-PAF
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Inflammation/Allergy
Adverse / Beneficial Action:
PAF receptor agonism may exacerbate inflammation, allergic asthma, atherosclerosis, psoriasis and neurotoxicity. PAF receptor antagonism may be useful as an adjunct in the treatment of hemorrhagic and septic shock; receptor antagonism may also impair memory.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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