alpha1A Human Adrenoceptor GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Adrenoreceptors 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. Adrenoreceptors are found in most peripheral tissue and within the central nervous system.
Family:
GPCR
Sub Family:
Adrenoceptor
Class:
Class A
Protein Name:
alpha1A
Uniprot Number:
P35348
Protein Aliases:
Alpha-1A adrenoceptor|Alpha-1C adrenergic receptor|Alpha-adrenergic receptor 1c
Gene Name:
ADRA1A
Gene ID:
148
Gene Aliases:
ADRA1L1|ADRA1C
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant adrenergic α1A receptors expressed in human Chem-1 cells are used in modified HEPES buffer pH 7.4. A 2 µgǂ aliquot is incubated with 0.6 nM [³H]Prazosin for 60 minutes at 25°C. Non-specific binding is estimated in the presence of 10 μM phentolamine. Receptors are filtered and washed, the filters are then counted to determine [³H]Prazosin specifically bound. Compounds are screened at 10 μM.
Ligand:
[³H] Prazosin
Ligand Kd (nM):
0.57
Ligand Concentration:
0.6 nM
Non Specific:
10 µM Phentolamine
Incubation:
60 min at 25°C
Control Inhibitor:
Prazosin hydrochloride
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Minimum Order Quantity:
2
Turnaround Time
Standard:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Adverse / Beneficial Action:
Adrenergic a1A receptor antagonism may result in hypotension as well as orthostatic hypotension and may be useful in the treatment of benign protatic hyperplasia.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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