CGP 12177 hydrochloride
Chemical Name: 4-[3-[(1,1-Dimethylethyl)amino]2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one hydrochloride
Biological ActivityPartial agonist at β3-adrenoceptors. β1- and β2-adrenoceptor antagonist (Ki values are 0.9, 4 and 88 nM for β1, β2 and β3 receptors respectively).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
On the presence of a putative fourth β-adrenoceptor in human adipose tissue.
Galitzky et al.
Metabolic response to various β-adrenoceptor agonists in β3-adrenoceptor knockout mice: evidence for a new β-adrenergic receptor in brown adipose tissue.
Preitner et al.
Function and regulation of the β3-adrenoceptor.
Strosberg and Pietri-Rouxel
CGP-12177. A hydrophilic beta-adrenergic receptor radioligand reveals high affinity binding of agonists to intact cells.
Staehelin et al.
Citations for CGP 12177 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for CGP 12177 hydrochloride include:
5 Citations: Showing 1 - 5
Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.
Authors: Littmann Et al.
Proc Natl Acad Sci U S A 2015;355:183
Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.
Authors: Gherbi Et al.
FASEB J 2015;29:2859
Application of BRET to monitor ligand binding to GPCRs.
Authors: Stoddart Et al.
Nat Methods 2015;12:661
Oleoylethanolamide enhances β-adrenergic-mediated thermogenesis and white-to-brown adipocyte phenotype in epididymal white adipose tissue in rat.
Authors: Suárez Et al.
Dis Model Mech 2014;7:129
Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP.
Authors: Gherbi Et al.
Br J Pharmacol 2014;171:5431
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