CGP 12177 hydrochloride
Partial 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).
|Storage||Store at RT|
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.
|Solubility||Soluble to 50 mM in water|
References are publications that support the biological activity of the product.
Galitzky et al (1998) On the presence of a putative fourth β-adrenoceptor in human adipose tissue. TiPS 19 164 PMID: 9652187
Preitner et al (1998) Metabolic response to various β-adrenoceptor agonists in β3-adrenoceptor knockout mice: evidence for a new β-adrenergic receptor in brown adipose tissue. Br.J.Pharmacol. 124 1684 PMID: 9756384
Staehelin et al (1983) CGP-12177. A hydrophilic beta-adrenergic receptor radioligand reveals high affinity binding of agonists to intact cells. J.Biol.Chem. 258 3496 PMID: 6131886
Strosberg and Pietri-Rouxel (1996) Function and regulation of the β3-adrenoceptor. TiPS 17 373 PMID: 8979772
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5 Citations for CGP 12177 hydrochloride
Citations are publications that use Tocris products. Selected citations for CGP 12177 hydrochloride include:
Gherbi et al (2015) Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation. FASEB J 29 2859 PMID: 25837585
Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661 PMID: 26030448
Suárez et al (2014) Oleoylethanolamide enhances β-adrenergic-mediated thermogenesis and white-to-brown adipocyte phenotype in epididymal white adipose tissue in rat. Dis Model Mech 7 129 PMID: 24159189
Gherbi et al (2014) Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP. Br J Pharmacol 171 5431 PMID: 25052258
Littmann et al (2015) Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands. Proc Natl Acad Sci U S A 355 183 PMID: 26306764
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.