CGP 12177 - CAS 81047-99-6
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Adrenergic Receptor
CGP 12177 is a partial β3-adrenoceptor agonist with Ki value of 88 nM. It is also an of β1- and β2-adrenoceptors antagonist with Ki values of 0.9 nM and 4 nM for β1-, β2adrenoceptors. CGP12177 can slightly activate L-type Ca2+ current in human ventricular myocytes.
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Soluble in DMSO
-20℃ Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
1.Cyclic AMP-independent relaxation mediated by beta3-adrenoceptors on guinea pig gastrointestine.
Horinouchi T1, Koike K. Eur J Pharmacol. 2002 May 3;442(1-2):137-46.
In this study, we investigated the signal transduction pathway involved in beta(3)-adrenoceptor-mediated relaxations of guinea pig gastric fundus and duodenum. In the presence of beta1- and beta2-adrenoceptor blockade, the potency (pD2 value) of catecholamines ((-)-isoprenaline, (-)-noradrenaline and (-)-adrenaline) and beta(3)-adrenoceptor agonists ((R*, R*)-(+/-)-4-[2-[(2-(3-chlorophenyl)-2-hydroxyethyl)amino]propyl]phenoxyacetic acid sodium (BRL37344) and (+/-)-[4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one] hydrochloride ((+/-)-CGP12177A)) to induce relaxation was not affected by the adenylate cyclase inhibitor, 9-(tetrahydro-2-furanyl)-9H-purin-6-amine (SQ-22,536, 100 microM). Catecholamines induced an elevation of cyclic AMP and SQ-22,536 significantly abolished the responses of gastric fundus. However, cyclic AMP levels were unaltered by the beta3-adrenoceptor agonists in gastric fundus and by the five agonists in duodenum.
2.Evidence for two atypical conformations of beta-adrenoceptors and their interaction with Gi proteins.
Santos IN1, Sumitame M, Caceres VM, Moreira MF, Krieger MH, Spadari-Bratfisch RC. Eur J Pharmacol. 2005 Apr 18;513(1-2):109-18. Epub 2005 Apr 1.
In this study, we investigated whether the responses of right atria from sinoaortic denervated rats to CGP12177 (4(3-t-butylamino-2-hydroxypropoxy benzidimidazole-2 one, hydrochloride)), isoprenaline and norepinephrine desensitized in parallel and whether CGP12177 interacted with distinct conformations of beta-adrenoceptors. Right atria from rats 48 h after sinoaortic denervation were subsensitive to isoprenaline, norepinephrine and CGP12177. One week after sinoaortic denervation, the sensitivity to CGP12177 had recovered whereas the responses to isoprenaline and norepinephrine were still subsensitive, suggesting that the binding sites for these molecules showed independent behavior. In atria from 48 h sinoaortic-denervated rats, propranolol or 3 microM CGP20712A (2-hydroxy-5(2-((2-hydroxy-3-(4-((methyl-4-trifluormethyl)1H imidazole-2-yl)-phenoxypropyl) amino) ethoxy)-benzamide monomethane sulphonate)) blocked the responses to 10 nM-1 microM CGP12177 and steepened the curves.
3.Transfected beta3- but not beta2-adrenergic receptors regulate cystic fibrosis transmembrane conductance regulator activity via a new pathway involving the mitogen-activated protein kinases extracellular signal-regulated kinases.
Robay A1, Toumaniantz G, Leblais V, Gauthier C. Mol Pharmacol. 2005 Mar;67(3):648-54. Epub 2004 Nov 24.
We have shown previously that in a heterologous mammalian expression system A549 cells, beta3-adrenoceptor (beta3-AR) stimulation regulates the activity of cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. The present investigation was carried out to determine the signaling pathway involved in this regulation. A549 cells were intranuclearly injected with plasmids encoding human CFTR and beta3-AR. CFTR activity was functionally assessed by microcytofluorimetry. The application of 1 microM 4-[3-t-butylamino-2-hydroxypropoxy]benzimidazol-2-1 hydrochloride (CGP-12177), a beta3-AR agonist, produced a CFTR activation that was not abolished by protein kinase A inhibitors. In pertussis toxin-pretreated cells, the CFTR activation induced by CGP-12177 was abolished. The overexpression of beta-adrenoceptor receptor kinase, an inhibitor of betagamma subunits, abolished the CGP-12177-induced CFTR activation, suggesting the involvement of betagamma subunits of Gi/o proteins.
4.Receptor imaging in the thorax with PET.
Elsinga PH1, van Waarde A, Vaalburg W. Eur J Pharmacol. 2004 Sep 19;499(1-2):1-13.
This review focuses on positron emission tomography (PET)-imaging of receptors in the sympathetic and the parasympathetic systems of heart and lung and highlights the human applications of PET. For the alpha-adrenoceptor, only [11C]GB67 (N2-[6-[(4-amino-6,7-dimethoxy-2-quinazolinyl)(methyl)amino]hexyl]-N2-[11C]methyl-2-furamide hydrochloride) has been developed. Its potential for application in patients needs to be assessed. For both the beta-adrenergic and the muscarinic systems, potent PET radioligands have been prepared and evaluated in patients. It has been possible to measure receptor densities quantitatively in human heart [[11C]MQNB: [11C]methylquinuclidinyl benzilate, [11C]CGP12177: S-(3'-t-butylamino-2'-hydroxypropoxy)-benzimidazol-2-[11C]one and [11C]CGP12388: (S)-4-(3-(2'-[11C]isopropylamino)-2-hydroxypropoxy)-2H-benzimidazol-2-one] and qualitatively in lung [[11C]VC002: N-[11C]-methyl-piperidin-4-yl-2-cyclohexyl-2-hydroxy-2-phenylacetate and [11C]CGP12177].
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CAS 81047-99-6 CGP 12177

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