CGP 12177 hydrochloride

Names

[ Name ]:
CGP 12177 hydrochloride

Biological Activity

[Description]:

CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[Target]

Beta-1 adrenergic receptor

Beta-2 adrenergic receptor

Beta-3 adrenergic receptor

α1-adrenergic receptor

[References]

[1]. Leblais V, et al. Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A, on the contraction of rat intrapulmonary artery. J Pharmacol Exp Ther. 2004 Apr;309(1):137-45.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₄H₂₂ClN₃O₃

[ Molecular Weight ]:
315.80

[ Exact Mass ]:
315.13500

[ PSA ]:
90.14000

[ LogP ]:
2.17690

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

ALpha1-adrenoceptor antagonist properties of CGP 12177A and other beta-adrenoceptor ligands: evidence against beta(3)- or atypical beta-adrenoceptors in rat aorta.

Br. J. Pharmacol. 142 , 781-787, (2004)

1. The alpha(1)-adrenoceptor antagonist properties of the beta-adrenoceptor nonconventional partial agonist, CGP 12177A, was investigated in functional assays in rat aorta and in radioligand binding a...

Contribution of beta-adrenoceptor subtypes to relaxation of colon and oesophagus and pacemaker activity of ureter in wildtype and beta(3)-adrenoceptor knockout mice.

Br. J. Pharmacol. 130 , 747-758, (2000)

The smooth muscle relaxant responses to the mixed beta(3)-, putative beta(4)-adrenoceptor agonist, (-)-CGP 12177 in rat colon are partially resistant to blockade by the beta(3)-adrenoceptor antagonist...

The effects of beta-adrenoceptor agonists on KCl-induced rhythmic contraction in the ureter of guinea pig.

J. Smooth Muscle Res. 36 , 13-19, (2000)

In the present study, we tried to determine what effects were induced by beta-adrenoceptor agonists on 40 mM KCl-induced rhythmic contraction and to clarify which beta-adrenoceptor subtypes are involv...

Related Compounds

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