| Identification | Back Directory | [Name]
(+/-) CGP 12177A | [CAS]
64208-32-8 | [Synonyms]
CGP12177A HCl
(+/-) CGP 12177A
4-(3-(tert-Butylamino)-2-hydroxypropoxy)-1H-benzo[d]imidazol-2(3H)-one hydrochloride
(±)-CGP-12177 hydrochloride, 4-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-1, 3-dihydro-2H-benzimidazol-2-one hydrochloride | [Molecular Formula]
C14H21N3O3.ClH | [MDL Number]
MFCD00069230 | [MOL File]
64208-32-8.mol | [Molecular Weight]
315.799 |
| Hazard Information | Back Directory | [Uses]
CGP 12177 Hydrochloride is a selective β3-adrenoceptor agonist. | [Biological Activity]
cgp 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors with ki values of 0.9, 4 and 88 nm for β1-, β2- and β3-adrenoceptors, respectively.β3-adrenoceptor is exists mainly in adipose tissue and plays an important role in the regulation of thermogenesis and lipolysis.cgp 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors. in human ventricular myocytes (hvms), cgp12177 slightly activated l-type ca2+ current (ica,l) [1].in sympathectomized (sx) interscapular brown adipose tissue (bat) isolated from rats, cgp-12177 restored normal thyroxine (t4) deiodination, which suggested that cgp-12177 activated 5’-deiodinase type ii through β3-adrenoceptor [2]. in spontaneously hypertensive rats (shr) and normotensive rats, cgp12177 induced vasorelaxant effects and decreased hindquartersperfusion pressure in a dose-dependent way induced by 5-hydroxytryptamine (5-ht), which was inhibited by bupranolol, a β1la-adrenoceptor antagonist. these results suggested that cgp12177 induced vasorelaxant effects through activation of β1la-adrenoceptor [3]. | [IC 50]
Beta-1 adrenergic receptor; Beta-2 adrenergic receptor; Beta-3 adrenergic receptor; α1-adrenergic receptor | [storage]
Store at RT | [References]
[1]. treinys r, zablockait? d, gendvilien? v, et al. β?-adrenergic regulation of l-type ca2? current and force of contraction in human ventricle. j membr biol, 2014, 247(4): 309-318.
[2]. hofer d, raíces m, schauenstein k, et al. the in vivo effects of beta-3-receptor agonist cgp-12177 on thyroxine deiodination in cold-exposed, sympathectomized rat brown fat. eur j endocrinol, 2000, 143(2): 273-277.
[3]. holopherne d, mallem my, le strat e, et al. cgp12177-induced haemodynamic and vascular effects in normotensive and hypertensive rats. eur j pharmacol, 2008, 591(1-3): 196-202. |
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