(+/-) CGP 12177A Struktur

(+/-) CGP 12177A

Bezeichnung:(+/-) CGP 12177A

CAS-Nr64208-32-8

Englisch Name:(+/-) CGP 12177A

CBNumberCB7972328

SummenformelC14H21N3O3.ClH

Molgewicht315.799

MOL-Datei64208-32-8.mol

(+/-) CGP 12177A physikalisch-chemischer Eigenschaften

storage temp.	Store at RT
Löslichkeit	DMSO: >10mg/mL
Aggregatzustand	solid
Farbe	white
Wasserlöslichkeit	Soluble to 50 mM in water

Sicherheit

WGK Germany

(+/-) CGP 12177A Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
CGP 12177 Hydrochloride is a selective β3-adrenoceptor agonist.
Biologische Aktivität
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].
Lager
Store at RT
Einzelnachweise
[1]. treinys r, zablockaitė d, gendvilienė v, et al. β₃-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.

(+/-) CGP 12177A Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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