5-[(2R)-2-([(2R)-2-(3-CHLOROPHENYL)-2-HYDROXYETHYL]AMINO)PROPYL]-1,3-BENZODIOXOLE-2,2-DICARBOXYLATE DISODIUM

Description

CL-316243 (151126-84-0) is a potent and selective β3-adrenergic receptor agonist. (EC50= 3 nM) Displays anti-obesity and anti-diabetic effects in mice. It increases brown fat thermogenesis and metabolic rate and decreases blood insulin and glucose levels.1?CL-316243 induces functionally active mitochondrial uncoupling protein (UCP) in white fat.2?Active?in vivo.

Uses

CL 316243 Disodium Salt is a potent and highly selective β3-adrenoceptor agonist.

Biological Activity

Potent and highly selective β 3 -adrenoceptor agonist (EC 50 = 3 nM); > 10000-fold selective over β 1 and β 2 receptors. Increases brown adipose tissue thermogenesis and metabolic rate, and decreases blood insulin and glucose levels following oral administration in vivo .

in vitro

the compound was a potent stimulant of rat adipocyte lipolysis (β3 effect, ec50 = (3.0±0.3) x 10-8 m), had no effect on the rate of contraction of guinea pig atria (β1 effect, ec50 > 10-4 m), and had only a very limited ability to inhibit insulin-stimulated [14c] glucose incorporation into glycogen in isolated rat soleus muacle (β2 effect, ic50 = (3.0±1.0) x 10-5 m) [1].

in vivo

in rat, cl-316,243 treatment resulted in increased growth rates and significant changes in food consumption at the end of the 10-day treatment period. cl-316,243 treatment increased insulin responsiveness and sensitivity in non-insulin-resistant rodent species. the cl-316,243 induced increases in whole-body glucose disposal were due entirely to increases in adipose tissue glucose uptake, while muscle glucose uptake remained unaltered [2].

References

1) Yoshida?et al. (1994),?Anti-obesity and anti-diabetic effects of CL 316,243, a highly specific beta 3-adrenoceptor agonist in yellow KK mice; Life Sci.,?54?491 2) Yoshida?et al. (1998),?β3-Adrenergic agonist induces a functionally active uncoupling protein in fat and slow-twitch muscle fibers; Am. J. Physiol.,?274?E469