Samples

LES smooth muscles

Preparation method

The solubility of this compound in sterile water is 100 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months.

Reacting condition

0.01 ~ 300 μM

Applications

CL 316243 concentration-dependently decreased the basal tension of the LES smooth muscle, with an ECmax value of 1 × 10-4 M. At corresponding ECmax values, the smooth muscle relaxation induced by CL 316243 was significantly longer than that triggered by isoproterenol. The smooth muscle relaxation in the isoproterenol group began to recover within 5 mins but it cost 1 hr in the case of CL 316243.

Animal models

Nonobese and nondiabetic Sprague-Dawley rats

Dosage form

1 mg/kg/day; s.c.; for 10 ~ 12 days

Applications

After 7 days of treatment, CL 316243 significantly increased food consumption, resting metabolic rates, as well as body core temperatures in rats. Besides, CL 316243 decreased the respiratory quotient by 14%. On day 11, an oral glucose load (2 g/kg) did not alter plasma glucose and insulin excursions. In addition, CL 316243 reduced abdominal and epididymal white fat pad weights, but doubled interscapular brown adipose tissue weight at the same time.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

• Toxicology (2021): 153014. PMID:34718029

EC50: (3.0±0.3) X 10-8 M for β3 adrenoceptor [1].

Benzodioxole-containing phenethanolamine CL-316,243 is a murine-selective β3 adrenoceptor agonist which can correct obesity and elevated blood glucose in diabetic rodents, which offers an exciting possibility for the treatment of non-insulin-dependent diabetes as well as obesity without undesired β-mediated side effects [3]. β3 adrenoceptor is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis.

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].

Clinical trial: So far, no clinical study has been conducted.