BRL 37344, sodium salt

BRL 37344, sodium salt是一种强效的和选择性的β3肾上腺素受体激动剂,作用于β3\β1和β2受体的Ki值分别为287\1750和1120 nM [1].

β3肾上腺素受体主要存在于脂肪组织中,并在产热和脂肪分解的调节中起重要作用.

BRL 37344, sodium salt是一种强效的和选择性的β3肾上腺素受体激动剂.在分离的大鼠褐色和白色脂肪细胞中,BRL 37344显著刺激脂解作用,在褐色脂肪细胞和白色脂肪细胞中的EC50值分别为5和56 nM [1].在离体豚鼠心脏中,BRL 37344(10-8-10-5 M)增加心脏收缩(dP/dt)和冠脉流量(CF).然而,BRL 37344(10 -8 M)完全抑制异丙肾上腺素诱导的收缩增加,这表明BRL 37344显示β1-拮抗特性[2].

在禁食兔中,BRL 37344通过β3肾上腺素受体显著增加血浆非酯化脂肪酸(NEFA)水平.然而,BRL 37344对血浆葡萄糖水平没有影响[3].在小鼠中,BRL 37344通过活化β3肾上腺素受体增加循环转氨酶水平[4].

参考文献：
[1].  Simard PM, Atgié C, Mauriège P, et al. Comparison of the lipolytic effects of norepinephrine and BRL 37344 in rat brown and white adipocytes. Obes Res, 1994, 2(5): 424-431.
[2].  Kozlovski VI, Chlopicki S, Gryglewski RJ. Effects of two beta3-agonists, CGP 12177A and BRL 37344, on coronary flow and contractility in isolated guinea pig heart. J Cardiovasc Pharmacol, 2003, 41(5): 706-713.
[3].  Reverte M, Rivas-Cabaero L. Effects of the beta 3-adrenoceptor agonist BRL 37344 on lipomobilization and plasma glucose levels in conscious fasted rabbits. Can J Physiol Pharmacol, 1996, 74(3): 251-256.
[4].  Kasahara H, Muto S, Motokawa Y, et al. β3-adrenoceptor-mediated increased circulating transaminase levels in mice treated with its agonist BRL 37344. J Toxicol Sci, 2010, 35(5): 779-784.