SR59230A is a potent and selective Adrenergic Receptor β3 antagonist with IC50 values of 40, 408, and 648nM for Adrenergic Receptor β3, β1 and β2, respectively. It shows blood-brain barrier penetrability.
Β3-adrenoceptor is the last identified member of adrenergic receptors, involved in different tumor conditions, such as melanoma[1]. SR59230A is a potent and selective β3-adrenoceptor antagonist with IC50 values of 40, 408, and 648 nM for β3-, β1-, and β2-receptors, respectively[2]. In the NB (neuroblastoma) cell lines, treatment with SR59230A for 24 h was able to reduce cell viability in a dose-dependent manner[1]. In 24-h fasted Wistar rats, both doses (10, 50 nmol) of SR59230A reduced the risk assessment (RA) frequency (number/30 min) (4 ± 2 for saline-treated vs 1 ± 1 for 10 nmol and 0.5 ± 1 for 50 nmol SR59230A-treated rats), an ethological parameter related to anxiety. Further, pretreatment with SR59230A (7.0 ± 0.5 g) abolished the hypophagia induced by BRL37344 (3.6 ± 0.9 g, agonist of β3-adrenoceptor)[2].
搜索
