Biological Activity |
SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating beta3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for beta3, beta1, and beta2 receptors, respectively[2]. IC50 & Target: IC50: 40 nM (beta3 receptor), 408 nM ((beta1 receptor), 648 nM (beta2 receptor)[2] In Vitro: SR59230A (100 nM-50 uM; 24 hours) is able to reduce cell viability in a dose-dependent manner in Neuro-2A, BE(2)C and SK-N-BE(2) NB cell lines[3]. In Vivo: MDMA (20 mg/kg) produces a slowly developing hyperthermia, reaching a maximum increase of 1.8C at 130 min post injection. SR59230A (0.5 mg/kg) produces a small but significant attenuation of the slowly developing hyperthermia to MDMA. SR59230A (5 mg/kg) reveals a significant and marked early hypothermic reaction to MDMA[4]. |