SR 59230A was used in the identification of β-adrenoceptors in rat aorta.3 It was tested as a potential therapeutic agent in improving cardiac function in rat model of heart failure.4
Potent and selective β 3 adrenoceptor antagonist (IC 50 values are 40, 408 and 648 nM for β 3 , β 1 and β 2 receptors respectively). Orally active in vivo . Also available as part of the β -Adrenoceptor Antagonist Tocriset™ .
SR 59230A is a β3-adrenoceptor antagonist. It has high affinity for the β3 adrenoceptors occurring in human gut that affect the function of human colonic circular smooth muscle.1 It is reported that SR 59230A inhibits the Kir2.1-2.3 cardiac potassium channels.2
MDMA (20 mg/kg) produces a slowly developing hyperthermia, reaching a maximum increase of 1.8°C 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].
| Animal Model: | Male C-57BL6J wild-type mice (22-35 g)[4] |
| Dosage: | 0.5 or 5 mg/kg |
| Administration: | Injected s.c.; administered 30 min prior to the injection s.c. of MDMA (20 mg/kg). |
| Result: | Modulated the actions of MDMA on temperature involve α1-adrenoceptor antagonism. |
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