| Identification | Back Directory | [Name]
SR 59230A HCl | [CAS]
1135278-41-9 | [Synonyms]
SR-59230A hydrochloride,SR59230A hydrochloride | [Molecular Formula]
C21H27NO2.HCl | [MDL Number]
MFCD06795851 | [MOL File]
1135278-41-9.mol | [Molecular Weight]
361.91 |
| Hazard Information | Back Directory | [Description]
SR 59230A (hydrochloride) is a β3-adrenergic receptor (β3-AR) antagonist (pA2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively). It is less selective for β3-AR in cells transfected with the human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively). At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism. In adipocytes, it induces phosphorylation of p38 MAPK via the Gs pathway. It has also been used in studies of heart failure to elucidate the role of the β3-ARs. | [Uses]
SR 59230A Hydrochloride is a potent and selective β3 adrenergic receptor antagonist. | [in vivo]
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. |
| [IC 50]
β adrenergic receptor | [storage]
Store at 4°C | [References]
[1] L MANARA. Functional identification of rat atypical beta-adrenoceptors by the first beta 3-selective antagonists, aryloxypropanolaminotetralins.[J]. British Journal of Pharmacology, 1996, 117 3: 435-442. DOI: 10.1111/j.1476-5381.1996.tb15209.x
[2] C HOFFMANN. Comparative pharmacology of human beta-adrenergic receptor subtypes–characterization of stably transfected receptors in CHO cells.[J]. Naunyn-Schmiedeberg’s archives of pharmacology, 2004, 369 2: 151-159. DOI: 10.1007/s00210-003-0860-y
[3] SOTIRIA BEXIS James R D. Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse[J]. British Journal of Pharmacology, 2009, 158 1: 259-266. DOI: 10.1111/j.1476-5381.2009.00186.x
[4] K. MIZUNO. Stimulation of β3‐adrenoceptors causes phosphorylation of p38 mitogen‐activated protein kinase via a stimulatory G protein‐dependent pathway in 3T3‐L1 adipocytes[J]. British Journal of Pharmacology, 2002, 135 1. DOI: 10.1038/sj.bjp.0704537
[5] RUN-TAO GAN. Chronic blocking of β3-adrenoceptor ameliorates cardiac function in rat model of heart failure[J]. Chinese Medical Journal, 2007, 120 1: 2250-2255. DOI: 10.1097/00029330-200712020-00018 |
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