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SR 59230A HCl

Product Name
SR 59230A HCl
CAS No.
1135278-41-9
Chemical Name
SR 59230A HCl
Synonyms
SR-59230A hydrochloride,SR59230A hydrochloride;SR 59230A hydrochloride, beta3 adrenoceptor antagonist
CBNumber
CB33038511
Molecular Formula
C21H27NO2.HCl
Formula Weight
361.91
MOL File
1135278-41-9.mol
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SR 59230A HCl Property

storage temp. 
Store at 4°C
solubility 
Soluble in DMSO
form 
solid
color 
White
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21407
Product name
SR 59230A (hydrochloride)
Purity
≥99%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
21407
Product name
SR 59230A (hydrochloride)
Purity
≥99%
Packaging
5mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
21407
Product name
SR 59230A (hydrochloride)
Purity
≥99%
Packaging
10mg
Price
$195
Updated
2024/03/01
Cayman Chemical
Product number
21407
Product name
SR 59230A (hydrochloride)
Purity
≥99%
Packaging
25mg
Price
$442
Updated
2024/03/01
TRC
Product number
S684443
Product name
SR59230AHydrochloride
Packaging
10mg
Price
$145
Updated
2021/12/16
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SR 59230A HCl Chemical Properties,Usage,Production

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 RT

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

SR 59230A HCl Preparation Products And Raw materials

Raw materials

Preparation Products

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1135278-41-9, SR 59230A HClRelated Search:


  • SR-59230A hydrochloride,SR59230A hydrochloride
  • SR 59230A hydrochloride, beta3 adrenoceptor antagonist
  • 1135278-41-9