SR 59230A hydrochloride - CAS 1135278-41-9
Category: Inhibitor
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Molecular Formula:
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Adrenergic Receptor
SR 59230A hydrochloride is a potent, selective and orally available β3 adrenoceptor antagonist (IC50 = 40, 408 and 648 nM for β3, β1 and β2 receptors, respectively). SR 59230A blocks MDMA-induced hyperthermia at low concentrations, while it blocks hyperthermia and also increases heat loss through an α1-AR antagonistic mechanism at high concentrations.
Brife Description:
β3 adrenoceptor antagonist
≥98% by HPLC
Related CAS:
174689-39-5 (free base)
SR 59230A hydrochloride; SR59230A hydrochloride; SR-59230A hydrochloride; 1-(2-Ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanol hydrochloride; (2S)-1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]amino]propan-2-ol hydrochloride
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1.Relaxations to beta-adrenoceptor subtype selective agonists in wild-type and NOS-3-KO mouse mesenteric arteries.
Al Zubair K;Bexis S;Docherty JR Eur J Pharmacol. 2008 Jun 10;587(1-3):216-23. doi: 10.1016/j.ejphar.2008.03.018. Epub 2008 Mar 29.
We have investigated the role of nitric oxide (NO) in relaxations to beta-adrenoceptor agonists in mesenteric artery from wild-type (WT) and NO synthase-3 knockout (NOS-3-KO) mice. Isoprenaline, formoterol and BRL 37344 ((R(),R())-(+/-)-4-[2-[(2-(3-chlorophenyl)-2-hydroxyethyl)amino]propyl]phenoxyacetic acid) were chosen as non-selective and beta(2)- and beta(3)-adrenoceptor agonists, respectively. Atenolol, ICI 118,551 ((+/-)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride) and SR59230A (1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanol hydrochloride) were chosen as selective beta(1)-, beta(2)- and beta(3)-adrenoceptor antagonists, respectively. Experiments employing isoprenaline were carried out in the presence of prazosin (0.1 microM). Isoprenaline produced relaxations with a potency of 5.68+/-0.36 (-log M, n=6) in WT mice. Relaxations to isoprenaline were blocked by atenolol (10 microM) and were absent in vessels from NOS-3-KO animals. Formoterol produced relaxations with two components. ICI 118,551 (1 microM) abolished relaxations to low concentrations of formoterol (0.1-10 microM), but failed to affect relaxations to formoterol (100 microM).
2.Evidence for a secondary state of the human beta3-adrenoceptor.
Baker JG Mol Pharmacol. 2005 Dec;68(6):1645-55. Epub 2005 Aug 29.
There are three members of the beta-adrenoceptor family, all of which are primarily coupled to G(s) proteins. Recent studies using the huge range of beta-ligands now available have given remarkable new insights into their pharmacology. beta1-adrenoceptors exist in at least two active conformations, whereas beta2-adrenoceptors are able to induce signaling via different agonist-induced receptor conformational states, and their affinity for antagonists can be altered by highly efficacious agonists. This study therefore examined the pharmacology of the human beta3-adrenoceptor stably expressed in Chinese hamster ovary cells. Several compounds described previously as beta-antagonists have agonist properties at the beta3-adrenoceptor. Antagonist affinity measurements varied at the beta3-adrenoceptor in a manner similar to those observed at human beta1-adrenoceptors and unlike those seen at beta2-adrenoceptors. Some ligands (e.g., fenoterol and cimaterol) were more readily inhibited by all antagonists, whereas other ligands [e.g., alprenolol and 1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanol hydrochloride [SR 59230A]) stimulated responses that were more resistant to antagonism.
3.Role of alpha 1- and beta 3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse.
Bexis S;Docherty JR Br J Pharmacol. 2009 Sep;158(1):259-66. doi: 10.1111/j.1476-5381.2009.00186.x. Epub 2009 Apr 30.
BACKGROUND AND PURPOSE: ;We have investigated the ability of the beta(3)-adrenoceptor antagonist 1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4,-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanol hydrochloride (SR59230A) to affect the hyperthermia produced by methylenedioxymethamphetamine (MDMA) in conscious mice and whether alpha(1)-adrenoceptor antagonist actions are involved.;EXPERIMENTAL APPROACH: ;Mice were implanted with temperature probes under anaesthesia, and allowed 2 week recovery. MDMA (20 mg x kg(-1)) was administered subcutaneously 30 min after vehicle or test antagonist and effects on body temperature monitored by telemetry.;KEY RESULTS: ;Following vehicle, MDMA produced a slowly developing hyperthermia, reaching a maximum increase of 1.8 degrees C at 130 min post injection. A low concentration of SR59230A (0.5 mg x kg(-1)) produced a small but significant attenuation of the slowly developing hyperthermia to MDMA. A high concentration of SR59230A (5 mg x kg(-1)) revealed a significant and marked early hypothermic reaction to MDMA, an effect that was mimicked by the alpha(1)-adrenoceptor antagonist prazosin. Functional and ligand binding studies revealed actions of SR59230A at alpha(1)-adrenoceptors.
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CAS 1135278-41-9 SR 59230A hydrochloride

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