Identification | Back Directory | [Name]
SR 58611A | [CAS]
121524-09-2 | [Synonyms]
SR 58611A SR 58611A hydrochloride Amibegron hydrochloride [[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydro-2-naphthalenyl]ox]yaceticacidethylesterhydrochloride Acetic acid, [[(7S)?-?7-?[[(2R)?-?2-?(3-?chlorophenyl)?-?2-?hydroxyethyl]?amino]?-?5,?6,?7,?8-?tetrahydro-?2-?naphthalenyl]?oxy]?-?, ethyl ester, hydrochloride (1:1) | [Molecular Formula]
C22H27Cl2NO4 | [MDL Number]
MFCD00886563 | [MOL File]
121524-09-2.mol | [Molecular Weight]
440.36 |
Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
DMSO: soluble20mg/mL, clear | [form ]
powder | [color ]
white to beige | [optical activity]
[α]/D -75 to -95°, c = 0.5 in methanol |
Hazard Information | Back Directory | [Uses]
SR 58611A is a selective β3-adrenergic receptor agonist with anxiolytic and antidepressant properties (1,2). SR 58611A is blood brain barrier permeable. | [Biochem/physiol Actions]
SR58611A is a potent, specific b3 adrenergic receptor agonist. The EC50 for reduction of β3-mediated spontaneous motility in rat distal colon sections is 3.5 nM. Minimal anti-depressant efficacious doses for SR58611A are 0.1-0.3 mpk in rodent models. | [in vivo]
Amibegron hydrochloride (SR 58611A, 0.1 to 0.3 mg/kg, i.p.) potentiates the toxicity produced by yohimbine in mice. Amibegron hydrochloride (0.6 and 2 mg/kg, i.p.) is also active in the learned helplessness model of antidepressant-like activity in rats. However, Amibegron hydrochloride exhibits no effect on the spontaneous locomotor activity of mice at up to 10 mg/kg and of rats at up tp 30 mg/kg[2]. Amibegron hydrochloride (3 and 10 mg/kg, p.o.) increases the synthesis of 5-HT and tryptophan (Trp) levels in several rodent brain areas such as cortex, hippocampus, hypothalamus, striatum. In addition, Amibegron hydrochloride (10 mg/kg, p.o.) promotes the release of 5-HT in rat prefrontal cortex. Systemic (3 mg/kg, i.v.) or chronic administration of SR58611A (10 mg/kg, p.o.) does not affect the activity of serotonergic neurons in the rat dorsal raphe nucleus[3]. | [IC 50]
β adrenergic receptor | [storage]
Desiccate at RT |
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