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Amibegron hydrochloride

Catalog No. T10302   CAS 121524-09-2
Synonyms: SR 58611A

Amibegron hydrochloride is a selective β3-adrenoceptor agonist (EC50: 3.5 nM for β-adrenoceptor in rat colon). It has anxiolytic and antidepressant activity.

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Amibegron hydrochloride Chemical Structure
Amibegron hydrochloride, CAS 121524-09-2
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 931.00
50 mg 6-8 weeks $ 1,210.00
100 mg 6-8 weeks $ 1,830.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Amibegron hydrochloride is a selective β3-adrenoceptor agonist (EC50: 3.5 nM for β-adrenoceptor in rat colon). It has anxiolytic and antidepressant activity.
Targets&IC50 β-adrenoceptor: 499 nM , β-adrenoceptor:(EC50)3.5 nM
In vitro Amibegron hydrochloride (SR 58611A) is a selective β-adrenoceptor agonist (EC50: 499 nM in rat uterus) [1]. Amibegron hydrochloride shows little effect on β1- and β2-adrenoceptors, 5-HT uptake, noradrenaline (NA) uptake, and dopamine (DA) uptake from rat brain tissue (IC50s: 4.6 and 1.2, 0.58, 2.5 and 3.2 μM). It exhibits no effect on 5-HT1A, 5-HT2, MAO-A, and MAO-B (IC50 > 10 μM) [2].
In vivo Amibegron hydrochloride (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 [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. In addition, Amibegron hydrochloride (10 mg/kg, p.o.) promotes the release of 5-HT in the 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].
Synonyms SR 58611A
Molecular Weight 440.36
Formula C22H27Cl2NO4
CAS No. 121524-09-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Bianchetti A, et al. In vitro inhibition of intestinal motility by phenylethanolaminotetralines: evidence of atypical beta-adrenoceptors in rat colon. Br J Pharmacol. 1990 Aug;100(4):831-9. 2. Simiand J, et al. Antidepressant profile in rodents of SR 58611A, a new selective agonist for atypical beta-adrenoceptors. Eur J Pharmacol. 1992 Aug 25;219(2):193-201. 3. Claustre Y, et al. Effects of the beta3-adrenoceptor (Adrb3) agonist SR58611A (amibegron) on serotonergic and noradrenergic transmission in the rodent: relevance to its antidepressant/anxiolytic-like profile. Neuroscience. 2008 Oct 2;156(2):353-64.

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Keywords

Amibegron hydrochloride 121524-09-2 Others SR 58611A Amibegron Hydrochloride inhibitor inhibit

 

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