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Datasheet Inhibitors / Agonists / Screening Libraries a DRUG SCREENING EXPERT Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT Product Name : Amibegron hydrochloride Catalog Number : T10302 CAS Number : 121524-09-2 Molecular Formula : C22H27Cl2NO4 Molecular Weight : 440.36 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. Storage: 2 years -80°C in solvent; 3 years -20°C powder; Receptor (IC50) β-adrenoceptor 499 nM In vitro Activity 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 Activity 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]. Reference 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. FOR RESEARCH PURPOSES ONLY. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE. Information for product storage and handling is indicated on the product datasheet. Targetmol products are stable for long term under the recommended storage conditions. Our products may be shipped under different conditions as many of them are stable in the short-term at higher or even room temperatures. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, please follow the storage recommendations on the product data sheet. [email protected] | Tel: +1-781-999-4286 | www.targetmol.com.
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