Amibegron
Amibegron is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron has anxiolytic and antidepressant activity.
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- CAS. Nr.: 121524-08-1
- Formel: C22H26ClNO4
- Molecular Weight:403.90
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
EC50: 3.5 nM (β-adrenoceptor, from rat colon), 499 nM (β-adrenoceptor, from rat uterus)[1], 1.2 μM (β2-adrenoceptor, from cerebellum), 4.6 μM (β1-adrenoceptor1, from cortex)[2]
Amibegron is a selective β-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon, and 499 nM in rat uterus[1]. Amibegron hydrochloride (SR 58611A) shows little effect on β1- and β2-adrenoceptors, 5-HT uptake, noradrenaline (NA) uptake, and dopamine (DA) uptake from rat brain tissue, with IC50s of 4.6 and 1.2, 0.58, 2.5 and 3.2 μM, respectively; exhibits no effect on 5-HT1A, 5-HT2, MAO-A and MAO-B (IC50 > 10 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 121524-08-1
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Molecular Weight 403.90
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Formel C22H26ClNO4
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SMILES
O[C@H](C1=CC(Cl)=CC=C1)CN[C@@H]2CC3=CC(OCC(OCC)=O)=CC=C3CC2
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Synonyms
SR-58611
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
Mice[2]
This test is performed on groups of 10-20 mice. Amibegron hydrochloride (0.1 to 0.3 mg/kg) or vehicle are administered i.p. 30 min before the administration of yohimbine. Yohimbine hydrochloride is administered s.c. at a dose of 30 mg/kg always at the same time of day, between 1.30 and 3.30 p.m. Lethality is recorded the next morning at 9 a.m[2].
Rats[2]
The rats (n = 10 per group) are treated randomly according to one of the following protocols: the control sample, which receives no shock, is given vehicle; experimental animals with inescapable shock are treated daily with vehicle or Amibegron hydrochloride (up to 30 mg/kg). Animals are treated orally over 5 consecutive days, i.e. 6 h after shock pretreatment on day 1, and then twice per day, a half dose in the morning (30 min before shuttle-box session) and a half dose in the afternoon (except on the 5th day). Statistical analysis is performed on themean number of escape failures using a two-way analysis of variance followed by Dunnett's test[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)