2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. 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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Amibegron Chemical Structure

Amibegron Chemical Structure

CAS No. : 121524-08-1

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Amibegron Related Antibodies

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Description

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.

IC50 & Target

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]
In Vitro

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.

Amibegron Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

403.90

Formula

C22H26ClNO4
CAS No.
SMILES

O[C@H](C1=CC(Cl)=CC=C1)CN[C@@H]2CC3=CC(OCC(OCC)=O)=CC=C3CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Amibegron Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Amibegron121524-08-1SR-58611SR58611SR 58611Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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