| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T51408 | ||||
| Target Name | Adrenergic receptor beta-3 (ADRB3) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Amibegron | Drug Info | IC50 = 10 nM | [4] | |
| L-751250 | Drug Info | IC50 = 6 nM | [5] | ||
| 1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol | Drug Info | Ki = 4 nM | [3] | ||
| 1-(2-allylphenoxy)-3-morpholinopropan-2-ol | Drug Info | Ki = 4960 nM | [2] | ||
| 1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol | Drug Info | Ki = 1770 nM | [2] | ||
| BMS-196085 | Drug Info | Ki = 21 nM | [1] | ||
| Action against Disease Model | Amibegron | Drug Info | The beta3 adrenoceptor agonist, amibegron (SR58611A) counteracts stress-induced behavioral and neurochemical changes. Under basal conditions (no previous exposure to stressors),different groups of male Wistar rats received acutely or repeatedly (once/day for 7days) intraperitoneal (i.p.) injections of amibegron (1, 5 and 10 mg/kg), the tricyclic antidepressant (TCA) clomipramine (50 mg/kg), the selective serotonin reuptake inhibitor (SSRI) citalopram (15 mg/kg) or their vehicles. The influence of stress-related conditions was studied in rats subjected to acute (4h) or repeated (4h/day for 7days) restraint stress, applied prior to the FST procedure. | [6] | |
| References | |||||
| REF 1 | Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4290-6. | ||||
| REF 2 | A vHTS approach for the identification of beta-adrenoceptor ligands. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. | ||||
| REF 3 | Synthesis and beta-adrenergic receptor blocking potency of 1-(substituted amino)-3-(4-indolyloxy)propan-2-ols. J Med Chem. 1986 Aug;29(8):1524-7. | ||||
| REF 4 | Stimulation of beta(3)-adrenoceptors causes phosphorylation of p38 mitogen-activated protein kinase via a stimulatory G protein-dependent pathway in 3T3-L1 adipocytes. Br J Pharmacol. 2002 Feb;135(4):951-60. | ||||
| REF 5 | Recent advances in cyclin-dependent kinase inhibition. Purine-based derivatives as anti-cancer agents. Roles and perspectives for the future. Curr Top Med Chem. 2002 Sep;2(9):1037-50. | ||||
| REF 6 | The beta3 adrenoceptor agonist, amibegron (SR58611A) counteracts stress-induced behavioral and neurochemical changes. Eur Neuropsychopharmacol. 2010 Oct;20(10):704-13. | ||||
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