| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T51408 | ||||
| Target Name | Beta-3 adrenergic receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | 1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol | Drug Info | Ki = 4 nM | [533374] | |
| Amibegron | Drug Info | IC50 = 10 nM | [552285] | ||
| BMS-196085 | Drug Info | Ki = 21 nM | [528868] | ||
| 1-(2-allylphenoxy)-3-morpholinopropan-2-ol | Drug Info | Ki = 4960 nM | [530883] | ||
| 1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol | Drug Info | Ki = 1770 nM | [530883] | ||
| L-751250 | Drug Info | IC50 = 6 nM | [552307] | ||
| Action against Disease Model | Amibegron | 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. | [553055] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Decreased metabolic rate;increased weight and body fat | [533374] | |||
| References | |||||
| Ref 533374 | J Med Chem. 1986 Aug;29(8):1524-7.Synthesis and beta-adrenergic receptor blocking potency of 1-(substituted amino)-3-(4-indolyloxy)propan-2-ols. | ||||
| Ref 552285 | 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 528868 | Bioorg Med Chem Lett. 2007 Aug 1;17(15):4290-6. Epub 2007 May 16.Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations. | ||||
| Ref 553055 | The beta3 adrenoceptor agonist, amibegron (SR58611A) counteracts stress-induced behavioral and neurochemical changes. Eur Neuropsychopharmacol. 2010 Oct;20(10):704-13. doi: 10.1016/j.euroneuro.2010.04.006. Epub 2010 May 26. | ||||
| Ref 530883 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands. | ||||
| Ref 530883 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands. | ||||
| Ref 552307 | 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. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.