L-755,507

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Background

IC50: 13 nM (binding at the human β3 adrenergic receptor) [1]Benzenesulfonamide derivative L-755,507 is a partial agonist for the human β3 receptor, with maximal activation 52% of that evoked by isoproterenol [2]. β3 adrenergic receptor is a G protein-coupled receptors which can enhancement of lipolysis in adipose tissue.In vitro: L-755,507 displays an excellent activity profile as an extremely potent human β3 adrenergic receptor agonist (β3 EC50 0.43 nM), with >440-fold selectivity over β1 and β2 binding [1]. L-755,507 is also a potent and selective b3 partial agonist in rhesus monkeys as assessed by its affinity for the cloned b adrenergic receptors, and stimulates lipolysis in rhesus adipocytes with an EC50 = 3.9 nM [2].In vivo: Dose rhesus monkeys with L-755,507 elicits lipolysis and metabolic rate elevation. The ED50 for glycerolemia was 0.03 mg/kg and the ED50 for tachycardia was 2.5 mg/kg, and stimulates metabolic rate by ~ 30% after acute bolus intravenous administration of 0.1 mg/kg [2].Clinical trial: So far, no clinical study has been conducted.

[1] Parmee ER, Ok HO, Candelore MR, Tota L, Deng L, Strader CD, Wyvratt MJ, Fisher MH, Weber AE. Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. Bioorg Med Chem Lett. 1998 May 5;8(9):1107-12.
[2] Fisher MH, Amend AM, Bach TJ, Barker JM, Brady EJ, Candelore MR, Carroll D, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hegarty-Friscino B, Guan XM, Hom GJ, Hutchins JE, Kelly LJ, Mathvink RJ, Metzger JM, Miller RR, Ok HO, Parmee ER, Saperstein R, Strader CD, Stearns RA, MacIntyre DE, et al. A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. J Clin Invest. 1998 Jun 1;101(11):2387-93.