β3-adrenergic receptor

ICI 118,551 hydrochloride (ICI 118551 hydrochloride) is a highly selective β2 adrenergic receptor antagonist (Kis: 0.7, 49.5, and 611 nM for β2, β1, and β3 receptors).

L748337 is a competitive and potent β3-adrenoceptor antagonist that inhibits the action of β3-, β2-, and β1-adrenoceptors, activates MAPK signaling, promotes phosphorylation of Erk1 2, and inhibits the protective effects of CL316243, and is used in the study of disorders caused by abnormalities of the β3-adrenoceptors.

CL316243 is a highly potent selective agonist of β3-adrenoceptor, with a EC50 of 3 nM. CL316243 is an effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.

LY377604 is a human β3-adrenergic receptor agonist (EC50: 2.4 nM) and β1 2-adrenergic receptor antagonist for the study of obesity.

Talibegron hydrochloride (ZD2079 hydrochloride) is a β3 adrenergic receptor agonist with a pD2 of 3.72 on phenylephrine-preconstricted rat mesenteric artery. It relaxes rat mesenteric artery and isolated aorta in vitro, and inhibits ob gene expression and circulating leptin levels in lean mice in vivo.

N-5984, a β3-adrenergic receptor agonist, is used potentially for the treatment of obesity, overactive bladder and type 2 diabetes.

Rafabegron (TAK677) is a potent and selective β3 adrenergic receptor agonist for the study of diabetes and obesity.

Ritobegron (KUC-7483), an effective and selective β3-adrenergic receptor agonist, shows effective β(3)-AR agonist activity on transfected human β-AR and has an effect on the bladder of rats Shows high selectivity with other organs.

Mirabegron (YM178) is a beta-3 adrenergic agonist that is used for treatment of overactive bladder syndrome.

Salmeterol Xinafoate (GR 33343X xinafoate) is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.

(S)-(-)-Propranolol hydrochloride, an adrenergic receptor antagonist, exhibits potential anticancer activity and may enhance the prognosis of burn patients.

ICI-118551 Hydrochloride (ICI-118,551) is a highly selective β2-adrenergic receptor antagonist with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

β3-AR agonist 1 is a highly selective, and orally available agonist of β3-adrenergic receptor (EC50: 18 nM), being inactive to β1-, β2-, and α1A-AR (β1 β3, β2 β3, and α1A β3>556-fold).

BRL 37344 sodium is a specific agonist of the β3-adrenergic receptor. The treatment of BRL 37344 sodium significantly lowers the bodyweight of obese mice.

β3-AR agonist 2 is a potent and selective agonist of β3-adrenergic receptor (β3-AR with an EC50 of 8 nM).

Salmeterol (GR33343X) is a long-acting agonist of beta2-adrenergic receptor (beta 2AR) used for treatment ofasthma.

Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist that promotes cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR (EC50: 22 nM). It is used to treat overactive bladder and irritable bowel syndrome.

SR59230A is a potent, selective antagonist of β3-adrenergic receptor(β3, β1, and β2 receptors with IC50s of 40, 408, and 648 nM , respectively).

SR59230A hydrochloride (SR59230A HCl) is a blood-brain permeable, selective and highly potent β3-adrenergic receptor antagonist that inhibits ultradian brown adipose tissue thermogenesis and interrupts associated paroxysmal brain and body heating.

SAR-150640, a selective β3-adrenergic receptor agonist, prevents an increase in MMP activity and production observed after LPS stimulation or in cases of chorioamnionitis.

Talibegron (ZD2079) is a β3-adrenergic receptor agonist that also enhances insulin sensitivity.

Ritobegron (also known as KUC-7483) is a potent and selective β3-adrenergic receptor agonist. In studies involving transfected human β-AR, Ritobegron exhibits significant and selective agonistic activity towards β(3)-AR. In rats, it shows high selectivity for the bladder over other organs. In anesthetized rats, Ritobegron effectively reduces bladder pressure with minimal impact on the cardiovascular system. It holds potential as a compound for treating overactive bladder.

LY 377604 is an innovative compound functioning as a mixed β3-adrenergic receptor agonist and β1 β2-adrenergic receptor antagonist, showing potential for antidiabetic and anti-obesity effects. In rodent models, LY 377604 has been found to enhance energy expenditure and fat oxidation, reduce blood glucose levels, and induce weight loss while preserving lean body mass. A phase II clinical trial for obesity has been conducted in the United States.

L-796568 free base is a β3 adrenergic receptor agonist potentially for the treatment of obesity. L-796568 is a potent full beta(3) agonist (EC50: 3.6 nM). It has 600-fold selectivity over the human beta(1) and beta(2) receptors.