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.

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.

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

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

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.

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

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.

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.

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

L-796568, is a β3 adrenergic receptor agonist. L-796568 is a potent full beta(3) agonist (EC(50) = 3.6 nM, 94% activation) with >600-fold selectivity over the human beta(1) and beta(2) receptors, which also displays good oral bioavailability in several

KUL-7211 is an β2 and β3 adrenergic receptor agonist. KUL-7211 is a potent ureteral relaxant with a relatively small hypotensive effect.

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

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.

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.

Zenidolol (ICI-118551), a selective β2 adrenergic receptor antagonist, demonstrates inhibition of β2-, β1-, and β3-adrenergic receptors with K i values of 0.7, 49.5, and 611 nM, respectively. It is employed as an ocular hypotensive agent in ophthalmic disease research.

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.

SB-206606 is a novel, highly specific radioactive ligand for the β3-adrenergic receptor.

Cyanopindolol is a β3-adrenergic receptor antagonist that also acts as a potent and selective antagonist at presynaptic serotonin autoreceptors in the rat cerebral cortex. It exhibits binding affinity for 5-HT1A and 5-HT1B receptors (Ki: 2.1 nM and 3 nM, respectively).

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.

Vemtoberant, a β3 Adrenergic Receptor antagonist, is utilized in the research of disorders mediated by the β3 adrenergic receptor, including heart failure.

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