β3-agonists bind ADRB3

Stable Identifier
R-HSA-9611839
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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The β3-adrenergic receptor (ADRB3) is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis (Cernecka et al. 2014, Bhadada et al. 2011). ADRB3 can also be found in the vasculature, the heart (Rozec & Gauthier 2006), gallbladder and urinary bladder, where in the latter it is involved in smooth muscle relaxation (Andersson et al. 2013). Drugs such as solabegron (Schemann et al. 2010) and mirabegron (Gras 2012, Nitti et al. 2013) that act as β3-agonists are commonly used in the treatment of patients with overactive bladders. The potent and selective β3-agonist drug vibegron has recently been approved for use in patients with overactive bladder in Japan only (Edmondson et al. 2016, Di Salvo et al. 2017, Yoshida et al. 2018a, b). Using β3-agonists to treat obesity and diabetes may have cardiac side effects, especially in patients with congestive heart failure. They cause vasodilation of microvessels in the islets of Langerhans and may participate in the pathogenesis of cardiac failure, during which modification of β1- and β2-adrenoceptor expression occurs. Since there are two types of ADRB3 (β3a and β3b), it may be possible to develop subtype-specific drugs that are more effective and have fewer side effects than those currently available.

Literature References
PubMed ID Title Journal Year
24890609 The odd sibling: features of β3-adrenoceptor pharmacology

Cernecka, H, Sand, C, Michel, MC

Mol. Pharmacol. 2014
23148172 β(3) Receptors: Role in Cardiometabolic Disorders

Bhadada, SV, Patel, BM, Mehta, AA, Goyal, RK

Ther Adv Endocrinol Metab 2011
27965369 Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder

Di Salvo, J, Nagabukuro, H, Wickham, LA, Abbadie, C, DeMartino, JA, Fitzmaurice, A, Gichuru, L, Kulick, A, Donnelly, MJ, Jochnowitz, N, Hurley, AL, Pereira, A, Sanfiz, A, Veronin, G, Villa, K, Woods, J, Zamlynny, B, Zycband, E, Salituro, GM, Frenkl, T, Weber, AE, Edmondson, SD, Struthers, M

J. Pharmacol. Exp. Ther. 2017
16480771 beta3-adrenoceptors in the cardiovascular system: putative roles in human pathologies

Rozec, B, Gauthier, C

Pharmacol. Ther. 2006
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