Muscarinic receptor binding activity in rat tissues by vibegron and prediction of its receptor occupancy levels in the human bladder

• Published in: International journal of urology Vol. 28; no. 12; pp. 1298 - 1303
• Main Authors: Yamada, Shizuo, Chimoto, Junko, Shiho, Mizuki, Okura, Takashi, Morikawa, Kana, Kagota, Satomi, Shinozuka, Kazumasa
• Format: Journal Article
• Language: English
• Published: Australia Wiley Subscription Services, Inc 01.12.2021
• Subjects: Acetylcholine receptors (muscarinic); Adrenergic receptors; Affinity; Animals; Bladder; Chlorides; Drug therapy; Erythrocytes; Humans; muscarinic receptor; Oral administration; Pyrimidinones; Pyrrolidines; Rats; receptor occupancy; Receptors, Muscarinic; Scopolamine; Submaxillary gland; Urinary Bladder; Urinary Bladder, Overactive - drug therapy; vibegron; receptor occupancy; vibegron; muscarinic receptor; bladder

Objectives To examine the effects of vibegron, a selective β3‐adrenoceptor agonist, used to treat overactive bladder, on muscarinic receptors in the rat bladder, and to predict the occupancy levels of muscarinic receptors by vibegron in the bladders of humans orally administered a clinical dose. Met...