Rafabegron - CAS 244081-42-3
Catalog number: 244081-42-3
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Rafabegron is a potent and selective beta3-adrenoceptor agonist.
Solid powder
2-[[3-[(2R)-2-[[(2R)-2-(3-chlorophenyl)-2-hydroxy-ethyl]amino]propyl]- 1H-indol-7-yl]oxy]acetic acid; TAK 677; TAK-677; TAK677; AD-9677; AD9677; AD 9677; AJ-9677; AJ-9677; AJ-9677; Rafabegron.
Canonical SMILES:
1.Effects of a novel beta(3)-adrenoceptor agonist, AJ-9677, on relaxation of the detrusor muscle: an in vitro study.
Otsuka A;Shinbo H;Hasebe K;Matsumoto R;Ozono S Int J Urol. 2008 Dec;15(12):1072-6. doi: 10.1111/j.1442-2042.2008.02165.x.
OBJECTIVES: ;To examine the relaxant effects of AJ-9677, a novel beta(3)-adrenoceptor agonist, on the isolated rat, monkey and human detrusor muscle.;METHODS: ;The isolated detrusor strips of rats, monkeys and humans were mounted in organ baths containing Krebs solution. By the cumulative addition of beta-adrenoceptor agonists (isoproterenol, AJ-9677, CL 316,243 and salbutamol in rats; isoproterenol, AJ-9677 and CL 316,243 in monkeys and humans), concentration-relaxation curves were obtained. The maximal relaxation responses and pEC(50) values were calculated. In rats, concentration-relaxation curves to isoproterenol and AJ-9677 were obtained in the presence and absence of propranolol or SR 59230A.;RESULTS: ;Isoproterenol, AJ-9677, CL 316,243 and salbutamol induced concentration-dependent relaxation in rats. The rank order of their relaxing potency in the rat detrusor muscle was AJ-9677 > isoproterenol > CL 316,243 > salbutamol. Isoproterenol and AJ-9677 also produced a concentration-dependent relaxation with high potency in monkeys and humans, whilst CL 316,243 had low relaxing potency. According to the antagonist studies in rats, propranolol and SR 59230A caused a rightward shift of the concentration-relaxation curves to isoproterenol or AJ-9677, respectively.
2.Urothelial beta-3 adrenergic receptors in the rat bladder.
Kullmann FA;Downs TR;Artim DE;Limberg BJ;Shah M;Contract D;de Groat WC;Rosenbaum JS Neurourol Urodyn. 2011 Jan;30(1):144-50. doi: 10.1002/nau.20965.
AIMS: ;To investigate the distribution of beta-3 adrenergic receptors (β(3)ARs) in the rat bladder and to examine the contribution of urothelial β(3)ARs to agonist-induced suppression of bladder reflexes and relaxation of smooth muscle.;METHODS: ;Bladder tissue was collected from 8- to 10-month old female SD rats. In some samples, the urothelium was surgically separated from the smooth muscle. The expression and localization of βAR mRNA and β(3)AR protein were determined using RT-PCR and immunohistochemistry. Contractile responses to the specific β(3)AR agonists TAK-677 and BRL37344 were measured in bladder strips with or without the urothelium. The contribution of urothelial β(3)ARs to the micturition reflex was assessed in continuous cystometry in urethane anesthetized rats using intravesical delivery of β(3)AR agonists.;RESULTS: ;RT-PCR detected mRNA of all βARs in urothelium and smooth muscle. Immunostaining detected β(3)ARs throughout the urothelium, in the smooth muscle, myofibroblast-like cells, and in the peripheral nerves. Ovariectomy did not change the distribution of β(3)ARs in any bladder structure. Intravesical administration of TAK-677 and BRL37344 (1-5 × 10(-4) M) decreased voiding frequency and amplitude of bladder contractions.
3.Lack of an effect of a novel beta3-adrenoceptor agonist, TAK-677, on energy metabolism in obese individuals: a double-blind, placebo-controlled randomized study.
Redman LM;de Jonge L;Fang X;Gamlin B;Recker D;Greenway FL;Smith SR;Ravussin E J Clin Endocrinol Metab. 2007 Feb;92(2):527-31. Epub 2006 Nov 21.
OBJECTIVE: ;Our objective was to test the safety and metabolic effects of a novel beta(3)-adrenoreceptor agonist (TAK-677) in humans.;DESIGN, SETTING, AND PARTICIPANTS: ;Sixty-five obese (body mass index = 33.9 +/- 2.1 kg/m2, mean +/- se) men and women (31.4 +/- 0.9 yr) participated in a double-blind placebo-controlled study at an institutional research center.;INTERVENTION: ;Participants were randomized to 0.1 mg TAK-677 twice daily (BID) (n = 21), 0.5 mg TAK-677 BID (n = 22), or placebo BID (n = 22) for 29 d.;OUTCOMES: ;Drug safety, 24-h respiratory quotient (RQ), 24-h energy expenditure (EE), body composition, fat distribution, and fasting plasma concentration of substrates and hormones were assessed. An acute-response study was also conducted.;RESULTS: ;The drug was well tolerated by all participants; however, heart rate was elevated (9 +/- 2 beats per minute) with the 0.5-mg BID dose. After 28 d of treatment and when compared with placebo, there was no change in 24-h RQ with either 0.1-mg BID (P = 0.1) or 0.5-mg BID (P = 1.0) doses of TAK-677. However, TAK, 0.5 mg BID, resulted in a small increase in 24-h EE that was significantly different from placebo [change from baseline, 13 +/- 17 (0.
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