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Solabegron

Names

[ CAS No. ]:
252920-94-8

[ Name ]:
Solabegron

Biological Activity

[Description]:

Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM[1]. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Metabolic Disease

[Target]

EC50: 22 nM (β3-AR in cells)[1].


[In Vivo]

Solabegron (GW427353) at 3 mg/kg i.v. evokes an increase in micturition volume threshold that prevented the acetic acid-evoked decreases in dogs. The low dose (1 mg/kg) shows no significant activity[1]. Animal Model: Adult female beagle dogs (6-10 kg)[1]. Dosage: 1, 3 mg/kg. Administration: I.V. once. Result: Dosage of 3 mg/kg evoked an increase in micturition volume threshold.

[References]

[1]. Hicks A, et al. GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. J Pharmacol Exp Ther. 2007 Oct;323(1):202-9.

[2]. Andersson KE, et al. Selective β3-adrenoceptor agonists for the treatment of overactive bladder. J Urol. 2013 Oct;190(4):1173-80.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H23ClN2O3

[ Molecular Weight ]:
410.89

[ Storage condition ]:
2-8℃


Related Compounds

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