Solabegron
{{Drugbox-lat | Watchedfields = | verifiedrevid = 443452701 | IUPAC_name = 3'-[(2 image = Solabegron-2d-skeletal.png | width = | image2 = | width2 =
| tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration =
| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =
| CAS_number_Ref = 
| CAS_number = 451470-34-1
| ATC_prefix = none
| ATC_suffix =
| PubChem = 6433123
| IUPHAR_ligand =
| ChEMBL_Ref =
| ChEMBL =
| DrugBank_Ref =
| DrugBank =
| UNII_Ref =
| UNII = 55P6YH9O6N
| KEGG_Ref =
| KEGG = D05879
| C=23 | H=23 | Cl=1 | N=2 | O=3
| molecular_weight = 410,892 g/mol
| smiles = OC(=O)c(c2)cccc2-c1cc(ccc1)NCCNCC(O)c3cccc(Cl)c3
| StdInChI_Ref =
| StdInChI =
| StdInChIKey_Ref =
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| synonyms = 3-(3-(2-[(2-(3-hlorofenil)-2-hidroksietil)amino]etilamino)fenil)benzojeva kiselina
}}
Solabegron (GW-427,353) je lek koji deluje kao selektivni agonist za β3 adrenergički receptor. On je u razvoju za tretman preaktivne bešike i sindroma iritabilnih creva.[1][2][3] Pokazano je da proizvodi unutrašnju analgeziju putem oslobađanja somatostatina iz adipocita.[4][5]
Solabegron je otkrio GlaksoSmitKlajn i otkupila kompanija AltheRx marta 2011. Solabegron relaksira glatke mišiće bešike putem stimulacije beta-3 adrenoceptora. To je nov mehanizam u poređenju sa trenutno dostupnim tretmanima.
Sinteza
[уреди | уреди извор]
Reference
[уреди | уреди извор]- ^ Hicks, Alexandra; McCafferty, Gerald P.; Riedel, Erin; Aiyar, Nambi; Pullen, Mark; Evans, Christopher; Luce, Trudy D.; Coatney, Robert W.; Rivera, Gian C.; Westfall, Timothy D.; Hieble, J. Paul (октобар 2007). „GW427353 (Solabegron), a Novel, Selective β3-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog”. Journal of Pharmacology and Experimental Therapeutics. 323 (1): 202—9. PMID 17626794. doi:10.1124/jpet.107.125757..
- ^ Grudell, A. B.; Camilleri, M; Jensen, K. L.; Foxx-Orenstein AE; Burton DD, Ryks MD, Baxter KL, Cox DS, Dukes GE, Kelleher DL, Zinsmeister AR (мај 2008). „Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel function, and somatostatin levels in health”. American Journal of Physiology. Gastrointestinal and Liver Physiology. 294 (5): G1114—9. PMID 18372395. doi:10.1152/ajpgi.00051.2008.
- ^ Kelleher DL, Hicks KJ, Cox DS,; et al. (2008). „Randomized, double-blind, placebo (PLA)-controlled, crossover study to evaluate efficacy and safety of the beta 3-adrenergic receptor agonist solabegron (SOL) in patients with irritable bowel syndrome (IBS)”. Neurogastroenterol Motil. 20 (Suppl 2): 131.
- ^ Cellek S, Thangiah R, Bassil AK, Campbell CA, Gray KM, Stretton JL, Lalude O, Vivekanandan S, Wheeldon A, Winchester WJ, Sanger GJ, Schemann M, Lee K (јул 2007). „Demonstration of functional neuronal beta3-adrenoceptors within the enteric nervous system”. Gastroenterology. 133 (1): 175—83. PMID 17631141. doi:10.1053/j.gastro.2007.05.009.
- ^ Schemann M, Hafsi N, Michel K, Kober OI, Wollmann J, Li Q, Zeller F, Langer R, Lee K, Cellek S. The beta3-adrenoceptor agonist GW427353 (solabegron) decreases excitability of human enteric neurons via release of somatostatin. Gastroenterology 2009 Sep 25. [Epub ahead of print]
Literatura
[уреди | уреди извор]- K.H. Donaldson, B.G. Shearer, D.E. Uehling, U.S. Patent 6,251,925 (2001).
