Solabegron

Из Википедије, слободне енциклопедије

{{Drugbox-lat | Watchedfields = | verifiedrevid = 443452701 | IUPAC_name = 3'-[(2-{[(2R)-2-(3-hlorofenil)-2-hidroksietil]amino}etil)amino]bifenil-3-karboksilna kiselina | 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 =  ДаY | CAS_number = 451470-34-1 | ATC_prefix = none | ATC_suffix = | PubChem = 6433123 | IUPHAR_ligand = | ChEMBL_Ref = | ChEMBL = | DrugBank_Ref =  ДаY | DrugBank = | UNII_Ref =  ДаY | UNII = 55P6YH9O6N | KEGG_Ref =  ДаY | 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 =  ДаY | StdInChI = | StdInChIKey_Ref =  ДаY | StdInChIKey = | 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]

Solabegron scheme.png

Reference[уреди]

  1. Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C, Luce TD, Coatney RW, Rivera GC, Westfall TD, Hieble JP. GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. Journal of Pharmacology and Experimental Therapeutics. 2007 Oct;323(1):202-9. doi:10.1124/jpet.107.125757 PMID 17626794
  2. Grudell AB, Camilleri M, Jensen KL, Foxx-Orenstein AE, Burton DD, Ryks MD, Baxter KL, Cox DS, Dukes GE, Kelleher DL, Zinsmeister AR. 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. 2008 May;294(5):G1114-9. PMID 18372395
  3. Kelleher DL, Hicks KJ, Cox DS, et al. 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 2008;20 (Suppl 2):131.
  4. 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. Demonstration of functional neuronal beta3-adrenoceptors within the enteric nervous system. Gastroenterology. 2007 Jul;133(1):175-83.
  5. 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]

Spoljašnje veze[уреди]