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Tegaserod maleate

Cat. No.:YN320825

  • CAS No. :189188-57-6

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    • 产品名称: Tegaserod maleate
      CAS No.: 189188-57-6
      Chemical Name: 2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentyl-hydrazinecarboximidamide, 2Z-butenedioate
      Synonyms:马来酸替加色罗; SDZ-HTF-919; HTF-919
      分子量:417.46
      分子式:C₂₀H₂₇N₅O₅
      SMILES:O=C(O)/C=C\C(O)=O.COC1=CC=C(NC=C2/C=N/NC(NCCCCC)=N)C2=C1
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: Tegaserod maleate 是选择性的、5-HT4受体的部分激动剂和5-HT2B受体的拮抗剂。Tegaserod maleate 在胃肠道中表现出促进的作用。
      IC50和靶点:
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      In Vivo:
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    • Long, D.D., Armstrong, S.R., Beattie, D.T., et al.Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT4 receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipationBioorg. Med. Chem. Lett.22(19),6048-6052(2012)

      Hedner, E., Sjögren, M., Frändberg, P.A., et al.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligandsJ. Nat. Prod.69(10),1421-1424(2006)

      Nguyen, A., Camilleri, M., Kost, L.J., et al.SDZ HTF 919 stimulates canine colonic motility and transit in vivoJ. Pharmacol. Exp. Ther.280(3),1270-1276(1997)

      Tack, J., Camilleri, M., Chang, L., et al.Systematic review: Cardiovascular safety profile of 5-HT4 agonists developed for gastrointestinal disordersAliment. Pharmacol. Ther.35(7),745-767(2012)

      Beattie, D.T., Smith, J.A.M., Marquess, D., et al.The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivoBr. J. Pharmacol.143(5),549-560(2004)

      McCullough, J.L., Armstrong, S.R., Hegde, S.S., et al.The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized ratPharmacol. Res.53(4),353-358(2006)

      Lemaître, S., Lepailleur, A., Bureau, R., et al.Novel antagonists of serotonin-4 receptors: Synthesis and biological evaluation of pyrrolothienopyrazinesBioorg. Med. Chem.17(6),2607-2622(2009)

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