A potent 5-HT4 agonist
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Tegaserod (maleate)

Item No. 14692

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentyl-hydrazinecarboximidamide, 2Z-butenedioate
CAS Number
189188-57-6
Synonyms
  • SDZ-HTF 919
  • Zelnorm
Molecular Formula
C16H23N5O • C4H4O4
Formula Weight
417.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2)(1:3): 0.03 mg/mlDMSO: 20 mg/ml
λmax
279, 316 nm
SMILES
COC(C=C1)=CC2=C1NC=C2/C=N/NC(NCCCCC)=N.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C16H23N5O.C4H4O4/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15;5-3(6)1-2-4(7)8/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21);1-2H,(H,5,6)(H,7,8)/b20-11+;2-1-
InChi Key
CPDDZSSEAVLMRY-FEQFWAPWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $81

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    10 mg

    $128

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    25 mg

    $239

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    50 mg

    $395

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    Product Description

    Tegaserod (maleate) is a potent agonist of the serotonin 4 receptor (5-HT4, Ki = 3.9-31 nM).1,2 As 5-HT4 receptors are associated with cholinergic nerves lining the colon, tegaserod (maleate) stimulates colonic motility and transit in vivo, in both healthy and diseased gastrointestinal tracts.3,4 However, it lacks selectivity, since it also acts as an antagonist for the 5-HT2A, 5-HT2B, and 5-HT2C receptors (Ki = 32, 3.9, and 100 nM, respectively).5,6,4 It is a weak agonist of 5-HT3 (Ki ≤ 10 μM).7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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 constipation. Bioorg. Med. Chem. Lett. 22(19), 6048-6052 (2012).

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

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

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

    5. 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 vivo. Br. J. Pharmacol. 143(5), 549-560 (2004).

    6. 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 rat. Pharmacol. Res. 53(4), 353-358 (2006).

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