Tegaserod-d₁₁ 

Tegaserod-d₁₁ is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research^[1][2][3].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
Tegaserod (3-5 μM; 24-72 h) causes a significant time and dose-dependent increase in apoptosis^[2].
Tegaserod (3-5 μM; 8-18 h) decreases phosphorylation of the kinase directly upstream of S6, p70 S6 at Thr⁴²¹/Ser^424[2].
Tegaserod (0.1-3 μM; 24h) inhibits 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA₂=8.3), consistent with 5-HT_2B receptor antagonist activity^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tegaserod (5?mg/kg/day; ip; for five consecutive days) delays tumor growth, reduces metastases, increases survival and suppresses p-S6 in vivo^[2].
Tegaserod (0.1-2.0 mg/kg; IP 15 min prior to gastric loading) significantly accelerates the gastric emptying rate of glucose in db/db mice, reducing the fraction of the meal remaining in the stomach at 30 min by 80% with 0.1mg/kg^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

312.45

C₁₆H₁₂D₁₁N₅O

1134188-56-9

N=C(NC([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])N/N=C/C1=CNC2=CC=C(OC)C=C21

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Wei Liu, et al. Repurposing the serotonin agonist Tegaserod as an anticancer agent in melanoma: molecular mechanisms and clinical implications. J Exp Clin Cancer Res. 2020 Feb 21;39(1):38.  [Content Brief]

  [3]. M D Crowell, et al. The effects of tegaserod, a 5-HT receptor agonist, on gastric emptying in a murine model of diabetes mellitus. Neurogastroenterol Motil. 2005 Oct;17(5):738-43.  [Content Brief]

  [4]. D T Beattie, et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60.  [Content Brief]