Tegaserod-d₁₁  (Synonyms: 替加色罗-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].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
替加色罗 (3-5 μM; 24-72 小时) 引起显着的时间和剂量依赖性细胞凋亡增加^[2]。
替加色罗 (3-5 μM; 8-18 小时) 降低 p-S6 ，p-p70 S6 (Thr⁴²¹/Ser⁴²⁴)^[2]。
替加色罗 (0.1-3 μM; 24 小时) 有效抑制 5-HT 介导的大鼠离体胃底收缩 (pA₂=8.3)，与 5-HT_2B 受体拮抗剂活性一致^[4]。

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

替加色罗 (5 mg/kg/天; 腹腔注射; 连续五天) 在体内延迟肿瘤生长、减少转移、增加存活率并抑制 p-S6^[2]。
替加色罗 (0.1-2.0 mg/kg; 胃负荷前 15 分钟腹腔注射) 显着加速 db/db 小鼠的胃葡萄糖排空率，在 0.1mg/kg 的情况下将 30 分钟时留在胃中的膳食部分减少 80%^[3].

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

312.45

C₁₆H₁₂D₁₁N₅O

1134188-56-9

145158-71-0

替加色罗-d₁₁

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]