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Velusetrag

CAS No. : 866933-46-2

MCE 国际站：Velusetrag

产品活性：Velusetrag (TD-5108) 是一种具有口服活性，有效和选择性的血清素 5-HT₄ 受体 (5-HT₄R) 激动剂，pK_i 为 7.7。Velusetrag 对 5-HT_2A 和 5-HT_2B 受体没有亲和力 (K_i>10 μM)。Velusetrag 可用于胃肠道疾病和帕金森病的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: Velusetrag (10 pM-100 μM) concentration-dependently increases the cAMP in HEK-293 cells stably transfected with the h5-HT4(c) receptor, with a pEC₅₀ of 8.3.
Velusetrag (100 pM-1 μM) produces concentration-dependent contraction of the guinea pig colonic longitudinal muscle/myenteric plexus (LMMP), with a pEC₅₀ of 7.9.
Velusetrag (0.001-10 μM) produces a concentration-dependent relaxation of the carbachol (3 μM)-precontracted rat esophagus, with a pEC₅₀ of 7.9.

In Vivo: Velusetrag (3 mg/kg; a single i.p.) significantly improves the facilitation of contextual fear extinction in PD mice.
Velusetrag (3 mg/kg; a single i.p.) increases hippocampal cAMP levels in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice.
Velusetrag (0.003-3 mg/kg; a single s.c.) increases colonic transit in a dose-dependent manner and reduces the time taken for excretion of the dye in guinea pigs.
Velusetrag (0.003-1 mg/kg; a single i.v.) dose-dependently increases inter-crystal distance, consistent with relaxation of the oesophagus in rats.

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