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Tegaserod maleate

CAS No. : 189188-57-6

MCE 站：Tegaserod maleate

产品活性：Tegaserod maleate 是选择性的、5-HT₄ 受体的部分激动剂和 5-HT_2B 受体的拮抗剂。Tegaserod maleate 在胃肠道中表现出促进的作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: Tegaserod was metabolized in human liver microsomes to O-desmethyl tegaserod at a low rate.
Tegaserod had significant binding affinity for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors (pK_i=7.5, 8.4 and 7.0, respectively).
Tegaserod (0.1-3 μM) inhibits 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA₂=8.3), consistent with 5-HT2B receptor antagonist activity.

In Vivo: Tegaserod increases the amplitude of excitatory postsynaptic currents mediated by nicotinic acetylcholine receptors which may contribute to the prokinetic effects by facilitating excitatory neurotransmission in mice.
Tegaserod (0.1 mg/kg) 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%.
Tegaserod (5, 10, 50, 100 μg/mL) promotes hindlimb motor function at 6 weeks after spinal cord injury compared to the control group receiving vehicle only.

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