الصفحة الرئيسية>>Signaling Pathways>> Neuroscience>> 5-HT Receptor>>RS 127445 HCl

RS 127445 HCl (Synonyms: RS-127445; MT 500; RS127445)

رقم الكتالوجGC10670

5-HT2B receptor antagonist,high affinity

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RS 127445 HCl التركيب الكيميائي

Cas No.: N/A

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
40٫00
متوفر
5mg
37٫00
متوفر
10mg
54٫00
متوفر
50mg
224٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

RS-127445 is a selective, high affinity 5-HT2B receptor antagonist.

The 5-HT2B receptor is a G-protein coupled receptor. 5-HT2B receptors are widely expressed in peripheral tissues of various species. 5-HT2B receptor expresses throughout the gastrointestinal tract including smooth muscle of the stomach fundus, oesophagus, colon and small intestine. The receptor has also been found in the placenta, uterus, lung and prostate. 5-HT2B receptors are present in many vascular beds and have been localized to both vascular smooth muscle and vascular endothelial cells [1].

RS-127445 (2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine) showed nanomolar affinity for the 5-HT2B receptor with the pKi of 9.5 ± 0.1. In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pKB = 9.5 ± 0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4 ± 0.1). RS-127445 blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5 ± 1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9 ± 0.3). In rats, RS-127445 was bioavailable via the oral or intraperitoneal routes.

Reference:
[1] Bonhaus D W, Flippin L A, Greenhouse R J, et al.  RS‐127445: a selective, high affinity, orally bioavailable 5‐HT2B receptor antagonist[J]. British journal of pharmacology, 1999, 127(5): 1075-1082.

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