159730-07-1
Chemical Structure
LY-272015
- CAS No.: 159730-07-1
- Formula:C21H24N2O2
- Molecular Weight:336.43
IUPAC Name: 1-(3,4-dimethoxybenzyl)-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
InChIKey: GDAJGLDMCDMPIR-UHFFFAOYSA-N
SMILES: CC1=CC2=C(NC3=C2CCNC3CC4=CC=C(OC)C(OC)=C4)C=C1
Biological Activity: LY-272015 is an orally active and selective 5-HT2B receptor antagonist. LY-272015 blocks 5-HT2 receptors and inhibits Fluoxetine (HY-B0102)-induced PDGFβ receptor transactivation. LY-272015 attenuates 5-HT-induced smooth muscle cell migration and proliferation, and inhibits downstream mTOR/p70S6K phosphorylation. LY-272015 reduces 5-HT-induced vasoconstriction. LY-272015 reverses the excitatory effect of BW-723C86 (HY-101369) on NTS neurons. LY-272015 lowers mean arterial blood pressure in severely hypertensive DOCA-salt rats. LY-272015 can be used in research related to diseases such as hypertension and cardiovascular calcification[1][2][3][4][5][6].
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LY-272015 | LY-272015 is an orally active and selective 5-HT2B receptor antagonist. LY-272015 blocks 5-HT2 receptors and inhibits Fluoxetine (HY-B0102)-induced PDGFβ receptor transactivation. LY-272015 attenuates 5-HT-induced smooth muscle cell migration and proliferation, and inhibits downstream mTOR/p70S6K phosphorylation. LY-272015 reduces 5-HT-induced vasoconstriction. LY-272015 reverses the excitatory effect of BW-723C86 (HY-101369) on NTS neurons. LY-272015 lowers mean arterial blood pressure in severely hypertensive DOCA-salt rats. LY-272015 can be used in research related to diseases such as hypertension and cardiovascular calcification. | |||||||||||||||||||||
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References
- [1]. Kruk JS, et al. Fluoxetine-induced transactivation of the platelet-derived growth factor type β receptor reveals a novel heterologous desensitization process. Molecular and cellular neurosciences. 2015 Mar;65:45-51.
- [2]. Liu Y. Inhibition of 5‐Hydroxytryptamine Receptor 2B Reduced Vascular Restenosis and Mitigated the β‐Arrestin2–Mammalian Target of Rapamycin/p70S6K Pathway. Journal of the American Heart Association. 2018 Jan 30;7(3):e006810.
- [3]. Niebert M. Expression and function of serotonin 2A and 2B receptors in the mammalian respiratory network. PLoS One. 2011 Jul 18;6(7):e21395.
- [4]. Watts SW, et al. 5-HT2B-receptor antagonist LY-272015 is antihypertensive in DOCA-salt-hypertensive rats. The American journal of physiology. 1999 Mar;276(3):H944-52. [Content Brief]
- [5]. Sévoz-Couche C, et al. In vivo modulation of vagal-identified dorsal medullary neurones by activation of different 5-Hydroxytryptamine(2) receptors in rats. Br J Pharmacol. 2000 Dec;131(7):1445-53.
- [6]. Hon A, et al. Specific serotonin receptor antagonist reduces murine calcific atherosclerosis. Atherosclerosis. 2026 Mar;414:120649.
