Oleoyl Serotonin

TRPV1 antagonist

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库存: 现货

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数量
5mg

￥825.00

660.00

- +
10mg

￥1375.00

1100.00

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50mg

￥5225.00

4180.00

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已选 0 种 0 瓶

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货号: ajci6536
CAS: 1002100-44-8
别名:
分子式: C28H44N2O2
分子量: 440.1
纯度: >98%
溶解度: ≤15mg/ml in DMSO;15mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1 [1].

The transient receptor potential vanilloid-type 1 (TRPV1) channel is a nonselective cation channel that may be activated by a variety of exogenous and endogenous physical and chemical stimuli. TRPV1 is decreased in the injured nerve fibers but increased in those proximal to the site damage. TRPV1 is a potential new target for the development of analgesic and anti-inflammatory drugs [1].

Oleoyl serotonin is a hybrid molecule patterned after arachidonoyl serotonin. Arachidonoyl serotonin is a dual antagonist of TRPV1 and fatty acid amide hydrolase (FAAH) with IC50 values of 0.27 and 8 μM, respectively. Arachidonoyl serotonin was highly effective against both acute and chronic peripheral pain [1][2]. In TRPV1 and FAAH assays, Oleoyl serotonin inhibited anandamide hydrolysis by FAAH and capsaicin-induced intracellular Ca2+ elevation in HEK293 cells overexpressing the human recombinant TRPV1 receptor with IC50 values of > 50 μM and 2.57 μM, respectively [1].

参考文献:
[1].? Ortar G, Cascio MG, De Petrocellis L, et al. New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. J Med Chem. 2007 Dec 27;50(26):6554-69.
[2].? Maione S, De Petrocellis L, de Novellis V, et al. Analgesic actions of N-arachidonoyl-serotonin, a fatty acid amide hydrolase inhibitor with antagonistic activity at vanilloid TRPV1 receptors. Br J Pharmacol. 2007 Mar;150(6):766-81.