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Palmitoyl Serotonin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Palmitoyl Serotonin图片
CAS NO:212707-51-2
规格:98%
分子量:414.6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
TRPV1 channel inhibitor
CAS:212707-51-2
分子式:C26H42N2O2
分子量:414.6
纯度:98%
存储:Store at -20°C

Background:

Palmitoyl Serotonin is a TRPV1 antagonist with IC50 value of 0.76 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].


Palmitoyl 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, Palmitoyl serotonin inhibited anandamide hydrolysis mediated by FAAH and capsaicin-induced intracellular Ca2+ elevation in HEK293 cells overexpressing the human recombinant TRPV1 receptor with IC50 values of >50 μM and 0.76 μM, respectively. However, the effects of replacing the arachidonoyl portion with the saturated 16-carbon palmitoyl moiety had not been studied [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.