67964-87-8

Usage

Biological Activity

stearoyl 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].stearoyl 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, stearoyl 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 18-carbon stearoyl moiety had not been studied [1].