I. LY2183240 basic Characters:
|Storage Temp:||-20°C Freezer|
1. What is LY2183240?
LY-2183240(CAS 874902-19-9) is a drug which acts both as a potent inhibitor of the reuptake of the endocannabinoid anandamide and as an inhibitor of fatty acid amide hydrolase (FAAH), LY2183240 inactivates FAAH by carbamylation of the enzyme’s serine nucleophile. More global screens using activity-based proteomic probes identified several additional serine hydrolases that are also inhibited by LY2183240. These results indicate that the blockade of anandamide uptake observed with LY2183240 may be due primarily to the inactivation of FAAH, providing further evidence that this enzyme serves as a metabolic driving force that promotes the diffusion of anandamide into cells. More generally, the proteome-wide target promiscuity of LY2183240 designates the heterocyclic urea as a chemotype with potentially excessive protein reactivity for drug design. LY2183240 may be an effective pharmacotherapy for individuals with anxiety disorders, such as post-traumatic stress disorder, but may not be appropriate for individuals with co-morbid anxiety and alcohol-use disorders.
2. LY2183240 Basic Characteristic:
|Chemical Name:||LY2183240 powder|
5-Biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide;
LY-2183240 MN-25; LY2183240/LY-2183240
|storage temp. :||Store at +4°C|
|Solubility:||DMSO: >10 mg/mL|
2. What’s the possible effects while taking LY2183240 ?
An attractive approach to the desired effects of LY-2183240 activation while avoiding the negative effects of global CB1 stimulation is to manipulate endogenous cannabinoid signaling by inhibiting LY-218324oand related enzymes. Due to the rapid hydrolysis of LY-2183240, the resting concentration of AEA in the CNS is very low. In addition, LY-2183240 controls levels of other lipid mediators with anti-inflammatory and analgesic properties, including PEA, which exerts its analgesic and anti-inflammatory effects through the non-cannabinoid pathway. Inhibition of LY-218324o is expected to increase the endogenous concentration of all of its substrates, thereby prolonging and enhancing its biological effects. This preferential action on the active pathway may be expected to have a reduced risk of psychotic effects compared to the full activation of the cannabinoid receptor by an exogenously applied agonist.
In addition, there are several additional therapeutic areas where changes in endogenous cannabinoid processing may be beneficial. In particular, concentration changes in tissues associated with many diseases, including immune diseases, mental disorders, metabolic and cardiovascular diseases, have been reported. In fact, the effects of LY-2183240 inhibition are theoretically quite complex given the number of potential substrates for the enzyme and the various targets (cannabinoids and non-cannabinoids) that interact with these substrates.