Iso-Olomoucine

- Overview
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    Background
    
    IC50: ≥ 1 mM for Cdk5Iso-Olomoucine is an inactive stereoisomer of the Cdk5 inhibitor olomoucine.Cyclin-dependent kinases (CDKs) are reported to be key regulators of cell cycle progression whose function/dysfunction has been implicated in cancer, human neurodegenerative diseases, as well as the response of addictive drugs through alteration of postsynaptic dopamine receptor signaling.In vitro: In a previous study, rat dorsal striatal synaptosomes were incubation with the Cdk5 inhibitors roscovitine, olomoucine, and GW8510 or the inactive congener iso-olomoucine, which led to a rapid, concentration-dependent inhibition of specific [3H]DA uptake. However, roscovitine was the only inhibitor that did not decrease [3H]2beta-carbomethoxy-3beta-(4-fluorophenyl)tropane binding to dSTR DATs. Roscovitine-induced inhibition of dSTR [3H]DA uptake was demonstrated by decreased maximal uptake velocity, without a change in cell-surface DAT levels. Moreover, roscovitine did not enhance [3H]DA release mediated by either DAT reverse-transport. Instead, roscovitine could enhance spontaneous [3H]DA outflow and inhibit DAT-mediated [3H]DA reaccumulation into dSTR slices. Additionally, in a Cdk5-independent manner, iso-olomoucine was able to rapidly inhibit dopamine transporter activity in rat dorsal striatal synaptosomes with a potency similar to that of olomoucine (IC50 ~37 μM) [1]In vivo: Up to now, there is no animal in vivo data reported.Clinical trial: So far, no clinical study has been conducted.
- Properties
  - Alternative Name
    
    2-[[7-methyl-6-[(phenylmethyl)amino]-7H-purin-2-yl]amino]-ethanol
    
    CAS Number
    
    101622-50-8
    
    Molecular Formula
    
    C15H18N6O
    
    Molecular Weight
    
    298.3
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤0.3mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Iso-Olomoucine

Background

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