NNC 55-0396

- Overview
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    Background
    
    IC50: 6.8 μM for Cav3.1 T-type channelNNC 55-0396 is a T-type calcium channel antagonist. T-type calcium channel activity is reported to be a critical component of the spontaneous voltage oscillation of inferior olive neurons occurring at a frequency similar to that of essential tremor.In vitro: NNC 55-0396 showed no effect against high voltage calcium channels at 100 μM, but inhibited T-type channels in HEK293 cells with a potency comparable to that of mibefradil (IC50 6.8 versus 10.1 μM) [1]. In vivo: NNC 55-0396 was better tolerated than mibefradil in the horizontalwire test. To assess for a potential interaction with harmaline in the inverted wire grid test, mice was given NNC 55-0396, followed by harmaline or vehicle. NNC 55-0396 ameliorated harmaline-induced test deficits. In the GABAA α1-null model, NNC 55-0396 at 12.5 mg/kg suppressed harmaline-induced tremor by half by 20–100 min, whereas mibefradil at the same dose did not significantly affect tremor. In contrast to mibefradil, NNC 55-0396 was well tolerated and suppresses tremor, and exerts less cytochrome P450 inhibition [1]. Clinical trial: N/A
    
    Reference:[1] Quesada A,Bui PH,Homanics GE,Hankinson O,Handforth A. Comparison of mibefradil and derivative NNC 55-0396 effects on behavior, cytochrome P450 activity, and tremor in mouse models of essential tremor. Eur J Pharmacol.2011 May 20;659(1):30-6.
- Properties
  - Categories
    
    T-type calcium channel blocker
    
    Alternative Name
    
    NNC 55-0396 dihydrochloride; 2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)(methyl)amino)ethyl)-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl cyclopropanecarboxylate dihydrochloride
    
    CAS Number
    
    357400-13-6
    
    Molecular Formula
    
    C30H40Cl2FN3O2
    
    Molecular Weight
    
    564.56
    
    Appearance
    
    White solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble to 25 mM in sterile water
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC(C1C2=C(C=C(F)C=C2)CCC1(OC(C3CC3)=O)CCN(CCCC4=NC5=CC=CC=C5N4)C)C.Cl.Cl
    
    * For Research Use Only