NNC 55-0396

Short Summary : T-type calcium channel blocker

Category : Membrane Transporter/Ion Channel|Calcium Channel

Purity : 0.98

CAS Number : 357400-13-6

Formula : C30H40Cl2FN3O2

Molecular Weight : 564.56

SMILE : CC(C1C2=C(C=C(F)C=C2)CCC1(OC(C3CC3)=O)CCN(CCCC4=NC5=CC=CC=C5N4)C)C.Cl.Cl

Solubility : Soluble to 25 mM in sterile water

Storage : Store at -20°C

Description : IC50: 6.8 M 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 M, but inhibited T-type channels in HEK293 cells with a potency comparable to that of mibefradil (IC50 6.8 versus 10.1 M) [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 1-null model, NNC 55-0396 at 12.5 mg/kg suppressed harmaline-induced tremor by half by 20C100 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/AReference:[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.

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