| Identification | Back Directory | [Name]
N-type calcium channel blocker-1 | [CAS]
241499-17-2 | [Synonyms]
N-type calcium channel blocker-1
4-Piperidinamine, 1-[[4-(dimethylamino)phenyl]methyl]-N-[4-(3,3-dimethylbutyl)phenyl]-N-(3-methyl-2-buten-1-yl)- | [Molecular Formula]
C31H47N3 | [MDL Number]
MFCD30533351 | [MOL File]
241499-17-2.mol | [Molecular Weight]
461.73 |
| Chemical Properties | Back Directory | [Boiling point ]
569.9±50.0 °C(Predicted) | [density ]
1.013±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
8.89±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
1-[[4-(Dimethylamino)phenyl]methyl]-N-[4-(3,3-dimethylbutyl)phenyl]-N-(3-methyl-2-buten-1-yl)-4-piperidinamine, is an N-type calcium channel blocker, and an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay. | [in vivo]
N-type calcium channel blocker-1 shows good activities in the acetic acid anti-writhing model (ED50=4 mg/kg, iv). N-type calcium channel blocker-1 exhibits oral activity (ED50=12 mg/kg, po). A time course study of N-type calcium channel blocker-1 in the anti-writhing model indicates that the CF-1 mice have maximal effect at 120 min after oral dosing at 60 mg/kg. Further evaluation of N-type calcium channel blocker-1 demonstrates several important and advantageous features: the pharmacokinetic profile of N-type calcium channel blocker-1 is improved (Versus of 5.9 L/kg and CL of 26 mL/min/kg) and the logPn of 26 is favorable for CNS agent (logPn measured to be 3.20)[1]. |
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