ChemicalBook--->CAS DataBase List--->241499-17-2

241499-17-2

241499-17-2 Structure

241499-17-2 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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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