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编 号：F612632
分子式：C5H10N3O4P
分子量：207.12
分子式：C5H10N3O4P
分子量：207.12
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CAS No: 446254-47-3
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Amifampridine (3,4-Diaminopyridine) phosphate is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine phosphate is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine phosphate increases transmitter release from neuromuscular junctions (NMJs). Amifampridine phosphate can be used for Lambert-Eaton myasthenic syndrome (LEMS) research.
体内研究：
Amifampridine phosphate (Oral gavage; 10 mg/kg; once) can antagonize muscle paralysis following BoNT/A intoxication.Amifampridine phosphate (2.5 mg/kg (IV); 10 mg/kg (PO); once) shows 1 hour plasma half-life and about 57% bioavailability (F) in mice.Amifampridine phosphate has a short plasma half-life and can induce seizures when present at high concentrations, following penetration of the blood-brain barrier.Animal Model:CD-1 mouse (female,25 g, 6 weeks old)
Dosage:10 mg/kg
Administration:Oral gavage, once, after BoNT/A administration (IP)
Result:Revealed that neither LEMs alone (182 ± 43 min) nor the maximum safe orally deliverable dose of 3,4-DAP alone (225 ± 24 min) could significantly increase the time to death following toxin administration (216 ± 29 min). However, when the 10/50/40 3,4-DAP/LEM/shellac formulation was administered at 25 mg/kg the time to death was 302 ± 26 min - a 40% increase as compared to toxin alone.
Animal Model:CD-1 mouse (30-35 g, 8 weeks old)
Dosage:2.5 mg/kg (IV); 10 mg/kg (PO)
Administration:IV, orally, once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of Amifampridine in CD-1 mouse.IV (2.5 mg/kg) PO (10 mg/kg)
t1/2 (h)1.041.28
AUC0-24 (μM·h)4.299.72
F (%)10056.7
体外研究：
Amifampridine phosphate (1.5 μM) significantly reduces Kv3.3 and Kv3.4 currents by about 10% in HEK293T cells, has no effect on Cav2.1 or Cav1.2 current.Amifampridine phosphate (0-100 μM) increases the duration of the presynaptic AP (action potential) waveform at mammalian and frog NMJs in a dose-dependent manner.
Amifampridine (3,4-Diaminopyridine) phosphate is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine phosphate is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine phosphate increases transmitter release from neuromuscular junctions (NMJs). Amifampridine phosphate can be used for Lambert-Eaton myasthenic syndrome (LEMS) research.
体内研究：
Amifampridine phosphate (Oral gavage; 10 mg/kg; once) can antagonize muscle paralysis following BoNT/A intoxication.Amifampridine phosphate (2.5 mg/kg (IV); 10 mg/kg (PO); once) shows 1 hour plasma half-life and about 57% bioavailability (F) in mice.Amifampridine phosphate has a short plasma half-life and can induce seizures when present at high concentrations, following penetration of the blood-brain barrier.Animal Model:CD-1 mouse (female,25 g, 6 weeks old)
Dosage:10 mg/kg
Administration:Oral gavage, once, after BoNT/A administration (IP)
Result:Revealed that neither LEMs alone (182 ± 43 min) nor the maximum safe orally deliverable dose of 3,4-DAP alone (225 ± 24 min) could significantly increase the time to death following toxin administration (216 ± 29 min). However, when the 10/50/40 3,4-DAP/LEM/shellac formulation was administered at 25 mg/kg the time to death was 302 ± 26 min - a 40% increase as compared to toxin alone.
Animal Model:CD-1 mouse (30-35 g, 8 weeks old)
Dosage:2.5 mg/kg (IV); 10 mg/kg (PO)
Administration:IV, orally, once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of Amifampridine in CD-1 mouse.IV (2.5 mg/kg) PO (10 mg/kg)
t1/2 (h)1.041.28
AUC0-24 (μM·h)4.299.72
F (%)10056.7
体外研究：
Amifampridine phosphate (1.5 μM) significantly reduces Kv3.3 and Kv3.4 currents by about 10% in HEK293T cells, has no effect on Cav2.1 or Cav1.2 current.Amifampridine phosphate (0-100 μM) increases the duration of the presynaptic AP (action potential) waveform at mammalian and frog NMJs in a dose-dependent manner.
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