Amifampridine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Amifampridine 通过阻断神经末梢钾通道流出来发挥作用，从而增加动作电位持续时间。然后，Ca2+ 通道可以打开更长的时间，并允许更多的乙酰胆碱释放，以刺激终板的肌肉。

Amifampridine is predominantly in the treatment of a number of rare muscle diseases. Amifampridine works by blocking potassium channel efflux in nerve terminals so that action potential duration is increased. Ca2+ channels can then be open for a longer time and allow greater acetylcholine release to stimulate muscle at the end plate.(In Vitro):Amifampridine (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 (0-100 μM) increases the duration of the presynaptic AP (action potential) waveform at mammalian and frog NMJs in a dose-dependent manner.(In Vivo):Amifampridine (Oral gavage; 10 mg/kg; once) can antagonize muscle paralysis following BoNT/A intoxication.Amifampridine (2.5 mg/kg (IV); 10 mg/kg (PO); once) shows 1 hour plasma half-life and about 57% bioavailability (F) in mice.Amifampridine has a short plasma half-life and can induce seizures when present at high concentrations, following penetration of the blood-brain barrier.

Amifampridine (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 (0-100 μM) increases the duration of the presynaptic AP (action potential) waveform at mammalian and frog NMJs in a dose-dependent manner.

Amifampridine (Oral gavage; 10 mg/kg; once) can antagonize muscle paralysis following BoNT/A intoxication.Amifampridine (2.5 mg/kg (IV); 10 mg/kg (PO); once) shows 1 hour plasma half-life and about 57% bioavailability (F) in mice.Amifampridine 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.

3,4-Diaminopyridine

Others

Other Targets

Others

Others-Field

——

54-96-6

109.13

C5H7N3

>98% (HPLC)

DMSO : ≥ 38 mg/mL; 348.21 mM

Nc1ccncc1N

——

(-20℃)

With Ice Pack

≥ 2 years