Amifampridine (3,4-Diaminopyridine) phosphate 是一种口服有效和可透过细胞的电压门控钾 (Kv) 通道阻断剂 (PCB)。Amifampridine phosphate 对 BoNT/A (HY-P79153) 中毒有明显的逆转作用。Amifampridine phosphate 可增加神经肌肉连接 (NMJs) 的递质释放。Amifampridine phosphate 可用于 Lambert-Eaton 肌无力综合征 (LEMS) 的研究。
| 生物活性 | Amifampridine (3,4-Diaminopyridine) phosphate is an orally active, potent and cell permeablevoltage-gated potassium (Kv) channelblocker (PCB). Amifampridine phosphate is efficacy in the reversal ofBoNT/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[1][2][3]. |
体外研究
(In Vitro) | 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[3].
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[3].
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体内研究
(In Vivo) | Amifampridine phosphate (Oral gavage; 10 mg/kg; once) can antagonize muscle paralysis following BoNT/A intoxication[2].
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[2].
Amifampridine phosphate has a short plasma half-life and can induce seizures when present at high concentrations, following penetration of the blood-brain barrier[2].
| Animal Model: | CD-1 mouse (female,25 g, 6 weeks old)[2] | | 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)[2] | | 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[1].
| IV (2.5 mg/kg) | PO (10 mg/kg) | | t1/2(h) | 1.04 | 1.28 | | AUC0-24(μM·h) | 4.29 | 9.72 | | F (%) | 100 | 56.7 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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