Evaluation of 4-aminopyridine and 3,4-diaminopyridine penetrability into cerebrospinal fluid in anesthetized rats

Lemeignan, M; Millart, Hervé; Lamiable, Denis; Molgo, J.; Lechat, P

doi:10.1016/0006-8993(84)90875-8

Cited by 63 publications

(28 citation statements)

References 8 publications

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“…In our experiments, the seizure-related symptoms were highly reproducible, as shown by the relatively small SEM values. A further advantage of 4-AP that it readily crosses the blood-brain barrier (Lemeignan et al, 1984), consequently the latencies of the symptoms are very short. The shortest latency of tremor at 14 mg/ kg 4-AP plus naltrexone was 2 min, that of the GC was 4 min, indicating that large groups of neurons were promptly involved by the action of 4-AP.…”

Section: Resultsmentioning

confidence: 99%

Naltrexone potentiates 4-aminopyridine seizures in the rat

Mihály

Bencsik

Solymosi

1990

J. Neural Transmission

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The effects of a pharmacological blockade of the mu opiate receptors on the manifestation of tonic-clonic seizures were investigated in freely moving animals. 4-aminopyridine, a specific blocker of the neuronal K+ channels was used to produce generalized convulsions. After pretreatment of adult rats with 1 mg/kg naltrexone HCl, 3, 5, 7, 9, 14 mg/kg 4-aminopyridine was injected intraperitoneally, and the latencies of the symptoms generated by 4-aminopyridine were measured. Naltrexone HCl decreased these latencies and enhanced the seizures significantly. The experiments provided further evidence for the existence of a tonic anticonvulsant opioid system in the brain.

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Section: Resultsmentioning

confidence: 99%

Naltrexone potentiates 4-aminopyridine seizures in the rat

Mihály

Bencsik

Solymosi

1990

J. Neural Transmission

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“…Furthermore, 4-AP is evidently more effective than 3,4-diaminopyridine31 36–38 41 because it crosses the blood-brain barrier more easily 42 43…”

Section: Discussionmentioning

confidence: 99%

A randomised double-blind, cross-over trial of 4-aminopyridine for downbeat nystagmus—effects on slowphase eye velocity, postural stability, locomotion and symptoms

Claaßen

Spiegel

Kalla

et al. 2013

J Neurol Neurosurg Psychiatry

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“…3,4-DAP blocks potassium channels in excitable membranes, which prolongs the duration of the nerve action potentials [30,32]. Experimental studies revealed 3,4-DAP to be more effective than 4-aminopyridine in facilitating neuromuscular transmission [30,32], whereas the penetrability of 3,4-DAP into the CNS is lower [33].…”

Section: Introduction To 34-dapmentioning

confidence: 99%

3,4-diaminopyridine for the treatment of Lambert–Eaton myasthenic syndrome

Wirtz¹,

Titulaer²,

Gerven³

et al. 2010

Expert Review of Clinical Immunology

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The Lambert-Eaton myasthenic syndrome (LEMS) is an autoimmune disease in which antibodies against voltage-gated calcium channels inhibit cholinergic neurotransmission. LEMS is clinically characterized by muscle weakness and autonomic dysfunction. 3,4-diaminopyridine (3,4-DAP) blocks potassium channels in nerve terminals, resulting in an increase in acetylcholine release. This article describes the four randomized placebo-controlled trials of 3,4-DAP in patients with LEMS. All trials demonstrated a significant effect on muscle strength and compound muscle action potential amplitude. Furthermore, the safety and tolerability of 3,4-DAP are reviewed. The side effects of 3,4-DAP are generally mild and most frequently consist of paresthesias, but epileptic seizures and arrhythmias have been described in patients using high doses. Given the efficacy and safety of 3,4-DAP in LEMS, this drug is the mainstay for symptomatic treatment of LEMS.

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Evaluation of 4-aminopyridine and 3,4-diaminopyridine penetrability into cerebrospinal fluid in anesthetized rats

Cited by 63 publications

References 8 publications

Naltrexone potentiates 4-aminopyridine seizures in the rat

Naltrexone potentiates 4-aminopyridine seizures in the rat

A randomised double-blind, cross-over trial of 4-aminopyridine for downbeat nystagmus—effects on slowphase eye velocity, postural stability, locomotion and symptoms

3,4-diaminopyridine for the treatment of Lambert–Eaton myasthenic syndrome

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