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Biological Activity for 4-Aminopyridine
4-Aminopyridine is a non-selective voltage-dependent K+-channel blocker (IC50 values are 170 and 230 μM at KV1.1 and KV1.2 respectively). Caged 4-AP (Cat. No. 3557) is also available.
Technical Data for 4-Aminopyridine
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for 4-Aminopyridine
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for 4-Aminopyridine
The following data is based on the product molecular weight 94.12. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||10.62 mL||53.12 mL||106.25 mL|
|5 mM||2.12 mL||10.62 mL||21.25 mL|
|10 mM||1.06 mL||5.31 mL||10.62 mL|
|50 mM||0.21 mL||1.06 mL||2.12 mL|
References for 4-Aminopyridine
References are publications that support the biological activity of the product.
Bouchard and Fedida (1995) Closed and open state binding of 4-aminopyridine to the cloned human potassium channel Kv1.5. J.Pharmacol.Exp.Ther. 275 864 PMID: 7473178
Smith et al (2009) In vitro electrophysiological activity of nerispirdine, a novel 4-aminopyridine derivative. Clin.Exp.Pharmacol.Physiol. 36 1104 PMID: 19413590
Tseng et al (1996) Reverse use dependence of Kv4.2 blockade by 4-aminopyridine. J.Pharmacol.Exp.Ther. 279 865 PMID: 8930194
Tseng (1999) Different state dependencies of 4-aminopyridine binding to rKv1.4 and rKv4.2: role of the cytoplasmic halves of the fifth and sixth transmembrane segments. J.Pharmacol.Exp.Ther. 290 569 PMID: 10411564
If you know of a relevant reference for 4-Aminopyridine, please let us know.
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Keywords: 4-Aminopyridine, 4-Aminopyridine supplier, K+, channel, blocker, Potassium, Channels, voltage-gated, voltage-dependent, Kv, hERG, Human, Ether-A-Go-Go, Gene, KCNQ, 4-AP, Voltage-Gated, 0940, Tocris Bioscience
32 Citations for 4-Aminopyridine
Citations are publications that use Tocris products. Selected citations for 4-Aminopyridine include:
Beas et al (2018) The locus coeruleus drives disinhibition in the midline thalamus via a dopaminergic mechanism. Nat Neurosci 21 963 PMID: 29915192
Collins et al (2018) Reciprocal Circuits Linking the Prefrontal Cortex with Dorsal and Ventral Thalamic Nuclei. Neuron 98 366 PMID: 29628187
Dong et al (2018) CAST/ELKS Proteins Control Voltage-Gated Ca2+ Channel Density and Synaptic Release Probability at a Mammalian Central Synapse. Cell Rep 24 284 PMID: 29996090
Li et al (2018) Hypothalamic Circuits for Predation and Evasion. Neuron 97 911 PMID: 29398361
Fan et al (2018) All-optical synaptic electrophysiology probes mechanism of ketamine-induced disinhibition. Nat Methods 15 823 PMID: 30275587
Chang and Higley (2018) Potassium channels contribute to activity-dependent regulation of dendritic inhibition. Physiol Rep 6 e13747 PMID: 29939492
Saunders et al (2015) Corelease of acetylcholine and GABA from cholinergic forebrain neurons. Front Neural Circuits 4 PMID: 25723967
Curcio et al (2015) Brain ischemia downregulates the neuroprotective GDNF-Ret signaling by a calpain-dependent mechanism in cultured hippocampal neurons. J Neurosci 6 e1645 PMID: 25675305
Cramer et al (2015) Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse. Front Cell Neurosci 35 5664 PMID: 25855180
Robinson et al (2015) Tissue plasminogen activator inhibits NMDA-receptor-mediated increases in calcium levels in cultured hippocampal neurons. J Neurosci 9 404 PMID: 26500501
Sun (2009) Experience-dependent intrinsic plasticity in interneurons of barrel cortex layer IV. EMBO J 102 2955 PMID: 19741102
Chiu et al (2019) NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content. Cell Rep 28 332 PMID: 31291571
Chanda et al (2014) Generation of induced neuronal cells by the single reprogramming factor ASCL1. J Neurosci 3 282 PMID: 25254342
Grace et al (2014) Identification of a pharmacological target for genioglossus reactivation throughout sleep. Elife 37 41 PMID: 24470694
Zhao et al (2017) A Central Catecholaminergic Circuit Controls Blood Glucose Levels during Stress. Neuron 95 138 PMID: 28625488
Gutzmann et al (2019) Functional Coupling of Cav2.3 and BK Potassium Channels Regulates Action Potential Repolarization and Short-Term Plasticity in the Mouse Hippocampus. Front Cell Neurosci 13 27 PMID: 30846929
Leal et al (2014) Neuronal activity induces synaptic delivery of hnRNP A2/B1 by a BDNF-dependent mechanism in cultured hippocampal neurons. PLoS One 9 e108175 PMID: 25286195
Chanda et al (2013) Neurons generated by direct conversion of fibroblasts reproduce synaptic phenotype caused by autism-associated neuroligin-3 mutation. J Biol Chem 110 16622 PMID: 24046374
Fontán-Lozano et al (2011) The A-current modulates learning via NMDA receptors containing the NR2B subunit. PLoS One 6 e24915 PMID: 21966384
Restituito et al (2011) Synaptic autoregulation by metalloproteases and γ-secretase. J Neurosci 31 12083 PMID: 21865451
Léveillé et al (2008) Neuronal viability is controlled by a functional relation between synaptic and extrasynaptic NMDA receptors. FASEB J 22 4258 PMID: 18711223
Dinamarca et al (2016) Ring finger protein 10 is a novel synaptonuclear messenger encoding activation of NMDA receptors in hippocampus. Elife 5 PMID: 26977767
Kaufman et al (2012) Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons. Sleep 32 3992 PMID: 22442066
Saliba et al (2012) Activity-dependent phosphorylation of GABAA receptors regulates receptor insertion and tonic current. J Neurophysiol 31 2937 PMID: 22531784
Hagiwara et al (2012) Optophysiological analysis of associational circuits in the olfactory cortex. Cell Death Dis 6 18 PMID: 22529781
Zhang et al (2018) Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation. Neuron 98 918 PMID: 29754751
Han et al (2007) DArgic modulation of spinal neuronal excitability. J Neurophysiol 27 13192 PMID: 18045913
Kiritoshi and Neugebauer (2018) Pathway-specific alterations of cortico-amygdala transmission in an arthritis pain model. ACS Chem Neurosci 9 2252 PMID: 29630339
Shulga et al (2012) The loop diuretic bumet. blocks posttraumatic p75NTR upregulation and rescues injured neurons. J Neurosci 32 1757 PMID: 22302815
Gaamouch et al (2012) Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity. J Neurosci 32 10767 PMID: 22855824
Gómez-Gonzalo et al (2010) An excitatory loop with astrocytes contributes to drive neurons to seizure threshold. PLoS Biol 8 e1000352 PMID: 20405049
Lenz and Avruch (2005) Glutamatergic regulation of the p70S6 kinase in primary mouse neurons. Stem Cell Reports 280 38121 PMID: 16183639
Do you know of a great paper that uses 4-Aminopyridine from Tocris? Please let us know.
Reviews for 4-Aminopyridine
Average Rating: 4.5 (Based on 2 Reviews.)
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We increased synaptic activity using a standard pharmacological approach (20 μM bicuculline and 100 μM 4-AP.
Our cell biology lab uses 4 Aminopyridine block Kv channels on different cell lines expressing different Kv channel from all across human body. The product works excellent and few papers have been published where it has been used. Greatly recommend.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.