Protein Information

Name voltage gated K channel (protein family or complex)
Synonyms Voltage gated K channel; Voltage gated potassium channel

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
11454932 Ceron PI, Cremonez DC, Bendhack LM, Tedesco AC: The relaxation induced by S-nitroso-glutathione and S-nitroso-N-acetylcysteine in rat aorta is not related to nitric oxide production. J Pharmacol Exp Ther. 2001 Aug;298(2):686-94.


The relaxation induced by GSNO and NACysNO was inhibited by the K+ channel blockers glibenclamide, selective K (ATP) channels, and apamin, selective for low-conductance Ca2+-activated K+ channels in rat aorta, but was not inhibited by charybdotoxin, a potent and selective Ca2+-activated K+ channel blocker, or by 4-aminopyridine, a voltage-gated K+ channel blocker.
0(0,0,0,0) Details
17327035 Weng ZP, Wang B, Wang SL, Cui N, Pan XY: [Influence of 4-aminopyridine on cell proliferation through inhibiting voltage-gated K+ channel in ovarian cancer]. Zhonghua Fu Chan Ke Za Zhi. 2006 Nov;41(11):762-5.
81(1,1,1,1) Details
19134331 Zhao ZM, Cui N, Xu SX, Gao FL, Hao GM, Cao JF: [Influence of 4-aminopyridine on human ovarian luteinized granulosa cell proliferation, production, and apoptosis through inhibiting voltage-gated K+ channel]. Zhonghua Fu Chan Ke Za Zhi. 2008 Dec;43(12):918-22.
81(1,1,1,1) Details
14527939 Li H, Guo W, Yamada KA, Nerbonne JM: Selective elimination of I (K,slow1) in mouse ventricular myocytes expressing a dominant negative Kv1.5alpha subunit. Am J Physiol Heart Circ Physiol. 2004 Jan;286(1):H319-28. Epub 2003 Oct 2.

Although previous studies have revealed a role for the voltage-gated K+ channel alpha-subunit Kv1.5 (KCNA5) in the generation of the 4-aminopyridine (4-AP)-sensitive component of delayed rectification in mouse ventricles (IK,slow1), the phenotypic consequences of manipulating IK,slow1 expression in vivo in different (mouse) models are distinct.
6(0,0,1,1) Details
18982871 Gan XG, An RH, Bai YF, Zong DB: Expressions of voltage-gated K+ channel 2.1 and 2.2 in rat bladder with detrusor hyperreflexia. Chin Med J. 2008 Aug 20;121(16):1574-7.

The frequency of DH in the experimental group was significantly different from that in the control group with or without treatment with 4-aminopyridine (4-AP) (P < 0.05), while the amplitude of DH did not change markedly.
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14632936 Chang KW, Yuan TC, Fang KP, Yang FS, Liu CJ, Chang CS, Lin SC: The increase of voltage-gated potassium channel Kv3.4 mRNA expression in oral squamous cell carcinoma. J Oral Pathol Med. 2003 Nov;32(10):606-11.

METHODS: We examined the expression of an A-type voltage-gated K+ channel, Kv3.4, in oral squamous cell carcinoma (OSCC) and esophageal squamous cell carcinoma (ESCC) compared with non-cancerous matched tissue (NCMT) using RT-PCR analysis.
In addition, administration of an A-type K+ channel blocker, 4-aminopyridine (4-AP), and an antisense oligodeoxynucleotide (ODN) directed specifically against Kv3.4 were performed to identify the involvement of Kv3.4 in the growth of OSCC cells.
1(0,0,0,1) Details
12679374 Thorneloe KS, Nelson MT: Properties and molecular basis of the mouse urinary bladder voltage-gated K+ current. J Physiol. 2003 May 15;549(Pt 1):65-74. Epub 2003 Apr 4.

The IK (V) was blocked by tetraethylammonium ions with an IC50 of 5.2 mM and was unaffected by 1 mM 4-aminopyridine.
RT-PCR for voltage-gated K+ channel (KV) subunits revealed the expression of Kv2.1, Kv5.1, Kv6.1, Kv6.2 and Kv6.3 in isolated UBSM myocytes.
1(0,0,0,1) Details
12838421 Fraser SP, Grimes JA, Diss JK, Stewart D, Dolly JO, Djamgoz MB: Predominant expression of Kv1.3 voltage-gated K+ channel subunit in rat prostate cancer cell lines: electrophysiological, pharmacological and molecular characterisation. Pflugers Arch. 2003 Aug;446(5):559-71. Epub 2003 Jul 1.

Thus, the currents were blocked by 4-aminopyridine, tetraethylammonium, verapamil, margatoxin, and charybdotoxin, with highly similar IC (50) s for given blockers.
1(0,0,0,1) Details
10856117 Korngreen A, Sakmann B: Voltage-gated K+ channels in layer 5 neocortical pyramidal neurones from young rats: subtypes and gradients. J Physiol. 2000 Jun 15;525 Pt 3:621-39.

The results suggest that the decrease of the voltage-gated K+ channel density from the soma along the apical dendrite of L5 pyramidal neurones helps to define a distal, low threshold region for the initiation of dendritic regenerative potentials.
The slow K+ current was completely blocked by tetraethylammonium (TEA) with an IC50 of 5 +/- 1 mM (mean +/- s.e.m.) and was partially blocked by 4-aminopyridine (4-AP).
1(0,0,0,1) Details
12062371 Belevych AE, Beck R, Tammaro P, Poston L, Smirnov SV: Developmental changes in the functional characteristics and expression of voltage-gated K+ channel currents in rat aortic myocytes. Cardiovasc Res. 2002 Apr;54(1):152-61.

I (Kv) in neonates was insensitive to a high concentration of tetraethylammonium (TEA, 10 mM) but blocked 4-aminopyridine (4-AP, IC (50)=0.5+/-0.1 mM), whereas I (Kv) in adult RAMs was almost completely abolished by 10 mM TEA and was relatively insensitive to low concentrations of 4-AP.
1(0,0,0,1) Details
19332619 Wang Z, Wong NC, Cheng Y, Kehl SJ, Fedida D: Control of voltage-gated K+ channel permeability to NMDG+ by a residue at the outer pore. J Gen Physiol. 2009 Apr;133(4):361-74.

The NMDG (+) current was inhibited by extracellular 4-aminopyridine (5 mM) or tetraethylammonium (10 mM), and largely eliminated in Kv3.2b by an S6 mutation that prevents the channel from opening (P468W) and by a pore helix mutation in Kv1.5 R487Y (W472F) that inactivates the channel at rest.
1(0,0,0,1) Details
12689856 Lin MT, Hessinger DA, Pearce WJ, Longo LD: Developmental differences in Ca2+-activated K+ channel activity in ovine basilar artery. Am J Physiol Heart Circ Physiol. 2003 Aug;285(2):H701-9. Epub 2003 Apr 10.


To test the hypothesis that these contractility differences result from maturational changes in voltage-gated K+ channel function, we compared this function in VSM myocytes from adult and fetal sheep cerebral arteries.
1(0,0,0,1) Details
11401838 Ekhterae D, Platoshyn O, Krick S, Yu Y, McDaniel SS, Yuan JX: Bcl-2 decreases voltage-gated K+ channel activity and enhances survival in vascular smooth muscle cells. Am J Physiol Cell Physiol. 2001 Jul;281(1):C157-65.

Blockade of Kv channels in control cells (-bcl-2) by 4-aminopyridine also inhibited the ST-induced increase in I (Kv) and apoptosis.
1(0,0,0,1) Details
10836990 Lang R, Lee G, Liu W, Tian S, Rafi H, Orias M, Segal AS, Desir GV: KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels. Am J Physiol Renal Physiol. 2000 Jun;278(6):F1013-21.

We conclude KCNA10 is a novel human voltage-gated K channel with features common to both K-selective and CNG cation channels.
The channel displays an unusual inhibitor profile because, in addition to being blocked by classical K channel blockers (barium tetraethylammonium and 4-aminopyridine), it is also sensitive to inhibitors of cyclic nucleotide-gated (CNG) cation channels (verapamil and pimozide).
1(0,0,0,1) Details