Protein Information

Name KCNA5
Synonyms HCK 1; HCK1; HK2; HPCN 1; HPCN1; KCNA 5; KCNA5; KV1.5…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
17876301 Wettwer E: Is there a functional correlate of Kv1.5 in the ventricle of canine heart and what would it mean for the use of I (Kur) blockers?. Br J Pharmacol. 2007 Nov;152(6):835-7. Epub 2007 Sep 17.

The cardiac ultrarapid outward current I (Kur), encoded by KCNA5, is of special pharmacological interest, because it is considered to be atrium-specific.
However, new work has detected a I (Kur)-like current in canine ventricular myocytes, sensitive to 4-aminopyridine and suppressed by the I (Kur) blocker DPO-1, findings that support the existence of a functional ventricular I (Kur).
1(0,0,0,1) Details
15140747 Brevnova EE, Platoshyn O, Zhang S, Yuan JX: Overexpression of human KCNA5 increases IK V and enhances apoptosis. Am J Physiol Cell Physiol. 2004 Sep;287(3):C715-22. Epub 2004 May 12.

Furthermore, ST-induced apoptotic cell shrinkage was significantly accelerated in COS-7 cells and rat PASMC transfected with KCNA5, and blockade of KCNA5 channels with 4-aminopyridine (4-AP) reduced K+ currents through KCNA5 channels and inhibited ST-induced apoptosis in KCNA5-transfected COS-7 cells.
88(1,1,1,8) Details
11349004 London B, Guo W, Pan Xh, Lee JS, Shusterman V, Rocco CJ, Logothetis DA, Nerbonne JM, Hill JA: Targeted replacement of KV1.5 in the mouse leads to loss of the 4-aminopyridine-sensitive component of I (K,slow) and resistance to drug-induced qt prolongation. Circ Res. 2001 May 11;88(9):940-6.
31(0,1,1,1) Details
17267549 Remillard CV, Tigno DD, Platoshyn O, Burg ED, Brevnova EE, Conger D, Nicholson A, Rana BK, Channick RN, Rubin LJ, O'connor DT, Yuan JX: Function of Kv1.5 channels and genetic variations of KCNA5 in patients with idiopathic pulmonary arterial hypertension. Am J Physiol Cell Physiol. 2007 May;292(5):C1837-53. Epub 2007 Jan 31.

Here, we report that overexpression of the Kv1.5 channel gene (KCNA5) in human PASMC and other cell lines produced a 15-pS single channel current and a large whole cell current that was sensitive to 4-aminopyridine.
9(0,0,1,4) 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
20018952 Burg ED, Platoshyn O, Tsigelny IF, Lozano-Ruiz B, Rana BK, Yuan JX: Tetramerization domain mutations in KCNA5 affect channel kinetics and cause abnormal trafficking patterns. Am J Physiol Cell Physiol. 2010 Mar;298(3):C496-509. Epub 2009 Dec 16.

4(0,0,0,4) Details
18774108 Burashnikov A, Antzelevitch C: Can inhibition of IKur promote atrial fibrillation? . Heart Rhythm. 2008 Sep;5(9):1304-9. Epub 2008 Aug 6.

However, it has been shown that I (Kur) block may abbreviate atrial repolarization and that loss-of-function mutations in KCNA5, which encodes K (v) 1.5 channels responsible for I (Kur), is associated with familial AF.
OBJECTIVE: Our objective in this study was to use low concentrations of 4-aminopyridine (4-AP, 10 to 50 microM), known to selectively block I (Kur), to assess the proarrhythmic and antiarrhythmic effects of I (Kur) block in healthy and remodeled atria.
1(0,0,0,1) Details
15673604 Barfield JP, Yeung CH, Cooper TG: The effects of putative K+ channel blockers on volume regulation of murine spermatozoa. Biol Reprod. 2005 May;72(5):1275-81. Epub 2005 Jan 26.

The presence of quinine (0.8 mM), cadmium (0.2 mM), flecainide (100 microM), 4-aminopyridine (4 mM), barium (1 mM), clofilium (10 microM), and phrixotoxin (100 nM) for 75 min resulted in significantly higher forward scatter values than sperm incubated in medium without an inhibitor.
These results imply that channels potentially involved in volume regulation of murine spermatozoa include the voltage-dependent Kv1.4 (also known as KCNA1), Kv1.5 (KCNA5), Kv4.1 (KCND1), Kv4.2 (KCND2), Kv4.3 (KCND3), mink (KCNE1), and acid-sensitive TASK2 (KCNK5) and TASK3 (KCNK9).
1(0,0,0,1) Details
19407249 Kang LS, Kim S, Dominguez JM 2nd, Sindler AL, Dick GM, Muller-Delp JM: Aging and muscle fiber type alter K+ channel contributions to the myogenic response in skeletal muscle arterioles. J Appl Physiol. 2009 Aug;107(2):389-98. Epub 2009 Apr 30.

Myogenic responses of first-order arterioles from the gastrocnemius and soleus muscles of 4- and 24-mo-old Fischer 344 rats were evaluated in the presence and absence of 4-aminopyridine (5 mM) or iberiotoxin (30 nM), inhibitors of KV and BKCa, respectively. 4-Aminopyridine enhanced myogenic tone with aging and normalized age-related differences in both muscle types.
KV1.5 is an integral component of KV channels in vascular smooth muscle; therefore, we determined the relative protein expression of KV1.5, as well as BKCa, in soleus and gastrocnemius arterioles.
1(0,0,0,1) Details