Page last updated: 2024-10-24

potassium channel activity

Definition

Target type: molecularfunction

Enables the facilitated diffusion of a potassium ion (by an energy-independent process) involving passage through a transmembrane aqueous pore or channel without evidence for a carrier-mediated mechanism. [GOC:BHF, GOC:mtg_transport, GOC:pr, ISBN:0815340729]

Potassium channel activity is a fundamental process in cellular physiology, enabling the selective and regulated passage of potassium ions (K+) across cell membranes. This movement of K+ ions is essential for a wide range of physiological functions, including:

* **Membrane potential regulation:** Potassium channels play a crucial role in establishing and maintaining the resting membrane potential of cells. They contribute to the negative charge inside the cell by allowing K+ to flow out, creating a concentration gradient.

* **Action potential generation and propagation:** In excitable cells like neurons and muscle cells, potassium channels are critical for the repolarization phase of action potentials. After the depolarization phase caused by sodium influx, potassium channels open, allowing K+ to exit the cell and restoring the negative membrane potential.

* **Synaptic transmission:** Potassium channels are involved in regulating the release of neurotransmitters at synapses. They contribute to the termination of the action potential at the presynaptic terminal, preventing excessive neurotransmitter release.

* **Cellular signaling and volume control:** Potassium channels are involved in various signaling pathways, including those related to cell growth, differentiation, and apoptosis. They also play a role in regulating cell volume by controlling the movement of K+ ions across the membrane.

* **Muscle contraction and relaxation:** In muscle cells, potassium channels contribute to muscle relaxation by repolarizing the membrane potential, allowing calcium ions to be taken up back into the sarcoplasmic reticulum.

The molecular mechanisms of potassium channel activity involve a complex interplay of structural elements and regulatory mechanisms. Potassium channels are typically composed of four subunits, each containing a pore-forming region that selectively allows the passage of K+ ions. These subunits assemble to form a tetrameric channel structure. The pore region of the channel is lined with amino acids that interact specifically with K+ ions, facilitating their movement through the channel.

The activity of potassium channels is highly regulated by various factors, including voltage, intracellular signaling pathways, and interactions with other proteins. This regulation ensures that potassium channel activity is precisely controlled and tailored to the specific needs of the cell.

The diversity of potassium channels, with various subtypes exhibiting distinct biophysical properties and regulatory mechanisms, underscores their critical role in a wide range of physiological processes. Understanding the molecular function of potassium channels is essential for comprehending normal cellular function and for developing therapeutic strategies for diseases involving potassium channel dysfunction.'
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Proteins (15)

ProteinDefinitionTaxonomy
Intermediate conductance calcium-activated potassium channel protein 4An intermediate conductance calcium-activated potassium channel protein 4 that is encoded in the genome of human. []Homo sapiens (human)
Potassium voltage-gated channel subfamily G member 1A voltage-gated potassium channel KCNG1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9UIX4]Homo sapiens (human)
Potassium channel subfamily K member 9A potassium channel subfamily K member 9 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9NPC2]Homo sapiens (human)
Potassium voltage-gated channel subfamily F member 1A voltage-gated potassium channel KCNF1 that is encoded in the genome of human. []Homo sapiens (human)
Potassium channel subfamily K member 17A potassium channel subfamily K member 17 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q96T54]Homo sapiens (human)
ATP-binding cassette sub-family C member 8An ATP-binding cassette sub-family C member 8 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q09428]Homo sapiens (human)
Potassium voltage-gated channel subfamily C member 4A voltage-gated potassium channel KCNC4 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q03721]Homo sapiens (human)
Potassium channel subfamily K member 10A potassium channel subfamily K member 10 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P57789]Homo sapiens (human)
Potassium voltage-gated channel subfamily KQT member 4A voltage-gated potassium channel subunit KCNQ4 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P56696]Homo sapiens (human)
Aquaporin-1An aquaporin-1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P29972]Homo sapiens (human)
Potassium voltage-gated channel subfamily A member 2A voltage-gated potassium channel subunit KCNA2 that is encoded in the genome of human. []Homo sapiens (human)
Potassium channel subfamily K member 5A potassium channel subfamily K member 5 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O95279]Homo sapiens (human)
ATP-binding cassette sub-family C member 9An ATP-binding cassette sub-family C member 9 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60706]Homo sapiens (human)
Intermediate conductance calcium-activated potassium channel protein 4An intermediate conductance calcium-activated potassium channel protein 4 that is encoded in the genome of human. []Homo sapiens (human)
Potassium channel subfamily K member 3A potassium channel subfamily K member 3 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O14649]Homo sapiens (human)

Compounds (54)

CompoundDefinitionClassesRoles
octoclothepineoctoclothepine: major tranquilizer with action similar to those of the phenothiazines; used in schizophrenic & manic psychoses; minor decriptor (77-86); on-line & INDEX MEDICUS search DIBENZOTHIEPINS (77-86); RN given refers to parent cpd without isomeric designationdibenzothiepine
N-(2-aminoethyl)-5-chloro-1-naphthalenesulfonamidenaphthalenes;
sulfonic acid derivative
5-methoxypsoralen5-methoxypsoralen : A 5-methoxyfurocoumarin that is psoralen substituted by a methoxy group at position 5.

5-Methoxypsoralen: A linear furanocoumarin that has phototoxic and anti-inflammatory properties, with effects similar to METHOXSALEN. It is used in PUVA THERAPY for the treatment of PSORIASIS.
5-methoxyfurocoumarin;
organic heterotricyclic compound;
psoralens
hepatoprotective agent;
plant metabolite
bupivacaine1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide : A piperidinecarboxamide obtained by formal condensation of the carboxy group of N-butylpipecolic acid with the amino group of 2,6-dimethylaniline.

bupivacaine : A racemate composed of equimolar amounts of dextrobupivacaine and levobupivacaine. Used (in the form of its hydrochloride hydrate) as a local anaesthetic.

Bupivacaine: A widely used local anesthetic agent.
aromatic amide;
piperidinecarboxamide;
tertiary amino compound
carvedilolcarbazoles;
secondary alcohol;
secondary amino compound
alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
clotrimazoleconazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes
antiinfective agent;
environmental contaminant;
xenobiotic
diazoxidediazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.

Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.
benzothiadiazine;
organochlorine compound;
sulfone
antihypertensive agent;
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
diuretic;
K-ATP channel agonist;
sodium channel blocker;
sympathomimetic agent;
vasodilator agent
glyburideglyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.

Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide
monochlorobenzenes;
N-sulfonylurea
anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
lidocainelidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.

Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.
benzenes;
monocarboxylic acid amide;
tertiary amino compound
anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
loratadineloratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.

Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.
benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide
anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
mepivacainemepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic.

Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168)
piperidinecarboxamidedrug allergen;
local anaesthetic
mexiletinemexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol.

Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.
aromatic ether;
primary amino compound
anti-arrhythmia drug
pinacidilPinacidil: A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)pyridines
propafenonepropafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.

Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.
aromatic ketone;
secondary alcohol;
secondary amino compound
anti-arrhythmia drug
tetracainetetracaine : A benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia.

Tetracaine: A potent local anesthetic of the ester type used for surface and spinal anesthesia.
benzoate ester;
tertiary amino compound
local anaesthetic
troglitazoneTroglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.chromanes;
thiazolidinone
anticoagulant;
anticonvulsant;
antineoplastic agent;
antioxidant;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
hypoglycemic agent;
platelet aggregation inhibitor;
vasodilator agent
etidocaineetidocaine : An amino acid amide in which 2-[ethyl(propyl)amino]butanoic acid and 2,6-dimethylaniline have combined to form the amide bond. Used as a local anaesthetic (amide caine), it has rapid onset and long action properties, similar to bupivacaine, and is given by injection during surgical procedures and during labour and delivery.

Etidocaine: A local anesthetic with rapid onset and long action, similar to BUPIVACAINE.
amino acid amidelocal anaesthetic
n-cyano-n'-(1,1-dimethylpropyl)-n''-(3-pyridinyl)guanidineN-cyano-N'-(1,1-dimethylpropyl)-N''-(3-pyridinyl)guanidine: potassium channel openerpyridines
flupirtineflupirtine: RN given refers to parent cpd without isomeric designationaminopyridine
mibefradil dihydrochloride
mevastatinmevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.

mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure
2-pyranones;
carboxylic ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)
antifungal agent;
apoptosis inducer;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
fungal metabolite;
Penicillium metabolite
repaglinidepiperidines
triphenylacetic acid
cromakalimCromakalim: A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also been tried in patients with asthma. (Martindale, The Extra Pharmacopoeia, 30th ed, p352)
rosiglitazoneaminopyridine;
thiazolidinediones
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
ezogabineezogabine : A substituted aniline that is benzene-1,2,4-triamine bearing ethoxycarbonyl and 4-fluorobenzyl substituents at positions N-1 and N-4 respectively. An anticonvulsant used to treat seizures associated with epilepsy in adults.

ezogabine: structure in first source
carbamate ester;
organofluorine compound;
secondary amino compound;
substituted aniline
anticonvulsant;
potassium channel modulator
mk 7675-((2,4-dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide: an antihyperlipidemic agent that also functions as an insulin sensitizer, PPARalpha agonist, and PPARgamma agonist; structure in first source
ropivacaine(S)-ropivacaine : A piperidinecarboxamide-based amide-type local anaesthetic (amide caine) in which (S)-N-propylpipecolic acid and 2,6-dimethylaniline are combined to form the amide bond.

ropivacaine : The piperidinecarboxamide obtained by the formal condensation of N-propylpipecolic acid and 2,6-dimethylaniline.

Ropivacaine: An anilide used as a long-acting local anesthetic. It has a differential blocking effect on sensory and motor neurons.
piperidinecarboxamide;
ropivacaine
local anaesthetic
zeneca zd 6169Zeneca ZD 6169: an ATP-sensitive potassium channel opener; structure given in first source
bms204352BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source
senicapocsenicapoc: a Gardos channel blocker; structure in first source
cromakalim1-benzopyran
(2'-(benzyloxycarbonylaminomethyl)biphenyl-2-carboxylic acid 2-(2-pyridyl)ethylamide)biphenyls
tram 34TRAM 34: inhibits IKCa1; structure in first sourceorganochlorine compound
clamikalantclamikalant: inhibits ATP-sensitive potassium channel; structure in first source
N-(2,4,6-trimethylphenyl)-3-bicyclo[2.2.1]heptanecarboxamidemonoterpenoid
zm226600ZM226600: an ATP-sensitive potassium channel opener; structure in first sourceanilide
anandamideanandamide : An N-acylethanolamine 20:4 resulting from the formal condensation of carboxy group of arachidonic acid with the amino group of ethanolamine.endocannabinoid;
N-acylethanolamine 20:4
human blood serum metabolite;
neurotransmitter;
vasodilator agent
cgp 71683 anaphthalenes;
sulfonic acid derivative
clathrodinclathrodin: structure given in first source; isolated from marine sponges of the genus Agelas
oroidinoroidin: from marine sponges of the genus Agelas; structure in first sourcepyrroles;
secondary carboxamide
metabolite
am-356methanandamide: structure given in first source; RN given refers to (all-Z)-(+-)-isomerfatty amide
hymenidinhymenidin: serotonergic receptor antagonist from Okinawan marine sponge Hymeniacidon; structure given in first source
gw2974GW2974: quinazoline derivative, which is able to block the activation of both the EGFR and erbB2pyridopyrimidine
ave 0118
a 1899A 1899: a TASK-1 potassium channel blocker; structure in first source
way 133537
ly 465608LY 465608: a nonthiazolidinedione agonist of both PPAR-alpha and PPAR-gamma of Ligand Pharm. and Eli Lilly
ica 27243N-(6-Chloropyridin-3-yl)-3,4-difluorobenzamide: a KCNQ2/3 channel activator; structure in first source
bm 131246
octoclothepine maleate
(r)-n-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide(R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide: structure in first source
nn 414NN 414: a hypoglycemic agent with insulin release modulating and potassium channel activating activities; structure in first source
7-chloro-3-isopropylamino-4h-1,2,4-benzothiadiazine 1,1-dioxide7-chloro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide: activates ATP-sensitive potassium channels; structure in first source