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extracellularly ATP-gated monoatomic cation channel activity

Definition

Target type: molecularfunction

Enables the transmembrane transfer of a monoatomic cation by a channel that opens when ATP is bound by the channel complex or one of its constituent parts on the extracellular side of the plasma membrane. [GOC:bf, GOC:mah, PMID:9755289]

Extracellularly ATP-gated monoatomic cation channel activity refers to a specific type of ion channel protein that is activated by the binding of ATP (adenosine triphosphate) to a site on the extracellular surface of the protein. This activation leads to the opening of the channel, allowing the passage of monoatomic cations, such as sodium (Na+), potassium (K+), and calcium (Ca2+). The channel remains closed when ATP is not bound. The molecular function of these channels involves a complex interplay of structural elements and specific amino acid residues. Upon ATP binding, conformational changes occur in the channel protein, ultimately leading to the opening of the pore. This opening allows for the flow of specific cations across the cell membrane, contributing to various physiological processes. These channels are essential for diverse cellular functions, including nerve impulse transmission, muscle contraction, and regulation of cellular volume and excitability. For instance, in neurons, ATP-gated cation channels contribute to synaptic transmission, allowing for the rapid communication between cells. Additionally, these channels play crucial roles in the regulation of vascular tone and the contraction of smooth muscle cells.'
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Proteins (6)

ProteinDefinitionTaxonomy
P2X purinoceptor 2A P2X purinoceptor 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UBL9]Homo sapiens (human)
P2X purinoceptor 7A P2X purinoceptor 7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99572]Homo sapiens (human)
P2X purinoceptor 4A P2X purinoceptor 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99571]Homo sapiens (human)
P2X purinoceptor 5A P2X purinoceptor 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q93086]Homo sapiens (human)
P2X purinoceptor 3A P2X purinoceptor 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P56373]Homo sapiens (human)
P2X purinoceptor 1A P2X purinoceptor 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P51575]Homo sapiens (human)

Compounds (47)

CompoundDefinitionClassesRoles
pyridoxal phosphatepyridoxal 5'-phosphate : The monophosphate ester obtained by condensation of phosphoric acid with the primary hydroxy group of pyridoxal.

Pyridoxal Phosphate: This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).
methylpyridines;
monohydroxypyridine;
pyridinecarbaldehyde;
vitamin B6 phosphate
coenzyme;
cofactor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
carbamazepinecarbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.

Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.
dibenzoazepine;
ureas
analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
carbamazepine epoxidecarbamazepine epoxide: metabolite of carbamazepine; RN given refers to unlabeled cpd

carbamazepine-10,11-epoxide : An epoxide and metabolite of carbamazepine.
dibenzoazepine;
epoxide;
ureas
allergen;
drug metabolite;
marine xenobiotic metabolite
oxatomideoxatomide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one substituted by a 3-[4-(diphenylmethyl)piperazin-1-yl]propyl group at position 1. It is an anti-allergic drug.

oxatomide: structure; an anti-allergic & an anti-asthmatic
benzimidazoles;
diarylmethane;
N-alkylpiperazine
anti-allergic agent;
anti-inflammatory agent;
geroprotector;
H1-receptor antagonist;
serotonergic antagonist
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid5'-phosphopyridoxal-6-azobenzene-2,4-disulfonic acid : An arenesulfonic acid that is pyridoxal 5'-phosphate carrying an additional 2,4-disulfophenylazo substituent at position 6.

pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid: a novel antagonist that selectively blocks P2 purinoceptor receptors; a useful tool to study co-transmission in tissues when ATP and coexisting neurotransmitters act in concert
arenesulfonic acid;
azobenzenes;
methylpyridines;
monohydroxypyridine;
organic phosphate;
pyridinecarbaldehyde
purinergic receptor P2X antagonist
suraminsuramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.

Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.
naphthalenesulfonic acid;
phenylureas;
secondary carboxamide
angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
adenosine diphosphateAdenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.adenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate
fundamental metabolite;
human metabolite
10,11-dihydrocarbamazepine
diadenosine tetraphosphateP(1),P(4)-bis(5'-adenosyl) tetraphosphate : A diadenosyl tetraphosphate compound having the two 5'-adenosyl residues attached at the P(1)- and P(4)-positions.diadenosyl tetraphosphateEscherichia coli metabolite;
mouse metabolite
ormetoprimormetoprim: proposed chemotherapeutic agent; minor descriptor (75-84); on-line & Index Medicus search PYRIMIDINES (75-84)dimethoxybenzene
arylid
oxcarbazepineoxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy.

Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.
cyclic ketone;
dibenzoazepine
anticonvulsant;
drug allergen
paroxetineparoxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.

Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.
aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines
antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
9-chloroacridine9-chloroacridine: chromogenic reagent for detection of arylhydroxylamines & arylamines on paper & thin layer chromatograms; structure
5'-adenylyl (beta,gamma-methylene)diphosphonate5'-adenylyl (beta,gamma-methylene)diphosphonate: do not confuse with alpha,beta-methyleneadenosine 5'-triphosphatenucleoside triphosphate analogue
alpha,beta-methyleneadenosine 5'-triphosphatealpha,beta-methyleneadenosine 5'-triphosphate: do not confuse with beta,gamma-methylene ATP; RN given refers to parent cpdnucleoside triphosphate analogue
10-hydroxycarbamazepine10,11-dihydro-10-hydroxycarbamazepine: main metabolite of oxcarbazepine; structure given in first source

licarbazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine, reduced across the C-10,11 positions and carrying a carbamoyl substituent at the azepine nitrogen and a hydroxy function at C-10. A voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects, it is related to oxcarbazepine and is an active metabolite of oxcarbazepine.
carboxamide;
dibenzoazepine;
ureas
anticonvulsant;
drug allergen;
sodium channel blocker
sb 203580imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
eslicarbazepine acetateeslicarbazepine acetate : The acetate ester, with S configuration, of licarbazepine. An anticonvulsant, it is approved for use in Europe and the United States as an adjunctive therapy for epilepsy.acetate ester;
carboxamide;
dibenzoazepine;
ureas
anticonvulsant;
drug allergen
adenosine 5'-o-(3-thiotriphosphate)adenosine 5'-[gamma-thio]triphosphate : A nucleoside triphosphate analogue that is ATP in which one of the oxygens attached to 3-phosphate group is replaced by sulfur.

adenosine 5'-O-(3-thiotriphosphate): RN given refers to cpd with unspecified locant for thio group; see also records for 1-thio & 2-thio-isomers
nucleoside triphosphate analogue
1-(5H-dibenzo[b,f]azepin-5-yl)ethan-1-onedibenzooxazepine
8-azidoadenosine 5'-triphosphate
6-thioinosine-5'-triphosphateorganic molecule
spinorphinspinorphin: heptapeptide which is a potent inhibitor of enkephalin-degrading enzymes from the spinal cord or brain; does not show inhibitory activity toward enkephalin-degrading enzymes from kidney or blood; member of the opioid hemorphin familyoligopeptide
mrs 2219MRS 2219: P2X1 receptor agonist; structure in first source
mrs2159MRS2159: an antagonist of both P2X1 and P2X7 receptors
imd 0354N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide: a cardioprotective agent that inhibits IkappaB kinase beta (IKKbeta); structure in first sourcebenzamides
2-methylthio-atp2-methylthio-ATP: purinergic receptors agonist; relaxes mammalian gut preparations; structure given in first source
adp beta sadenosine 5'-O-(2-thiodiphosphate): partial agonist toward platelet aggregation; see also record for 1-thiodiphosphate cpd
kn 62KN 62: inhibitor of Ca/calmodulin-dependent protein kinase IIpiperazines
nf023
nf 449
bafilomycin a1bafilomycin A1 : The most used of the bafilomycins, a family of toxic macrolide antibiotics derived from Streptomyces griseus.

bafilomycin A1: from Streptomyces griseus; structure given in first source
cyclic hemiketal;
macrolide antibiotic;
oxanes
apoptosis inducer;
autophagy inhibitor;
bacterial metabolite;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.14 (H(+)-transporting two-sector ATPase) inhibitor;
ferroptosis inhibitor;
fungicide;
potassium ionophore;
toxin
az 11645373AZ 11645373: InChIKey: VQEHBLGYANQWEA-UHFFFAOYSA-N
a-317491A-317491: structure in first source
az10606120AZ10606120: a P2X7 receptor antagonist
ce 224,535CE 224,535: structure in first source
a-438079
af 3535-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine: a P2X3 and P2X2/3 receptor antagonist; structure in first source
a 803467A 803467: an Nav1.8 sodium channel blocker; structure in first source
archazolid aarchazolid A: inhibits vacuolar-type ATPase; isolated from Archangium gephyra; structure in first source
archazolid barchazolid B: structure in first sourcemacrolide
gsk1482160
af-219Gefapixant: a P2X3 receptor antagonist
a-839977A-839977: a selective P2X7 receptor antagonist, analgesic; structure in first source
jnj-47965567JNJ-47965567: a P2X7 purinergic receptor antagonist; structure in first source
mk-8742elbasvir : A complex organic heterotetracyclic compound that is a hepatitis C virus nonstructural protein 5A inhibitor used in combination with grazoprevir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults.

elbasvir: inhibits NS5A protein of hepatitis C virus
carbamate ester;
imidazoles;
L-valine derivative;
N-acylpyrrolidine;
organic heterotetracyclic compound;
ring assembly
antiviral drug;
hepatitis C virus nonstructural protein 5A inhibitor;
hepatoprotective agent