Page last updated: 2024-10-24
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)
| Protein | Definition | Taxonomy |
|---|---|---|
| P2X purinoceptor 2 | A P2X purinoceptor 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UBL9] | Homo sapiens (human) |
| P2X purinoceptor 7 | A P2X purinoceptor 7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99572] | Homo sapiens (human) |
| P2X purinoceptor 4 | A P2X purinoceptor 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99571] | Homo sapiens (human) |
| P2X purinoceptor 5 | A P2X purinoceptor 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q93086] | Homo sapiens (human) |
| P2X purinoceptor 3 | A P2X purinoceptor 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P56373] | Homo sapiens (human) |
| P2X purinoceptor 1 | A P2X purinoceptor 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P51575] | Homo sapiens (human) |
Compounds (47)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| pyridoxal phosphate | pyridoxal 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 |
| carbamazepine | carbamazepine : 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 epoxide | carbamazepine 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 |
| oxatomide | oxatomide : 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 acid | 5'-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 |
| suramin | suramin : 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 diphosphate | Adenosine 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 tetraphosphate | P(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 tetraphosphate | Escherichia coli metabolite; mouse metabolite |
| ormetoprim | ormetoprim: proposed chemotherapeutic agent; minor descriptor (75-84); on-line & Index Medicus search PYRIMIDINES (75-84) | dimethoxybenzene | |
| arylid | |||
| oxcarbazepine | oxcarbazepine : 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 |
| paroxetine | paroxetine : 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-chloroacridine | 9-chloroacridine: chromogenic reagent for detection of arylhydroxylamines & arylamines on paper & thin layer chromatograms; structure | ||
| 5'-adenylyl (beta,gamma-methylene)diphosphonate | 5'-adenylyl (beta,gamma-methylene)diphosphonate: do not confuse with alpha,beta-methyleneadenosine 5'-triphosphate | nucleoside triphosphate analogue | |
| alpha,beta-methyleneadenosine 5'-triphosphate | alpha,beta-methyleneadenosine 5'-triphosphate: do not confuse with beta,gamma-methylene ATP; RN given refers to parent cpd | nucleoside triphosphate analogue | |
| 10-hydroxycarbamazepine | 10,11-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 203580 | imidazoles; 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 acetate | eslicarbazepine 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-one | dibenzooxazepine | ||
| 8-azidoadenosine 5'-triphosphate | |||
| 6-thioinosine-5'-triphosphate | organic molecule | ||
| spinorphin | spinorphin: 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 family | oligopeptide | |
| mrs 2219 | MRS 2219: P2X1 receptor agonist; structure in first source | ||
| mrs2159 | MRS2159: an antagonist of both P2X1 and P2X7 receptors | ||
| imd 0354 | N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide: a cardioprotective agent that inhibits IkappaB kinase beta (IKKbeta); structure in first source | benzamides | |
| 2-methylthio-atp | 2-methylthio-ATP: purinergic receptors agonist; relaxes mammalian gut preparations; structure given in first source | ||
| adp beta s | adenosine 5'-O-(2-thiodiphosphate): partial agonist toward platelet aggregation; see also record for 1-thiodiphosphate cpd | ||
| kn 62 | KN 62: inhibitor of Ca/calmodulin-dependent protein kinase II | piperazines | |
| nf023 | |||
| nf 449 | |||
| bafilomycin a1 | bafilomycin 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 11645373 | AZ 11645373: InChIKey: VQEHBLGYANQWEA-UHFFFAOYSA-N | ||
| a-317491 | A-317491: structure in first source | ||
| az10606120 | AZ10606120: a P2X7 receptor antagonist | ||
| ce 224,535 | CE 224,535: structure in first source | ||
| a-438079 | |||
| af 353 | 5-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine: a P2X3 and P2X2/3 receptor antagonist; structure in first source | ||
| a 803467 | A 803467: an Nav1.8 sodium channel blocker; structure in first source | ||
| archazolid a | archazolid A: inhibits vacuolar-type ATPase; isolated from Archangium gephyra; structure in first source | ||
| archazolid b | archazolid B: structure in first source | macrolide | |
| gsk1482160 | |||
| af-219 | Gefapixant: a P2X3 receptor antagonist | ||
| a-839977 | A-839977: a selective P2X7 receptor antagonist, analgesic; structure in first source | ||
| jnj-47965567 | JNJ-47965567: a P2X7 purinergic receptor antagonist; structure in first source | ||
| mk-8742 | elbasvir : 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 |