Target type: biologicalprocess
A process in which membrane potential cycles through a depolarizing spike, triggered in response to depolarization above some threshold, followed by repolarization. This cycle is driven by the flow of ions through various voltage gated channels with different thresholds and ion specificities. [GOC:dph, GOC:go_curators, GOC:tb, ISBN:978-0-07-139011-8]
An action potential is a rapid, transient change in the electrical potential across the plasma membrane of a neuron or muscle cell, which transmits signals along the cell. It is a fundamental process in the nervous system, enabling communication between neurons and the initiation of muscle contractions.
The action potential arises from the coordinated movement of ions across the cell membrane, primarily sodium (Na+) and potassium (K+). These ions flow through voltage-gated channels, specialized proteins embedded in the membrane that open or close in response to changes in membrane potential.
**Steps in Action Potential Generation:**
1. **Resting potential:** In the resting state, the neuron maintains a negative membrane potential, typically around -70 mV. This is due to a higher concentration of K+ inside the cell and Na+ outside the cell, maintained by the sodium-potassium pump.
2. **Depolarization:** When a stimulus, such as a neurotransmitter, triggers the opening of Na+ channels, Na+ ions rush into the cell, causing the membrane potential to become less negative. This is known as depolarization. If the depolarization reaches a threshold level, typically around -55 mV, an action potential is triggered.
3. **Rising phase:** Once the threshold is reached, the influx of Na+ ions becomes self-reinforcing, leading to a rapid and dramatic rise in membrane potential. This phase is known as the rising phase or upstroke of the action potential. The membrane potential reaches a peak value of around +30 mV.
4. **Repolarization:** As the membrane potential reaches its peak, the Na+ channels begin to inactivate, while K+ channels open. This allows K+ ions to flow out of the cell, bringing the membrane potential back towards its resting value. This phase is called repolarization.
5. **Hyperpolarization:** In some cases, the membrane potential may briefly become more negative than the resting potential, a phenomenon called hyperpolarization. This is due to the continued outflow of K+ ions.
6. **Refractory period:** After an action potential, there is a brief period during which the neuron is less excitable. This is known as the refractory period, and it prevents the neuron from generating another action potential immediately.
**Propagation:** Action potentials travel along the axon of a neuron by a process called saltatory conduction. The myelin sheath, a fatty insulating layer that surrounds the axon, speeds up the conduction by limiting the leakage of ions across the membrane. The action potential jumps from one node of Ranvier, a gap in the myelin sheath, to the next.
**Importance of Action Potentials:**
Action potentials play a crucial role in various physiological functions, including:
- **Neural communication:** Transmission of signals between neurons at synapses.
- **Muscle contraction:** Activation of muscle fibers to generate force.
- **Sensory perception:** Transduction of sensory stimuli into electrical signals.
- **Hormone release:** Regulation of hormone secretion by endocrine cells.
**Factors Affecting Action Potential:**
Several factors can influence the characteristics of action potentials, including:
- **Temperature:** Higher temperatures tend to increase the speed of conduction.
- **Ion concentration:** Changes in the concentration of ions like Na+ and K+ can alter the resting potential and threshold.
- **Myelination:** Myelination increases the speed of conduction.
- **Presence of drugs or toxins:** Some substances can block ion channels or alter their function.
Action potentials are a fundamental process in the nervous system, ensuring rapid and efficient communication between neurons and the generation of physiological responses.'
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Protein | Definition | Taxonomy |
---|---|---|
Guanine nucleotide-binding protein G(q) subunit alpha | A guanine nucleotide-binding protein G(q) subunit alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P50148] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily G member 1 | A voltage-gated potassium channel KCNG1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9UIX4] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily S member 3 | A voltage-gated potassium channel KCNS3 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9BQ31] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily S member 1 | A voltage-gated potassium channel KCNS1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q96KK3] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily S member 2 | A voltage-gated potassium channel KCNS2 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9ULS6] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily C member 2 | A voltage-gated potassium channel KCNC2 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q96PR1] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily D member 1 | A voltage-gated potassium channel KCND1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9NSA2] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily A member 6 | A voltage-gated potassium channel subunit KCNA6 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P17658] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily A member 4 | A voltage-gated potassium channel alpha subunit KCNA4 that is encoded in the genome of human. [] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily V member 1 | A voltage-gated potassium channel KCNV1 that is encoded in the genome of human. [] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily V member 2 | A voltage-gated potassium channel KCNV2 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q8TDN2] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily A member 10 | A voltage-gated potassium channel subunit KCNA10 that is encoded in the genome of human. [] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily KQT member 1 | A voltage-gated potassium channel subunit KCNQ1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P51787] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily G member 4 | A voltage-gated potassium channel subfamily G member 4 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q8TDN1] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily A member 3 | A voltage-gated potassium channel subunit KCNA3 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P22001] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily D member 3 | A voltage-gated potassium channel KCND3 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9UK17] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily C member 1 | A voltage-gated potassium channel KCNC1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P48547] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily A member 5 | A voltage-gated potassium channel subunit KCNA5 that is encoded in the genome of human. [] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily G member 3 | A voltage-gated potassium channel subfamily G member 3 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q8TAE7] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily F member 1 | A voltage-gated potassium channel KCNF1 that is encoded in the genome of human. [] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily KQT member 2 | A voltage-gated potassium channel subunit KCNQ2 that is encoded in the genome of human. [] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily A member 2 | A voltage-gated potassium channel subunit KCNA2 that is encoded in the genome of human. [] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily A member 7 | A voltage-gated potassium channel subunit KCNA7 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q96RP8] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily B member 2 | A voltage-gated potassium channel KCNB2 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q92953] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily C member 3 | A voltage-gated potassium channel KCNC3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q14003] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily C member 4 | A voltage-gated potassium channel KCNC4 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q03721] | Homo sapiens (human) |
Guanine nucleotide-binding protein subunit alpha-11 | A guanine nucleotide-binding protein subunit alpha-11 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P29992] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily G member 2 | A voltage-gated potassium channel KCNG2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UJ96] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily A member 1 | A voltage-gated potassium channel subunit KCNA1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q09470] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily D member 2 | A voltage-gated potassium channel KCND2 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9NZV8] | Homo sapiens (human) |
Potassium voltage-gated channel subfamily B member 1 | A voltage-gated potassium channel KCNB1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q14721] | Homo sapiens (human) |
ATP-sensitive inward rectifier potassium channel 11 | An ATP-sensitive inward rectifier potassium channel 11 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q14654] | Homo sapiens (human) |
Neuronal acetylcholine receptor subunit alpha-4 | A neuronal acetylcholine receptor subunit alpha-4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P43681] | Homo sapiens (human) |
ATP-binding cassette sub-family C member 9 | An ATP-binding cassette sub-family C member 9 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60706] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
nornicotine | nornicotine: agricultural or horticultural insecticide; RN given refers to (+-)-isomer; structure | ||
bupropion | bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring. Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE. | aromatic ketone; monochlorobenzenes; secondary amino compound | antidepressant; environmental contaminant; xenobiotic |
3-(1-methylpyrrolidin-2-yl)pyridine | 3-(1-methylpyrrolidin-2-yl)pyridine : An N-alkylpyrrolidine that consists of N-methylpyrrolidine bearing a pyridin-3-yl substituent at position 2. | N-alkylpyrrolidine; pyridine alkaloid; pyrrolidine alkaloid | |
epibatidine | alkaloid | ||
dimethylphenylpiperazinium iodide | piperazines | ||
4-aminopyridine | aminopyridine; aromatic amine | avicide; orphan drug; potassium channel blocker | |
N-(2-aminoethyl)-5-chloro-1-naphthalenesulfonamide | naphthalenes; sulfonic acid derivative | ||
alfuzosin | alfuzosin: structure given in first source | monocarboxylic acid amide; quinazolines; tetrahydrofuranol | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
anabasine | piperidine alkaloid; pyridine alkaloid | nicotinic acetylcholine receptor agonist; plant metabolite; teratogenic agent | |
5-methoxypsoralen | 5-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 |
verapamil | 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine. Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent. | aromatic ether; nitrile; polyether; tertiary amino compound | |
carbamylcholine | |||
clotrimazole | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic | |
diazoxide | diazoxide : 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 |
flecainide | flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart). Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS. | aromatic ether; monocarboxylic acid amide; organofluorine compound; piperidines | anti-arrhythmia drug |
glyburide | glyburide : 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 |
granisetron | aromatic amide; indazoles | ||
lidocaine | lidocaine : 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 |
lamotrigine | 1,2,4-triazines; dichlorobenzene; primary arylamine | anticonvulsant; antidepressant; antimanic drug; calcium channel blocker; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; excitatory amino acid antagonist; geroprotector; non-narcotic analgesic; xenobiotic | |
mecamylamine | Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. | primary aliphatic amine | |
n-methylcarbamylcholine | N-methylcarbamylcholine: structure given in first source | ||
nifedipine | Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
ondansetron | Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. | carbazoles | |
pinacidil | Pinacidil: 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 | |
propafenone | propafenone : 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 |
tetraethylammonium | Tetraethylammonium: A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90) | quaternary ammonium ion | |
tilorone | tilorone : A member of the class of fluoren-9-ones that is 9H-fluoren-9-one which is substituted by a 2-(diethylamino)ethoxy group at positions 2 and 7. It is an interferon inducer and a selective alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) agonist. Its hydrochloride salt is used as an antiviral drug. Tilorone: An antiviral agent used as its hydrochloride. It is the first recognized synthetic, low-molecular-weight compound that is an orally active interferon inducer, and is also reported to have antineoplastic and anti-inflammatory actions. | aromatic ether; diether; fluoren-9-ones; tertiary amino compound | anti-inflammatory agent; antineoplastic agent; antiviral agent; interferon inducer; nicotinic acetylcholine receptor agonist |
troglitazone | Troglitazone: 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 |
tetramethylammonium | tetramethylammonium : The simplest quaternary ammonium cation, comprising a central nitrogen linked to four methyl groups. tetramethylammonium: RN given refers to parent cpd | quaternary ammonium ion | |
indopan | alpha-methyltryptamine : A tryptamine derivative having a methyl substituent at the alpha-position. indopan: RN given refers to parent cpd without isomeric designation | tryptamines | |
boldine | aporphine alkaloid | ||
cytisine | alkaloid; bridged compound; lactam; organic heterotricyclic compound; secondary amino compound | nicotinic acetylcholine receptor agonist; phytotoxin; plant metabolite | |
anatabine | anatabine: alkaloid found in tobacco; structure | bipyridines | |
diphenoxylate | diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin. Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. | ethyl ester; nitrile; piperidinecarboxylate ester; tertiary amine | antidiarrhoeal drug |
dihydro-beta-erythroidine | dihydro-beta-erythroidine : An organic heterotetracyclic compound resulting from the partial hydrogenation of the 1,3-diene moiety of beta-erythroidine to give the corresponding 2-ene. Dihydro-beta-Erythroidine: Dihydro analog of beta-erythroidine, which is isolated from the seeds and other plant parts of Erythrina sp. Leguminosae. It is an alkaloid with curarimimetic properties. | delta-lactone; organic heterotetracyclic compound; tertiary amino compound | nicotinic antagonist |
diltiazem | diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions. | 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate | antihypertensive agent; calcium channel blocker; vasodilator agent |
n-cyano-n'-(1,1-dimethylpropyl)-n''-(3-pyridinyl)guanidine | N-cyano-N'-(1,1-dimethylpropyl)-N''-(3-pyridinyl)guanidine: potassium channel opener | pyridines | |
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 |
flupirtine | flupirtine: RN given refers to parent cpd without isomeric designation | aminopyridine | |
sertindole | sertindole : A phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-oxoimidazolidin-1-yl)ethyl group. | heteroarylpiperidine; imidazolidinone; organochlorine compound; organofluorine compound; phenylindole | alpha-adrenergic antagonist; H1-receptor antagonist; second generation antipsychotic; serotonergic antagonist |
duloxetine | duloxetine | ||
nelfinavir | nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties. Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children. | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
khellinone | khellinone: a Kv1.3 potassium channel blocker | ||
cromakalim | Cromakalim: 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) | ||
nebivolol | 2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group. | chromanes; diol; organofluorine compound; secondary alcohol; secondary amino compound | |
uk 68798 | aromatic ether; sulfonamide; tertiary amino compound | anti-arrhythmia drug; potassium channel blocker | |
polygodial | aldehyde | ||
doripenem | Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS. | carbapenems | |
4'-methoxyflavone | 4'-methoxyflavone: from seeds of Psoralea corylifolia (Fabaceae); structure in first source | ether; flavonoids | |
rosiglitazone | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug | |
N-methyl-N-(3-pyridylmethyl)amine | aralkylamine | ||
nicotine | (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum. | 3-(1-methylpyrrolidin-2-yl)pyridine | anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic |
lobeline | (-)-lobeline : An optically active piperidine alkaloid having a 2-oxo-2-phenylethyl substituent at the 2-position and a 2-hydroxy-2-phenylethyl group at the 6-position. | aromatic ketone; piperidine alkaloid; tertiary amine | nicotinic acetylcholine receptor agonist |
tadalafil | benzodioxoles; pyrazinopyridoindole | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent | |
paliperidone | 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia. | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine; secondary alcohol | |
3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole | 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole: structure in first source | ||
293b cpd | 6-cyano-4-(N-ethylsulfonyl-N-methylamino)-3-hydroxy-2,2-dimethylchromane: RN given for (trans-(+-))-isomer | 1-benzopyran | |
ezogabine | ezogabine : 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 |
desvenlafaxine | O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine. | cyclohexanols; phenols; tertiary amino compound | antidepressant; drug metabolite; marine xenobiotic metabolite |
mk 767 | 5-((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 | ||
moxifloxacin | moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents. Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent. | aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone; quinolone antibiotic | antibacterial drug |
solifenacin | isoquinolines | ||
telbivudine | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor | |
philanthotoxin 343 | philanthotoxin 343: structure given in first source (see article's footnote); identical to philanthotoxin 433 except that the number of methylene groups between the respective amine moieties is 3,4,3 instead of 4,3,3 | N-acyl-amino acid | |
erysodine | erysodine : An erythrina alkaloid with formula C18H21NO3 isolated from several erythrina plant species. It is a competitive antagonist of nicotinic acetylcholine receptors and exhibits antiparasitic and insecticidal activities. erysodine: structure given in first source | aromatic ether; diether; Erythrina alkaloid; organic heterotetracyclic compound; phenols | antiparasitic agent; nicotinic antagonist; phytogenic insecticide |
varenicline | varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking. Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION. | ||
zeneca zd 6169 | Zeneca ZD 6169: an ATP-sensitive potassium channel opener; structure given in first source | ||
pozanicline | |||
etravirine | aminopyrimidine; aromatic ether; dinitrile; organobromine compound | antiviral agent; HIV-1 reverse transcriptase inhibitor | |
lapatinib | furans; organochlorine compound; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor | |
darunavir | darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors. Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS. | carbamate ester; furofuran; sulfonamide | antiviral drug; HIV protease inhibitor |
deferasirox | deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions. Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA. | benzoic acids; monocarboxylic acid; phenols; triazoles | iron chelator |
bms204352 | BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source | ||
senicapoc | senicapoc: a Gardos channel blocker; structure in first source | ||
lacosamide | Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES. | N-acyl-amino acid | |
cortisone | 11-oxo steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | human metabolite; mouse metabolite | |
anatoxin a | anatoxin a: found in Anabaena; was indexed to cyanobacterial toxin (MARINE TOXINS) 1978-2006; also see anatoxin-a(s) | tropane alkaloid | |
quinidine | quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission. | cinchona alkaloid | alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker |
cromakalim | 1-benzopyran | ||
tolterodine | tertiary amine | antispasmodic drug; muscarinic antagonist; muscle relaxant | |
darifenacin | darifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence. | 1-benzofurans; monocarboxylic acid amide; pyrrolidines | antispasmodic drug; muscarinic antagonist |
deformylflustrabromine | deformylflustrabromine: has antineoplastic activity; isolated from Flustra folicea; structure in first source | tryptamines | |
tropacocaine | tropacocaine: RN given refers to (exo)-isomer; structure | ||
cardamonin | cardamonin: found in Zingiberaceae; structure in first source | chalcones | |
s 1033 | (trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor | |
tropisetron | tropisetron : An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine. Tropisetron: An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting. | indolyl carboxylic acid | |
(2'-(benzyloxycarbonylaminomethyl)biphenyl-2-carboxylic acid 2-(2-pyridyl)ethylamide) | biphenyls | ||
xe 991, anthracenone | 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone: neurotransmitter release enhancer and potassium channel blocker; structure given in first source | anthracenes | |
tram 34 | TRAM 34: inhibits IKCa1; structure in first source | organochlorine compound | |
uk 78282 | diarylmethane | ||
lobeline | |||
epibatidine | |||
capsaicin | ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers. | capsaicinoid | non-narcotic analgesic; TRPV1 agonist; voltage-gated sodium channel blocker |
maraviroc | tropane alkaloid | ||
anatoxin a | anatoxin I: found mainly in ANABAENA; was indexed to cyanobacterial toxin (MARINE TOXINS). isolated from many salt-tolerant freshwater cyanobacteria | ||
clamikalant | clamikalant: inhibits ATP-sensitive potassium channel; structure in first source | ||
dasatinib | dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source | 1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
abt 594 | |||
N-(2,4,6-trimethylphenyl)-3-bicyclo[2.2.1]heptanecarboxamide | monoterpenoid | ||
n-(6-chloropyridin-3-yl)-4-fluorobenzamide | N-(6-chloropyridin-3-yl)-4-fluorobenzamide: structure in first source | ||
sitagliptin | sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | triazolopyrazine; trifluorobenzene | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic |
5-(6-chloro-3-pyridinyl)-9-azabicyclo[4.2.1]non-4-ene | azepine | ||
zm226600 | ZM226600: an ATP-sensitive potassium channel opener; structure in first source | anilide | |
acacetin | 5,7-dihydroxy-4'-methoxyflavone : A monomethoxyflavone that is the 4'-methyl ether derivative of apigenin. | dihydroxyflavone; monomethoxyflavone | anticonvulsant; plant metabolite |
trans-metanicotine | metanicotine: RN given refers to parent cpd with unspecified isomeric designation | ||
a 85380 | A 85380: structure given in first source; A-85380 is the S-enantiomer; A-159470 is the R-enantiomer | ||
ar-r 17779 | AR-R 17779: structure in first source | ||
3-(2,4-dimethoxybenzylidene)anabaseine | 3-(2,4-dimethoxybenzylidene)anabaseine: an alpha7nAChR nicotinic receptor agonist | dimethoxybenzene | |
mdl 100907 | Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes. | ||
silodosin | silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source | indolecarboxamide | |
su 11248 | monocarboxylic acid amide; pyrroles | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist | |
clathrodin | clathrodin: structure given in first source; isolated from marine sponges of the genus Agelas | ||
alvimopan anhydrous | alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain | peptide | |
oroidin | oroidin: from marine sponges of the genus Agelas; structure in first source | pyrroles; secondary carboxamide | metabolite |
palonosetron | palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting. | azabicycloalkane; delta-lactam; organic heterotricyclic compound | antiemetic; serotonergic antagonist |
mg 624 | triethyl-(beta-4-stilbenoxyethyl)ammonium: inhibits alpha7 nicotinic receptors; structure in first source | ||
hymenidin | hymenidin: serotonergic receptor antagonist from Okinawan marine sponge Hymeniacidon; structure given in first source | ||
everolimus | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor | |
5-(4-phenylbutoxy)psoralen | 5-(4-phenylbutoxy)psoralen: structure in first source psora 4 : A member of the class of psoralens that is psoralen substituted by a 4-phenylbutoxy group at position 5. It is a potent inhibitor of the voltage-gated potassium channel Kv1.3 (EC50 = 3 nM). | aromatic ether; benzenes; psoralens | geroprotector; immunosuppressive agent; potassium channel blocker |
6-cyano-4-(n-ethylsulfonyl-n-methylamino)-3-hydroxy-2,2-dimethylchromane, (trans-(+))-isomer | |||
5-ia-85380 | aromatic ether | ||
lu 208075 | ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension | diarylmethane | |
a 84543 | |||
azd 0328 | spiro(1-azabicyclo(2.2.2)octane-3,2'(3H)-furo(2,3-b)pyridine): AZD-0328 is the (2'R)-isomer and D-tartrate salt; an alpha7 neuronal nicotinic receptor agonist; structure in first source | ||
radafaxine | radafaxine: a bupropion metabolite; radafaxine is a (+)-isomer of hydroxybupropion | ||
ispronicline | ispronicline: a neuronal nicotinic acetylcholine receptor modulator; has antidepressant, neuroprotective, and cognitive effects; structure in first source | ||
a 1899 | A 1899: a TASK-1 potassium channel blocker; structure in first source | ||
way 133537 | |||
hmr 1556 | HMR 1556: an I(Ks) channel blocker; structure in first source | ||
10,10-bis((2-fluoro-4-pyridinyl)methyl)-9(10h)-anthracenone | DMP 543: neurotransmitter release enhancer; structure given in first source | anthracenes | |
ly 465608 | LY 465608: a nonthiazolidinedione agonist of both PPAR-alpha and PPAR-gamma of Ligand Pharm. and Eli Lilly | ||
ica 27243 | N-(6-Chloropyridin-3-yl)-3,4-difluorobenzamide: a KCNQ2/3 channel activator; structure in first source | ||
ym-254890 | YM-254890: structure in first source | ||
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | |||
bm 131246 | |||
desnitroimidacloprid | desnitroimidacloprid: a nicotinic receptor agonist; structure in first source | ||
dianicline | dianicline: an alpha4beta2 nicotinic receptor agonist; may be useful as an aid in quitting smoking; structure in first source | ||
n-methylepibatidine | N-methylepibatidine: structure in first source | ||
sazetidine-a | sazetidine-A: a ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them; structure in first source | ||
ns 9283 | 3-(3-(pyridine-3-yl)-1,2,4-oxadiazol-5-yl)benzonitrile: an alpha4beta2 nAChR agonist | ||
FR900359 | FR900359: G-protein inhibitor from Ardisia crenata sims that shows inhibition of platelet aggregation and decrease of blood pressure | cyclodepsipeptide | |
a 803467 | A 803467: an Nav1.8 sodium channel blocker; structure in first source | ||
[[(1S,2S,5R)-5-methyl-2-propan-2-ylcyclohexyl]-phenylphosphoryl]benzene | monoterpenoid | ||
a-582941 | A-582941: nicotinic acetylcholine receptor (alpha7 nAChR) agonist | ||
n,n-diallyl-5-methoxytryptamine | N,N-diallyl-5-methoxytryptamine: structure in first source | tryptamines | |
(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 | ||
raltegravir | 1,2,4-oxadiazole; dicarboxylic acid amide; hydroxypyrimidine; monofluorobenzenes; pyrimidone; secondary carboxamide | antiviral drug; HIV-1 integrase inhibitor | |
imidacloprid | (E)-imidacloprid : The E-isomer of imidacloprid. | imidacloprid; imidazolidines; monochloropyridine | environmental contaminant; genotoxin; neonicotinoid insectide; nicotinic acetylcholine receptor agonist; xenobiotic |
sildenafil | sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position. | piperazines; pyrazolopyrimidine; sulfonamide | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
vardenafil | vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine. | imidazotriazine; N-alkylpiperazine; N-sulfonylpiperazine | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
nn 414 | NN 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-dioxide | 7-chloro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide: activates ATP-sensitive potassium channels; structure in first source | ||
amg531 | |||
3-(4-hydroxy-2-methoxybenzylidene)anabaseine |