Target type: biologicalprocess
Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an acetylcholine stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:21238497]
Acetylcholine, a neurotransmitter, is a critical molecule in the nervous system, mediating a wide range of physiological processes. The response to acetylcholine involves a complex series of events that begin with its release from presynaptic neurons and culminate in the activation of specific cellular pathways.
1. **Release of Acetylcholine:** When a nerve impulse arrives at the synapse, a presynaptic neuron releases acetylcholine from synaptic vesicles into the synaptic cleft, the narrow gap between the presynaptic and postsynaptic neurons. This release is triggered by the influx of calcium ions into the presynaptic terminal.
2. **Binding to Receptors:** Acetylcholine diffuses across the synaptic cleft and binds to its receptors on the postsynaptic membrane. There are two main types of acetylcholine receptors:
* **Nicotinic receptors:** These are ligand-gated ion channels, meaning that acetylcholine binding directly opens the channel, allowing ions to flow across the membrane. Nicotinic receptors are found in both the central nervous system (CNS) and the peripheral nervous system (PNS), including skeletal muscle.
* **Muscarinic receptors:** These are G protein-coupled receptors (GPCRs). Binding of acetylcholine to muscarinic receptors triggers a cascade of intracellular signaling events that ultimately alter cellular function. Muscarinic receptors are found in the CNS and PNS, mediating effects on smooth muscle, cardiac muscle, and glands.
3. **Signal Transduction:** Binding of acetylcholine to its receptors initiates a signaling cascade. In the case of nicotinic receptors, the opening of ion channels leads to a rapid depolarization of the postsynaptic membrane, triggering an action potential. For muscarinic receptors, activation of GPCRs leads to the production of intracellular signaling molecules, such as cyclic AMP (cAMP) or inositol triphosphate (IP3), which regulate various cellular processes.
4. **Cellular Response:** The specific cellular response to acetylcholine depends on the type of receptor involved and the target cell. Examples include:
* **Muscle contraction:** Acetylcholine binding to nicotinic receptors at the neuromuscular junction triggers muscle fiber contraction.
* **Neurotransmitter release:** Acetylcholine plays a role in the release of other neurotransmitters in the CNS, such as dopamine and serotonin.
* **Cardiac function:** Acetylcholine binding to muscarinic receptors in the heart slows down heart rate and reduces the force of contraction.
* **Smooth muscle contraction and relaxation:** Acetylcholine can cause both contraction and relaxation of smooth muscle, depending on the specific type of muscarinic receptor involved and the location.
* **Glandular secretion:** Acetylcholine stimulates the secretion of various glands, such as salivary glands and sweat glands.
5. **Acetylcholine Degradation:** To terminate the signal, acetylcholine is rapidly broken down by the enzyme acetylcholinesterase (AChE). AChE hydrolyzes acetylcholine into choline and acetate, both of which are taken back up by the presynaptic neuron for recycling.
The intricate interplay of acetylcholine release, receptor binding, signal transduction, and degradation ensures that this neurotransmitter effectively mediates a diverse range of physiological processes. Disruptions in acetylcholine signaling can lead to various neurological and muscular disorders.
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Protein | Definition | Taxonomy |
---|---|---|
Neuronal acetylcholine receptor subunit alpha-7 | A neuronal acetylcholine receptor subunit alpha-7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P36544] | Homo sapiens (human) |
Neuronal acetylcholine receptor subunit alpha-3 | A neuronal acetylcholine receptor subunit alpha-3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P32297] | Homo sapiens (human) |
Translocator protein | [no definition available] | Homo sapiens (human) |
Endothelin-1 receptor | An endothelin-1 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P25101] | Homo sapiens (human) |
Neuronal acetylcholine receptor subunit beta-2 | A neuronal acetylcholine receptor subunit beta-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P17787] | 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 | ||
1,3-dipropyl-8-(4-sulfophenyl)xanthine | 1,3-dipropyl-8-(4-sulfophenyl)xanthine: adenosine receptor antagonist | ||
pk 11195 | PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine | aromatic amide; isoquinolines; monocarboxylic acid amide; monochlorobenzenes | antineoplastic agent |
ro 5-4864 | 4'-chlorodiazepam: selectively binds peripheral benzodiazepine receptor | ||
amiodarone | amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias. Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance. | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
anabasine | piperidine alkaloid; pyridine alkaloid | nicotinic acetylcholine receptor agonist; plant metabolite; teratogenic agent | |
carbamylcholine | |||
clonazepam | clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation. Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses. | 1,4-benzodiazepinone; monochlorobenzenes | anticonvulsant; anxiolytic drug; GABA modulator |
decamethonium | decamethonium : A quaternary ammonium ion that is a depolarising muscle relaxant whose structure comprises a decane-1,10-diamine core in which each amino group carries three methyl substituents. decamethonium: RN given refers to parent cpd | quaternary ammonium ion | muscle relaxant; nicotinic acetylcholine receptor agonist |
nordazepam | nordazepam : A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety. Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam. | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; GABA modulator; human metabolite; sedative |
diazepam | diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
flunitrazepam | flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia. Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug. | 1,4-benzodiazepinone; C-nitro compound; monofluorobenzenes | anxiolytic drug; GABAA receptor agonist; sedative |
granisetron | aromatic amide; indazoles | ||
avapro | irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease. | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
isoflurane | Isoflurane: A stable, non-explosive inhalation anesthetic, relatively free from significant side effects. | organofluorine compound | inhalation anaesthetic |
kynurenic acid | kynurenic acid : A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4. Kynurenic Acid: A broad-spectrum excitatory amino acid antagonist used as a research tool. | monohydroxyquinoline; quinolinemonocarboxylic acid | G-protein-coupled receptor agonist; human metabolite; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist; Saccharomyces cerevisiae metabolite |
lorazepam | Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. | benzodiazepine | |
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 | ||
mianserin | mianserin : A dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere. Mianserin: A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. | dibenzoazepine | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; geroprotector; H1-receptor antagonist; histamine agonist; sedative; serotonergic antagonist |
nitrazepam | nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome). Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic. | 1,4-benzodiazepinone; C-nitro compound | anticonvulsant; antispasmodic drug; drug metabolite; GABA modulator; sedative |
cm 7116 | norflutoprazepam: structure | benzodiazepine | |
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 | |
oxazepam | oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5. Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia. | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
propranolol | propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs. | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
sb 206553 | SB 206553: a high-affinity 5-HT(2C/2B) antagonist; structure given in first source | pyrroloindole | |
sulfathiazole | sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position. Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine. | 1,3-thiazoles; substituted aniline; sulfonamide; sulfonamide antibiotic | antiinfective agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
sulfisoxazole | sulfisoxazole : A sulfonamide antibacterial with an oxazole substituent. It has antibiotic activity against a wide range of gram-negative and gram-positive organisms. Sulfisoxazole: A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms. | isoxazoles; sulfonamide; sulfonamide antibiotic | antibacterial drug; drug allergen |
temazepam | Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | benzodiazepine | |
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 |
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 | |
laudanosine | laudanosine: opium alkaloid | isoquinolines | |
5-hydroxyindole | hydroxyindoles | human metabolite | |
chlordesmethyldiazepam | benzodiazepine | ||
anabaseine | anabaseine: structure given in first source | bipyridines | |
halazepam | halazepam: structure | organic molecular entity | |
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 |
alpidem | imidazoles | ||
polygodial | aldehyde | ||
n-desmethylflunitrazepam | |||
7-aminonitrazepam | 7-aminonitrazepam: urinary metabolite of nitrazepam | benzodiazepine | |
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 |
ro 20-1815 | 7-aminoflunitrazepam: flunitrazepam metabolite; structure given in first source | benzodiazepine | |
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 |
bosentan anhydrous | Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
1h-indene-2-carboxylic acid, 1-(1,3-benzodioxol-5-yl)-3-(2- (carboxymethoxy)-4-methoxyphenyl)-2,3-dihydro-5-propoxy-, (1s,2r,3s)- | 1H-Indene-2-carboxylic acid, 1-(1,3-benzodioxol-5-yl)-3-(2- (carboxymethoxy)-4-methoxyphenyl)-2,3-dihydro-5-propoxy-, (1S,2R,3S)-: an ET(A) and ET(B) endothelin receptor antagonist; structure in first source | ||
thiacloprid | (Z)-thiacloprid : The (Z)-stereoisomer of thiacloprid. thiacloprid : A nitrile that is cyanamide in which the hydrogens are replaced by a 1,3-thiazolidin-2-ylidene group which in turn is substituted by a (6-chloropyridin-3-yl)methyl group at the ring nitrogen. thiacloprid: structure in first source | monochloropyridine; nitrile; thiazolidines | environmental contaminant; neonicotinoid insectide; xenobiotic |
3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole | 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole: structure in first source | ||
ro 46-2005 | Ro 46-2005: an orally active non-peptide antagonist of endothelin receptors; structure given in first source | ||
dx 9065 | |||
pd 142893 | PD 142893: functional antagonist of endothelin-stimulated vasoconstriction | ||
5-(dimethylamino)-n-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide | 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide: structure in first source; endothelin receptor antagonist | naphthalenes; sulfonic acid derivative | |
tak 044 | TAK 044: endothelin receptor antagonist | ||
ro 11-6893 | Ro 11-6893: RN given refers to (R)-isomer | ||
endothelin (16-21) | endothelin (16-21): C-terminal hexapeptide of endothelin; amino acid seq. given in first source | peptide | |
n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide | N,N-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide: binds with high affinity to glial mitochondrial diazepam binding inhibitor receptors & increases mitochondrial steroidogenesis | phenylindole | |
tezosentan | tezosentan: structure in first source | ||
bms 207940 | N-((2'-(((4,5-dimethyl-3-isoxazolyl)amino)sulfonyl)-4-(2-oxazolyl)(1,1'-biphenyl)-2-yl)methyl)-N,3,3-trimethylbutanamide: an ET(A) receptor antagonist; structure in first source | ||
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 | |
atrasentan | Atrasentan: A pyrrolidine and benzodioxole derivative that acts a RECEPTOR, ENDOTHELIN A antagonist. It has therapeutic potential as an antineoplastic agent and for the treatment of DIABETIC NEPHROPATHIES. | pyrrolidines | |
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. | ||
lu 135252 | |||
pozanicline | |||
enrasentan | enrasentan : A member of the class of indanes that is 2,3-dihydro-1H-indene which is substituted by a 1,3-benzodioxol-5-yl group, carboxy group, 2-(2-hydroxyethoxy)-4-methoxyphenyl group and a propoxy group at positions 1S, 2R, 3S and 5, respectively. It is an orally active mixed endothelin A/B receptor antagonist with a 100-fold greater affinity for the endothelin A receptor. The drug was being developed by GSK for the treatment of congestive heart failure and pulmonary hypertension (clinical trials discontinued). enrasentan: decreases ischemic brain injury; an endothelin A and B receptor antagonist; structure in first source | aromatic ether; benzodioxoles; indanes; monocarboxylic acid; monomethoxybenzene; primary alcohol | antihypertensive agent; endothelin receptor antagonist |
7-aminoclonazepam | benzodiazepine | ||
ro 5-3438 | Ro 5-3438: structure | ||
2-[(4,6-dimethyl-2-pyrimidinyl)oxy]-3-methoxy-3,3-diphenylpropanoic acid | diarylmethane | ||
tbc-11251 | sitaxsentan: endothelin A receptor antagonist; structure in first source | benzodioxoles | |
pnu 120596 | 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea: an alpha7nAChR agonist; structure in first source | ureas | |
harmicine | harmicine: structure in first source | ||
anatoxin a | anatoxin a: found in Anabaena; was indexed to cyanobacterial toxin (MARINE TOXINS) 1978-2006; also see anatoxin-a(s) | tropane alkaloid | |
bisabolol | Kamillosan: drug combination containing chamomile and bisabolol; used to treat dermatitis | sesquiterpenoid | |
bq 123 | cyclo(Trp-Asp-Pro-Val-Leu): derived from the modification of a natural lead of BE-18257B, an endothelin A receptor antagonist; has neuroprotective activity; amino acid sequence given in first source | cyclic peptide | |
n-desmethylflunitrazepam | N-desmethylflunitrazepam: metabolite of flunitrazepam | ||
ro 05-4082 | ID 690: methyl deriv of clonazepam; structure | ||
deformylflustrabromine | deformylflustrabromine: has antineoplastic activity; isolated from Flustra folicea; structure in first source | tryptamines | |
tropacocaine | tropacocaine: RN given refers to (exo)-isomer; structure | ||
isoliquiritigenin | chalcones | antineoplastic agent; biological pigment; EC 1.14.18.1 (tyrosinase) inhibitor; GABA modulator; geroprotector; metabolite; NMDA receptor antagonist | |
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 | |
lobeline | |||
epibatidine | |||
hmr 3647 | |||
anatoxin a | anatoxin I: found mainly in ANABAENA; was indexed to cyanobacterial toxin (MARINE TOXINS). isolated from many salt-tolerant freshwater cyanobacteria | ||
abt 594 | |||
5-(6-chloro-3-pyridinyl)-9-azabicyclo[4.2.1]non-4-ene | azepine | ||
naringenin chalcone | 2',4,4',6'-tetrahydroxychalcone : A member of the class of chalcones that is trans-chalcone substituted by hydroxy groups at positions 2' ,4, 4', and 6' respectively. naringenin chalcone: RN given refers to cpd with unspecified stereoisomer & from CA Vol 92 Form Index; RN for cpd not in Chemline 7/6/83; structure in first source | chalcones; polyphenol | anti-allergic agent; anti-inflammatory agent; 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 | |
a 192621 | A 192621: ET(B) receptor antagonist | ||
irl 2500 | IRL 2500: Endothelin-B receptor antagonist; structure in first source | ||
ro 46-8443 | Ro 46-8443: a non-peptide endothelin ET(B) receptor selective antagonist; structure given in first source | ||
sulindac sulfone | sulindac sulfone : A sulfone metabolite of sulindac that inhibits cell growth by inducing apoptosis independently of cyclooxygenase inhibition. It inhibits the development and induces regression of premalignant adenomatous polyps. Lipoxygenase and Cox-2 inhibitor. sulindac sulfone: inhibits K-ras-dependent cyclooxygenase-2; sulfated analog of indomethacin;; CP248 is an antineoplastic agent that fosters microtubule depolymerization; structure in first source | monocarboxylic acid; organofluorine compound; sulfone | apoptosis inducer; cyclooxygenase 2 inhibitor; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor |
2,4,2'-trihydroxychalcone | 2,4,2'-trihydroxychalcone: structure in first source | ||
ro 47-8634 | Ro 47-8634: structure in first source | ||
clazosentan | clazosentan: endothelin A receptor antagonist used for cerebral vasospasm; structure in first source; | ||
lu 224332 | felotaxel: an antineoplastic agent; structure in first source | ||
ac-5216 | |||
mg 624 | triethyl-(beta-4-stilbenoxyethyl)ammonium: inhibits alpha7 nicotinic receptors; structure in first source | ||
cb 34 | CB 34: ligand for peripheral benzodiazepine receptors; structure in first source | ||
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 | ||
pnu-282987 | carbonyl compound; organohalogen compound | ||
ssr180711 | SSR180711: a selective alpha7 acetylcholine nicotinic receptor (n-AChRs) partial agonist; structure in first source | ||
ispronicline | ispronicline: a neuronal nicotinic acetylcholine receptor modulator; has antidepressant, neuroprotective, and cognitive effects; structure in first source | ||
n-(2-methoxybenzyl)-n-(4-phenoxypyridin-3-yl)acetamide | N-(2-methoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide: for imaging brain peripheral benzodiazepine receptors; structure in first source | ||
bms 193884 | |||
ci 1020 | |||
lu 302872 | LU 224332: endothelin-A/B receptor antagonist | ||
bms 248360 | |||
zibotentan | ZD4054: a potent endothelin receptor A antagonist that inhibits ovarian carcinoma cell proliferation | phenylpyridine | |
avosentan | Avosentan: structure in first source | ||
ssr180575 | SSR180575: structure in first source | ||
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | |||
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 | ||
crispine a | crispine A: pyrrolo(2,1-a)isoquinoline alkaloid from Carduus crispus; structure in first source | ||
daa 1106 | |||
pnu-282987 | |||
amd 070 | mavorixafor: a derivative of AMD3100; a CXCR4 blocker | aminoquinoline | |
naluzotan | naluzotan: an antidepressant and anti-anxiety agent; structure in first source | ||
dpa-713 | |||
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 | ||
3-bromocytisine | 3-bromocytisine: structure in first source | ||
macitentan | aromatic ether; organobromine compound; pyrimidines; ring assembly; sulfamides | antihypertensive agent; endothelin receptor antagonist; orphan drug | |
a 803467 | A 803467: an Nav1.8 sodium channel blocker; structure in first source | ||
endothelin-1 | Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63) | ||
a 867744 | 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide: positive modulator of alpha7 nicotinic acetylcholine receptor; structure in first source | ||
pd 156707 | |||
act-132577 | ACT-132577 : A member of the class of sulfamides in which one of the amino groups of sulfonamide is substituted by a 5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl group. An active metabolite of macitentan (obtained by oxidative depropylation), an orphan drug used for the treatment of pulmonary arterial hypertension. aprocitentan: a macitentan metabolite | aromatic ether; organobromine compound; pyrimidines; sulfamides | antihypertensive agent; drug metabolite; endothelin receptor antagonist; xenobiotic metabolite |
n-fluoroacetyl-n-(2,5-dimethoxybenzyl)-2-phenoxyaniline | N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline: a peripheral benzodiazepine receptor PET ligand; structure in first source | ||
a-582941 | A-582941: nicotinic acetylcholine receptor (alpha7 nAChR) agonist | ||
endothelins | |||
nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source | ||
evp-6124 | |||
n,n-diallyl-5-methoxytryptamine | N,N-diallyl-5-methoxytryptamine: structure in first source | tryptamines | |
MS-417 | MS-417 : A member of the class of thienotriazolodiazepines that is the methyl ester of [(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetic acid. A bromodomain and extra-terminal domain (BET)-specific inhibitor that belongs to a group of thienodiazepine-based compounds | methyl ester; monochlorobenzenes; thienotriazolodiazepine | |
imidacloprid | (E)-imidacloprid : The E-isomer of imidacloprid. | imidacloprid; imidazolidines; monochloropyridine | environmental contaminant; genotoxin; neonicotinoid insectide; nicotinic acetylcholine receptor agonist; xenobiotic |
3-(4-hydroxy-2-methoxybenzylidene)anabaseine |