Page last updated: 2024-10-24

excitatory extracellular ligand-gated monoatomic ion channel activity

Definition

Target type: molecularfunction

Enables the transmembrane transfer of an ion by a channel that opens when a specific extracellular ligand has been bound by the channel complex or one of its constituent parts, where channel opening contributes to an increase in membrane potential. [GOC:mah, ISBN:0323037070]

Excitatory extracellular ligand-gated monoatomic ion channel activity involves the opening of ion channels in response to the binding of specific extracellular ligands, resulting in an influx of ions into the cell. These channels are typically permeable to cations such as sodium, potassium, or calcium, and their activation can lead to depolarization of the cell membrane. This depolarization, in turn, can trigger a variety of cellular processes, including the initiation of action potentials in neurons, the release of neurotransmitters, and the activation of muscle contraction. The molecular mechanisms underlying this activity are complex and involve a number of key steps. First, the extracellular ligand binds to its specific receptor site on the channel protein. This binding event triggers a conformational change in the channel protein, which ultimately leads to the opening of the pore. The opening of the pore allows ions to flow through the channel, down their electrochemical gradient. The duration of the channel opening is regulated by a number of factors, including the concentration of the ligand, the presence of other modulators, and the intrinsic properties of the channel itself. The specific ions that are permeable through the channel, as well as the kinetics of channel opening and closing, are determined by the amino acid sequence and structure of the channel protein. Excitatory extracellular ligand-gated monoatomic ion channel activity is essential for a wide range of physiological processes, including neuronal signaling, muscle contraction, and sensory transduction. Mutations or dysregulation of these channels can lead to a variety of diseases, including epilepsy, myasthenia gravis, and various neurological disorders.'
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Proteins (9)

ProteinDefinitionTaxonomy
Glycine receptor subunit alpha-2A glycine receptor subunit alpha-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P23416]Homo sapiens (human)
5-hydroxytryptamine receptor 3BA 5-hydroxytryptamine receptor 3B that is encoded in the genome of human. [PRO:DNx, UniProtKB:O95264]Homo sapiens (human)
Glycine receptor subunit alpha-1A glycine receptor subunit alpha-1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P23415]Homo sapiens (human)
5-hydroxytryptamine receptor 3EA 5-hydroxytryptamine receptor 3E that is encoded in the genome of human. [PRO:DNx, UniProtKB:A5X5Y0]Homo sapiens (human)
5-hydroxytryptamine receptor 3AA 5-hydroxytryptamine receptor 3A that is encoded in the genome of human. [PRO:DNx, UniProtKB:P46098]Homo sapiens (human)
5-hydroxytryptamine receptor 3CA 5-hydroxytryptamine receptor 3C that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8WXA8]Homo sapiens (human)
Glycine receptor subunit betaA glycine receptor subunit beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48167]Homo sapiens (human)
5-hydroxytryptamine receptor 3DA 5-hydroxytryptamine receptor 3D that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q70Z44]Homo sapiens (human)
Transient receptor potential cation channel subfamily V member 1A transient receptor potential cation channel TRPV1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q8NER1]Homo sapiens (human)

Compounds (186)

CompoundDefinitionClassesRoles
glycinealpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid
EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
1-(1-naphthyl)piperazine1-(1-naphthyl)piperazine: serotonin agonist; structure given in first sourceN-arylpiperazine
1-(2-methoxyphenyl)piperazine1-(2-methoxyphenyl)piperazine: RN given refers to parent cpdpiperazines
1-(3-chlorophenyl)biguanide1-(3-chlorophenyl)biguanide: RN given refers to parent cp; a 5-HT3 receptor agonistbiguanides;
monochlorobenzenes
1-(3-chlorophenyl)piperazine1-(3-chlorophenyl)piperazine : A N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone.

1-(3-chlorophenyl)piperazine: supposed metabolite of TRAZODONE; RN given refers to parent cpd; structure
monochlorobenzenes;
N-arylpiperazine
drug metabolite;
environmental contaminant;
serotonergic agonist;
xenobiotic
2-methyl-5-ht2-methyl-5-HT: M-receptor agonisttryptaminesserotonergic agonist
2-aminoethoxydiphenyl borate2-aminoethoxydiphenyl borate: is a novel membrane-penetrable modulator and transient receptor potential channel blocker; structure in first source; do not confuse with 2-APB cpd

2-aminoethoxydiphenylborane : An organoboron compound that is diphenylborane in which the borane hydrogen is replaced by a 2-aminoethoxy group.
organoboron compound;
primary amino compound
calcium channel blocker;
IP3 receptor antagonist;
potassium channel opener
methylbufotenin5-methoxy-N,N-dimethyltryptamine : A tryptamine alkaloid that is N,N-dimethyltryptamine substituted by a methoxy group at position 5.aromatic ether;
tertiary amino compound;
tryptamine alkaloid
hallucinogen;
plant metabolite
alosetronalosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.imidazoles;
pyridoindole
antiemetic;
gastrointestinal drug;
serotonergic antagonist
astemizoleastemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.

Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.
benzimidazoles;
piperidines
anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
benzyl isothiocyanatebenzyl isothiocyanate: inhibits carcinogen-induced neoplasia; structure in Negwer, 5th ed, #715; also promotes urinary bladder carcinomabenzenes;
isothiocyanate
antibacterial drug
buspironebuspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.

Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.
azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines
anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
cannabinolCannabinol: A physiologically inactive constituent of Cannabis sativa L.dibenzopyran
cgs 120664-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline : A pyrroloquinoxaline that is pyrrolo[1,2-a]quinoxaline bearing additional 4-methylpiperazin-1-yl and trifluoromethyl substituents at positions 4 and 7 respectively. A 5-hydroxytryptamine receptor 1B (5-HT1B) full agonist, 10-fold selective over 5-HT1A and 1000-fold selective over 5-HT2C receptors. Centrally active following systemic administration.N-arylpiperazine;
organofluorine compound;
pyrroloquinoxaline
serotonergic agonist
eucalyptol
cisapridecisapride : The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oesophageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere.

Cisapride: A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed)
benzamides
n(6),n(6)-dimethyladenineN(6),N(6)-dimethyladenine : A tertiary amine that is adenine substituted at N-6 by geminal methyl groups.tertiary amine
fluspirileneFluspirilene: A long-acting injectable antipsychotic agent used for chronic schizophrenia.diarylmethane
granisetronaromatic amide;
indazoles
mefloquine hydrochloride[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4.organofluorine compound;
piperidines;
quinolines;
secondary alcohol
metoclopramidemetoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.

Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.
benzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound
antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic
mianserinmianserin : 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.
dibenzoazepineadrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
H1-receptor antagonist;
histamine agonist;
sedative;
serotonergic antagonist
mirtazapineMirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders.benzazepine;
tetracyclic antidepressant
alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
oneirogen;
serotonergic antagonist
1-(3-trifluoromethylphenyl)piperazine1-(3-(trifluoromethyl)phenyl)piperazine : A N-arylpiperazine that is piperazine substituted by a 3-(trifluoromethyl)phenyl group at position 1. A serotonergic agonist used as a recreational drug.

1-(3-trifluoromethylphenyl)piperazine: acts as serotonin agonist; structure
(trifluoromethyl)benzenes;
N-arylpiperazine
environmental contaminant;
psychotropic drug;
serotonergic agonist;
xenobiotic
octopamineoctopamine : A member of the class of phenylethanolamines that is phenol which is substituted at the para- position by a 2-amino-1-hydroxyethyl group. A biogenic phenylethanolamine which has been found to act as a neurotransmitter, neurohormone or neuromodulator in invertebrates.

Octopamine: An alpha-adrenergic sympathomimetic amine, biosynthesized from tyramine in the CNS and platelets and also in invertebrate nervous systems. It is used to treat hypotension and as a cardiotonic. The natural D(-) form is more potent than the L(+) form in producing cardiovascular adrenergic responses. It is also a neurotransmitter in some invertebrates.
phenylethanolamines;
tyramines
neurotransmitter
ondansetronOndansetron: 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
palmidrolpalmidrol: a cannabinoid receptor-inactive eCB-related molecule used as prophylactic in helping to prevent respiratory viral infection

palmitoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of palmitic (hexadecanoic) acid.
endocannabinoid;
N-(long-chain-acyl)ethanolamine;
N-(saturated fatty acyl)ethanolamine
anti-inflammatory drug;
anticonvulsant;
antihypertensive agent;
neuroprotective agent
phenyl biguanidephenyl biguanide : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a phenyl group.

phenyl biguanide: RN given refers to parent cpd
guanidinescentral nervous system drug
quipazineQuipazine: A pharmacologic congener of serotonin that contracts smooth muscle and has actions similar to those of tricyclic antidepressants. It has been proposed as an oxytocic.piperazines;
pyridines
6-nitroquipazine6-nitroquipazine: structure given in first sourcenitro compound;
quinolines
n-methylquipazineN-methylquipazine : An aminoquinoline that consists of quinoline in which the hydrogen at position 2 is substituted by a 4-methylpiperazin-1-yl group. A 5-HT3 agonist. Has almost the same affinity for 5-HT3 sites as quipazine but unlike the latter, does not bind to 5-HT1B sites.

N-methylquipazine: structure in first source
aminoquinoline;
N-alkylpiperazine;
N-arylpiperazine
serotonergic agonist
risperidonerisperidone : A member of the class of pyridopyrimidines that is 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.

Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.
1,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine
alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
rizatriptanrizatriptan: structure given in first source; RN given refers to benzoatetryptaminesanti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
sdz 205-557methoxybenzoic acid
sumatriptansumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.

Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
sulfonamide;
tryptamines
serotonergic agonist;
vasoconstrictor agent
tyraminemonoamine molecular messenger;
primary amino compound;
tyramines
EC 3.1.1.8 (cholinesterase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter
6-methylthiopurine6-methylthiopurine : A thiopurine that is 9H-purine substituted by a methylsulfanyl group at position 6.thiopurine
allyl isothiocyanateallyl isothiocyanate : An isothiocyanate with the formula CH2=CHCH2N=C=S. A colorless oil with boiling point 152degreeC, it is responsible for the pungent taste of mustard, horseradish, and wasabi.

allyl isothiocyanate: used in the manufacture of flavors, war gases; medical use as a counterirritant; structure
alkenyl isothiocyanate;
isothiocyanate
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
lachrymator;
metabolite
linaloollinalool : A monoterpenoid that is octa-1,6-diene substituted by methyl groups at positions 3 and 7 and a hydroxy group at position 3. It has been isolated from plants like Ocimum canum.

linalool: RN given refers to parent cpd without isomeric designation; structure
monoterpenoid;
tertiary alcohol
antimicrobial agent;
fragrance;
plant metabolite;
volatile oil component
phenylpiperazinephenylpiperazine: RN given refers to parent cpd
citronellolcitronellol : A monoterpenoid that is oct-6-ene substituted by a hydroxy group at position 1 and methyl groups at positions 3 and 7.

citronellol: alcohol form of citronellal; found in rose oil; RN given refers to parent cpd without isomeric designation; structure

insect repellent : An insecticide that acts as a repellent to insects.
monoterpenoidplant metabolite
citronellyl acetatecitronellol acetate : A monoterpenoid that is the acetate ester of citronellol. It has been isolated from Citrus hystrix.

citronellyl acetate: RN given refers to cpd without isomeric designation
acetate ester;
monoterpenoid
plant metabolite
indopanalpha-methyltryptamine : A tryptamine derivative having a methyl substituent at the alpha-position.

indopan: RN given refers to parent cpd without isomeric designation
tryptamines
amanozinediamino-1,3,5-triazine
dronabinolDelta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.

Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.
benzochromene;
diterpenoid;
phytocannabinoid;
polyketide
cannabinoid receptor agonist;
epitope;
hallucinogen;
metabolite;
non-narcotic analgesic
phenylguanidinephenylguanidine: RN given refers to parent cpd
pimozidepimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.

Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)
benzimidazoles;
heteroarylpiperidine;
organofluorine compound
antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
phenethyl isothiocyanatephenethyl isothiocyanate : An isothiocyanate having a phenethyl group attached to the nitrogen. It is a naturally occurring compound found in some cruciferous vegetables (e.g. watercress) and is known to possess anticancer properties.

phenethyl isothiocyanate: a dietary liver aldehyde dehydrogenase inhibitor; promotes urinary bladder carcinoma
isothiocyanateantineoplastic agent;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
metabolite
4-chlorophenylbiguanide
metergolinemetergoline : An ergoline alkaloid that is the N-benzyloxycarbonyl derivative of lysergamine. A 5-HT2 antagonist. Also 5-HT1 antagonist and 5-HT1D ligand. Has moderate affinity for 5-HT6 and high affinity for 5-HT7.

Metergoline: A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.
carbamate ester;
ergoline alkaloid
dopamine agonist;
geroprotector;
serotonergic antagonist
cannabichromene1-benzopyran
adapaleneadapalene : A naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether.

Adapalene: A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.
adamantanes;
monocarboxylic acid;
naphthoic acid
dermatologic drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
non-steroidal anti-inflammatory drug
aripiprazolearipiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.

Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.
aromatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone
drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist
ziprasidoneziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.

ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone
1,2-benzisothiazole;
indolones;
organochlorine compound;
piperazines
antipsychotic agent;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
psychotropic drug;
serotonergic antagonist
allicinbotanical anti-fungal agent;
sulfoxide
antibacterial agent
lerisetron
telmisartantelmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.

Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.
benzimidazoles;
biphenyls;
carboxybiphenyl
angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
4-phenylpiperidine
voacaminealkaloid ester;
methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
tertiary amino compound
angiogenesis inhibitor;
antineoplastic agent;
plant metabolite
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)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
(6ar-trans)-isomer of tetrahydrocannabivarin 9
1-(4-chlorophenyl)piperazine1-(4-chlorophenyl)piperazine: increases serotonin & decreases 5-hydroxyindoleacetic acid concentration in rat brain 6 hours after administration; RN given refers to parent cpd
cp-55,940
gr 127935GR 127935 : A member of the class of benzamides obtained by formal condensation of the carboxy group of 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxylic acid and the anilino group of 4-methoxy-3-(4-methylpiperazin-1-yl)aniline. Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.

GR 127935: a 5-HT 1D receptor antagonist
1,2,4-oxadiazole;
benzamides;
N-alkylpiperazine;
N-arylpiperazine
ramosetronindoles
zacopridebenzamides
gr 113808GR 113808 : An indolyl carboxylate ester obtained by formal condensation between the carboxy group of 1-methylindole-3-carboxylic acid with the hydroxy group of N-{2-[4-(hydroxymethyl)piperidin-1-yl]ethyl}methanesulfonamide.

GR 113808: structure given in first source; a 5-HT(4) receptor antagonist: GR 125487 is the HCl salt
indolyl carboxylate ester;
piperidines;
sulfonamide
serotonergic antagonist
pramipexolepramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively.

Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.
benzothiazoles;
diamine
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
radical scavenger
sb 204070a
sr 57227adialkylarylamine;
tertiary amino compound
sc 53116SC 53116: serotonin agonist; pyrrolizidine cpd but not alkaloid; structure given in first source
1,1'-biphenyl-4-yl-boronic acid
pumosetragPumosetrag: a 5-HT3 receptor agonist MKC-733 on upper gastrointestinal motility in human
cinacalcetcinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group.(trifluoromethyl)benzenes;
naphthalenes;
secondary amino compound
calcimimetic;
P450 inhibitor
harmalanharmalan: structure given in first sourceharmala alkaloid
4-hydroxybenzyl isothiocyanate4-hydroxybenzyl isothiocyanate: found in white mustard; structure in first sourcephenols
piboserodSerotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
nantenine, (+-)-isomer
rs 23597-190methoxybenzoic acid
ngd 94-1NGD 94-1: D(4) receptor antagonist; structure in first source
1-(4-methoxyphenyl)piperazine1-(4-methoxyphenyl)piperazine: a designer drug; structure in first source
1-methyl-6-methoxy-dihydro-beta-carboline
strychninestrychnine : A monoterpenoid indole alkaloid that is strychnidine bearing a keto substituent at the 10-position.

Strychnine: An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.
monoterpenoid indole alkaloid;
organic heteroheptacyclic compound
avicide;
cholinergic antagonist;
glycine receptor antagonist;
neurotransmitter agent;
rodenticide
Tetrahydropiperinebenzodioxoles
geraniol3,7-dimethylocta-2,6-dien-1-ol;
monoterpenoid;
primary alcohol
allergen;
fragrance;
plant metabolite;
volatile oil component
tropacocainetropacocaine: RN given refers to (exo)-isomer; structure
piperinepiperine : A N-acylpiperidine that is piperidine substituted by a (1E,3E)-1-(1,3-benzodioxol-5-yl)-5-oxopenta-1,3-dien-5-yl group at the nitrogen atom. It is an alkaloid isolated from the plant Piper nigrum.benzodioxoles;
N-acylpiperidine;
piperidine alkaloid;
tertiary carboxamide
food component;
human blood serum metabolite;
NF-kappaB inhibitor;
plant metabolite
ilepcimideilepcimide: structure given in first source; RN given refers to compound with no isomeric designationbenzodioxoles
nerolnerol : The (2Z)-stereoisomer of 3,7-dimethylocta-2,6-dien-1-ol. It has been isolated from the essential oils from plants like lemon grass.3,7-dimethylocta-2,6-dien-1-olfragrance;
plant metabolite;
volatile oil component
cannabidiolcannabidiol : An cannabinoid that is cyclohexene which is substituted by a methyl group at position 1, a 2,6-dihydroxy-4-pentylphenyl group at position 3, and a prop-1-en-2-yl group at position 4.

Cannabidiol: Compound isolated from Cannabis sativa extract.
olefinic compound;
phytocannabinoid;
resorcinols
antimicrobial agent;
plant metabolite
tropisetrontropisetron : 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
sb 366791N-(3-methoxyphenyl)-4-chlorocinnamanilide: a TRPV1 antagonist; structure in first source
bemesetron
(e)-3-(4-t-butylphenyl)-n-(2,3-dihydrobenzo(b)(1,4)dioxin-6-yl)acrylamide3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo(b)(1,4)dioxin-6-yl)acrylamide: a vanilloid receptor 1 antagonist and antihyperalgesic agent; structure in first source
4-(benzylsulfanyl)thieno[2,3-d]pyrimidine4-(benzylsulfanyl)thieno[2,3-d]pyrimidine : A thienopyrimidine that is thieno[2,3-d]pyrimidine which is substituted at position 4 by a benzylsulfanediyl group.aryl sulfide;
benzenes;
thienopyrimidine
hc 0300312-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropylphenyl)acetamide: a TRPA1 channel blocker
sulindacsulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.

Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.
monocarboxylic acid;
organofluorine compound;
sulfoxide
analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent
zucapsaicinmethoxybenzenes;
phenols
capsaicinALGRX-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.
capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
geranyl acetategeranyl acetate : A monoterpenoid that is the acetate ester derivative of geraniol.

geranyl acetate: constituted about 90% of the palmarosa oil
acetate ester;
monoterpenoid
plant metabolite
capsazepinecapsazepine : A benzazepine that is 2,3,4,5-tetrahydro-1H-2-benzazepine which is substituted by hydroxy groups at positions 7 and 8 and on the nitrogen atom by a 2-(p-chlorophenyl)ethylaminothiocarbonyl group. A synthetic analogue of capsaicin, it was the first reported capsaicin receptor antagonist.

capsazepine: modified capsaicin molecule; a capsaicin receptor antagonist
benzazepine;
catechols;
monochlorobenzenes;
thioureas
capsaicin receptor antagonist
2-(4-chlorophenyl)guanidineorganochlorine compound
norcisapridenorcisapride: metabolite of cisapridebenzamides
phorbol 12-phenylacetate 13-acetate 20-homovanillatephorbol 12-phenylacetate 13-acetate 20-homovanillate: behavior contrasts with resiniferatoxin and capsaicin in the lack of cooperativity in binding vanilloid (capsaicin) receptor
prucaloprideprucalopride: a 5-HT4 agonist enterokinetic compoundbenzamides
6-iodonordihydrocapsaicin6-iodonordihydrocapsaicin: a TRPV1 antagonistmethoxybenzenes;
phenols
pinosylvinpinosylvin: phytoalexin found in pine and eucalyptuspinosylvin
cholecalciferolcalciol : A hydroxy seco-steroid that is (5Z,7E)-9,10-secocholesta-5,7,10(19)-triene in which the pro-S hydrogen at position 3 has been replaced by a hydroxy group. It is the inactive form of vitamin D3, being hydroxylated in the liver to calcidiol (25-hydroxyvitamin D3), which is then further hydroxylated in the kidney to give calcitriol (1,25-dihydroxyvitamin D3), the active hormone.

Cholecalciferol: Derivative of 7-dehydroxycholesterol formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. It differs from ERGOCALCIFEROL in having a single bond between C22 and C23 and lacking a methyl group at C24.
D3 vitamins;
hydroxy seco-steroid;
seco-cholestane;
secondary alcohol;
steroid hormone
geroprotector;
human metabolite
harmineharmine : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7.

Harmine: Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's.
harmala alkaloidanti-HIV agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
metabolite
Pinosylvin methyl etherstilbenoid
pterostilbenediether;
methoxybenzenes;
stilbenol
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
neuroprotective agent;
neurotransmitter;
plant metabolite;
radical scavenger
shogaolshogaol: from ginger, ZINGIBER OFFICINALE; less mutagenic than GINGEROL; structure given in first sourceenone;
monomethoxybenzene;
phenols
anandamideanandamide : An N-acylethanolamine 20:4 resulting from the formal condensation of carboxy group of arachidonic acid with the amino group of ethanolamine.endocannabinoid;
N-acylethanolamine 20:4
human blood serum metabolite;
neurotransmitter;
vasodilator agent
arachidonyl dopaminearachidonyl dopamine: a ligand for the vanilloid receptor VR1catechols;
fatty amide;
N-(fatty acyl)-dopamine;
secondary carboxamide
4,4'-dihydroxystilbenestilbene-4,4'-diol
linoleoyl ethanolamidelinoleoyl ethanolamide : An N-acylethanolamine 18:2 that is the ethanolamide of linoleic acid.

linoleoyl ethanolamide: RN given for (Z,Z)-isomer
N-acylethanolamine 18:2EC 3.5.1.99 (fatty acid amide hydrolase) inhibitor
n-oleoylethanolamineN-oleoylethanolamine: ceramidase inhibitor

oleoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of oleic acid. The monounsaturated analogue of the endocannabinoid anandamide.
endocannabinoid;
N-(long-chain-acyl)ethanolamine;
N-acylethanolamine 18:1
EC 3.5.1.23 (ceramidase) inhibitor;
geroprotector;
PPARalpha agonist
4-hydroxystilbene4-hydroxystilbene: RN given refers to cpd without isomeric designation

stilben-4-ol : A phenol having the structure of stilbene with a hydroxy function at C-4 of one of the phenyl rings; the stereochemistry across the alkene bond is not specified.
stilben-4-ol
6-methylpurine6-methylpurine : Purine bearing a methyl substituent at position 6.purinesEC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor
olvanilmethoxybenzenes;
phenols
l 7458703-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo(2,3-b)pyridine: selective for D(4) receptors; structure in first sourcepiperazines
cannabigerolcannabigerol : A member of the class of resorcinols that is resorcinol which is substituted by a (2E)-3,7-dimethylocta-2,6-dien-1-yl group at position 2 and by a pentyl group at position 5. It is a natural product found in Cannabis sativa and Helichrysum species.

cannabigerol: RN given refers to (E)-isomer; structure given in first source
phytocannabinoid;
resorcinols
anti-inflammatory agent;
antibacterial agent;
antioxidant;
appetite enhancer;
cannabinoid receptor agonist;
neuroprotective agent;
plant metabolite
3,5-dimethoxy-trans-stilbene3,5-dimethoxystilbene: structure in first sourcestilbenoid
albaconolalbaconol: from the mushroom Albatrellus; structure in first source
Piperaninebenzodioxoles
piperlongumininepiperlonguminine: from Piper longum; structure in first sourcebenzodioxoles
naltrexonenaltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.

Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
cyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound
antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
batimastatbatimastat : A secondary carboxamide resulting from the formal condensation of the carboxy group of (2S,3R)-5-methyl-3-{[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]carbamoyl}-2-[(thiophen-2-ylsulfanyl)methyl]hexanoic acid with the amino group of hydroxylamine. It a broad-spectrum matrix metalloprotease inhibitor.

batimastat: structure given in first source; a synthetic matrix metalloproteinase inhibitor
hydroxamic acid;
L-phenylalanine derivative;
organic sulfide;
secondary carboxamide;
thiophenes;
triamide
angiogenesis inhibitor;
antineoplastic agent;
matrix metalloproteinase inhibitor
3,4',5-trimethoxystilbene3,4',5-trimethoxystilbene: structure in first source
catharanthinealkaloid ester;
bridged compound;
methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
tertiary amino compound
iodoresiniferatoxiniodoresiniferatoxin: a vanilloid receptor 1 antagonist
ginkgolide b
palonosetronpalonosetron : 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
1-(3-(5-(1,2,4-triazol-4-yl)-1h-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine1-(3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine: an h5-HT(1D) receptor agonist; structure in first source
arvanilarvanil: structure in first sourcemethoxybenzenes;
phenols
am 404anilide
sb 269970SB 269970: a 5-HT(7) antagonist; structure in first sourcesulfonamide
dutasteridedutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland.

Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.
(trifluoromethyl)benzenes;
aza-steroid;
delta-lactam
antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
sarizotansarizotan: serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models
2-ethyl-5-methoxy-n,n-dimethyltryptamine2-ethyl-5-methoxy-N,N-dimethyltryptamine: a 5-HT(6) receptor agonist; structure in first source
1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea: structure in first source
azd 0328spiro(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
pnu-282987carbonyl compound;
organohalogen compound
ssr180711SSR180711: a selective alpha7 acetylcholine nicotinic receptor (n-AChRs) partial agonist; structure in first source
s 21007
bn 52020
sb 705498SB 705498: structure in first source
n-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2h)-carboxamideN-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide: a vanilloid receptor 1 antagonist and analgesic; structure in first sourcepiperazines;
pyridines
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride
vortioxetinevortioxetine : An N-arylpiperazine in which the aryl group is specified as 2-[(2,4-dimethylphenyl)sulfanyl]phenyl. Used (as its hydrobromide salt) for treatment of major depressive disorder.

Vortioxetine: A piperazine derivative that acts as a serotonin reuptake inhibitor, as a 5-HT3 receptor antagonist, and 5-HT1A receptor agonist. It is used for the treatment of anxiety and depression.
aryl sulfide;
N-arylpiperazine
antidepressant;
anxiolytic drug;
serotonergic agonist;
serotonergic antagonist
arachidonoylserotoninarachidonoylserotonin: an NSAID with antinociceptive activity; fatty acid amide hydrolase inhibitor; structure in first source

N-arachidonoylserotonin : An N-acylserotonin obtained by formal condensation of the carboxy group of arachidonic acid with the primary amino group of serotonin.
N-acylserotonin;
phenols
anti-inflammatory agent;
anticonvulsant;
antioxidant;
capsaicin receptor antagonist;
EC 3.5.1.99 (fatty acid amide hydrolase) inhibitor;
human metabolite;
signalling molecule
5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h-indole5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole: a 5-HT6 agonist; structure in first sourceindoles
jyl 1421JYL 1421: a vanilloid receptor antagonist; structure in first source
m-chlorophenylguanidine
methylhistaprodifen
fauc 113
histaprodifen
regorafenib(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide
antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor
barettinbarettin: isolated as a Z/E mixture from sponge Geodia barretti; structure in first sourceorganic molecular entity
abt 102ABT 102: a TRPV1 antagonist; structure in first source
jnj 17203212
a 7841681-(3-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethylsulfonyl)phenyl)-1,2,3,6-tetrahydropyridine-4-carboxamide: a TRPV1 antagonist
ly2183240LY2183240: structure in first sourcebiphenyls
methylphenidateN-phenyl-4-(quinolin-2-ylmethyl)piperazine-1-carboxamide: a fatty acid amide hydrolase inhibitor; structure in first source
5-hydroxy-2-(2-phenylethyl)chromone5-hydroxy-2-(2-phenylethyl)chromone: neuroprotective compound from rhizomes of Imperata cylindrica; structure in first source
cannabidivarincannabidivarin: from Cannabis sativamonoterpenoid
af 3535-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine: a P2X3 and P2X2/3 receptor antagonist; structure in first source
amg 517
a 803467A 803467: an Nav1.8 sodium channel blocker; structure in first source
sp 2033-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile: a radioligand for mGlu5 receptor; structure in first source
mavatrepmavatrep: a transient receptor potential vanilloid 1 antagonist; structure in first source
vuf10166
am 6701
cep 26401pyridazines;
ring assembly
pf 3246799
nitd 609NITD 609: an antimalarial and coccidiostat; structure in first source
voacristinevoacristine: indole alkaloid from leaves of Ervatamia coronaria; RN given for 20(S)-isomer; structure given in first source
evp-6124
abt 116ABT 116: a TRPV1 antagonist with analgesic activity; structure in first source
n,n-diallyl-5-methoxytryptamineN,N-diallyl-5-methoxytryptamine: structure in first sourcetryptamines
a-1155463A-1155463: a Bcl-X(L) inhibitor; structure in first source
clozapineclozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.

Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.
benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound
adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
olanzapineolanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.

Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.
benzodiazepine;
N-arylpiperazine;
N-methylpiperazine
antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
tegaserodtegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first sourcecarboxamidine;
guanidines;
hydrazines;
indoles
gastrointestinal drug;
serotonergic agonist
methylaplysinopsinmethylaplysinopsin: isolated from Dictyoceratid sponge Aplysinopsis reticulata; affects serotogenic neurotransmission; structure given in first source
aplysinopsinaplysinopsin: antineoplastic tryptophan deriv from Verongia spengetii (marine sponge); structure