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positive regulation of sodium:proton antiporter activity

Definition

Target type: biologicalprocess

Any process that activates or increases the activity of a sodium:hydrogen antiporter, which catalyzes the reaction: Na+(out) + H+(in) = Na+(in) + H+(out). [GOC:mah]

Positive regulation of sodium:proton antiporter activity involves the modulation of proteins responsible for transporting sodium ions (Na+) out of the cell and protons (H+) into the cell, against their concentration gradients. This process is crucial for maintaining cellular pH, ion homeostasis, and other vital physiological functions. Here is a detailed breakdown:

1. **Sodium:Proton Antiporters (NHEs):** These membrane-bound proteins facilitate the exchange of Na+ and H+ across the cell membrane. They are driven by the electrochemical gradient of Na+, meaning that the movement of Na+ down its concentration gradient provides the energy for the movement of H+ against its concentration gradient.

2. **Regulation Mechanisms:** The activity of NHEs can be regulated by various mechanisms, including:
- **Phosphorylation:** NHE activity can be increased or decreased by phosphorylation events, catalyzed by kinases and phosphatases, respectively.
- **Binding of Regulatory Proteins:** Specific proteins can bind to NHEs and modulate their activity. Some proteins activate NHEs, while others inhibit them.
- **Cellular Signaling Pathways:** NHE activity is influenced by various signaling pathways, including those triggered by hormones, neurotransmitters, and growth factors.

3. **Role in pH Regulation:** NHEs play a crucial role in regulating intracellular pH. When the intracellular pH drops (becomes more acidic), NHEs transport H+ out of the cell, restoring pH balance. This is essential for maintaining optimal conditions for enzyme activity and other cellular processes.

4. **Importance in Ion Homeostasis:** NHEs contribute to ion homeostasis by regulating the intracellular concentration of Na+ and H+. This is vital for maintaining cell volume and osmotic pressure.

5. **Other Biological Functions:** NHEs are involved in various other biological processes, including:
- **Cell Growth and Proliferation:** NHE activation promotes cell growth and proliferation.
- **Cell Migration:** NHEs contribute to cell migration and movement.
- **Tissue Remodeling:** NHEs are involved in tissue remodeling and repair.

6. **Clinical Significance:** Dysregulation of NHE activity has been implicated in various diseases, including:
- **Hypertension:** Increased NHE activity contributes to hypertension by promoting sodium retention.
- **Cancer:** NHEs promote cell growth and proliferation, contributing to cancer development.
- **Kidney Disease:** NHE dysregulation can lead to kidney damage and dysfunction.

7. **Therapeutic Targets:** Due to their involvement in various physiological processes and disease states, NHEs are attractive targets for therapeutic interventions. Developing drugs that modulate NHE activity could potentially lead to new treatments for hypertension, cancer, kidney disease, and other conditions.'
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Proteins (1)

ProteinDefinitionTaxonomy
D(4) dopamine receptorA D(4) dopamine receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P21917]Homo sapiens (human)

Compounds (146)

CompoundDefinitionClassesRoles
2-(n-phenethyl-n-propyl)amino-5-hydroxytetralin2-(N-phenethyl-N-propyl)amino-5-hydroxytetralin: potent, specific D2 dopamine receptor agonist; RN given refers to parent cpdtetralins
3-[(4-chlorophenyl)-phenylmethoxy]-8-methyl-8-azabicyclo[3.2.1]octanediarylmethane
amiodaroneamiodarone : 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
amoxapineamoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.

Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.
dibenzooxazepineadrenergic uptake inhibitor;
antidepressant;
dopaminergic antagonist;
geroprotector;
serotonin uptake inhibitor
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
chlorpromazinechlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.

Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.
organochlorine compound;
phenothiazines;
tertiary amine
anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
cleboprideclebopride: antidopaminergic; RN given refers to parent cpd; structurepiperidines
clotrimazoleconazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes
antiinfective agent;
environmental contaminant;
xenobiotic
disulfiramorganic disulfide;
organosulfur acaricide
angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor
ebastineorganic molecular entity
econazole1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 4-chlorobenzyl group.

econazole : A racemate composed of equimolar amounts of (R)- and (S)-econazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections.

Econazole: An imidazole derivative that is commonly used as a topical antifungal agent.
dichlorobenzene;
ether;
imidazoles;
monochlorobenzenes
fentanylfentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.

Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078)
anilide;
monocarboxylic acid amide;
piperidines
adjuvant;
anaesthesia adjuvant;
anaesthetic;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
fluphenazineN-alkylpiperazine;
organofluorine compound;
phenothiazines
anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug
haloperidolhaloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.

Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)
aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol
antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
isoproterenolisoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.

Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
catechols;
secondary alcohol;
secondary amino compound
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
jl 18JL 18: a pyridobenzodiazepine derivative bioisoster of clozapine
ketanserinketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group.

Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.
aromatic ketone;
organofluorine compound;
piperidines;
quinazolines
alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
loperamideloperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.

Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.
monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol
anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
loxapineLoxapine: An antipsychotic agent used in SCHIZOPHRENIA.dibenzooxazepineantipsychotic agent;
dopaminergic antagonist
methadone6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4.

methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.

Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)
benzenes;
diarylmethane;
ketone;
tertiary amino compound
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
miconazole1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 2,4-dichlorobenzyl group.

miconazole : A racemate composed of equimolar amounts of (R)- and (S)-miconazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.

Miconazole: An imidazole antifungal agent that is used topically and by intravenous infusion.
dichlorobenzene;
ether;
imidazoles
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
modafinil2-[(diphenylmethyl)sulfinyl]acetamide : A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group.

modafinil : A racemate comprising equimolar amounts of armodafinil and (S)-modafinil. A central nervous system stimulant, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. The optical enantiomers of modafinil have similar pharmacological actions in animals.

Modafinil: A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.
monocarboxylic acid amide;
sulfoxide
mosapramine1'-[3-(3-chloro-10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)propyl]hexahydro-2H-spiro[imidazo[1,2-a]pyridine-3,4'-piperidin]-2-one : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(2-oxohexahydro-2H-spiro[imidazo[1,2-a]pyridine-3,4'-piperidin]-1'-yl)propyl group.

mosapramine : A racemate comprising equimolar amounts of (R)- and (S)-mosapramine. It is a second-generation antipsychotic used for the treatment of schizophrenia.

mosapramine: structure given in first source
azaspiro compound;
dibenzoazepine;
organochlorine compound;
tertiary amino compound
nemonaprideN-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide : A benzamide obtained by formal condensation of the carboxy group of 5-chloro-2-methoxy-4-(methylamino)benzoic acid with the amino group of 1-benzyl-2-methylpyrrolidin-3-amine.benzamides;
monochlorobenzenes;
monomethoxybenzene;
N-alkylpyrrolidine;
secondary amino compound;
secondary carboxamide;
substituted aniline
prazosinprazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.

Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines
alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
prochlorperazineprochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.

Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612)
N-alkylpiperazine;
N-methylpiperazine;
organochlorine compound;
phenothiazines
alpha-adrenergic antagonist;
antiemetic;
cholinergic antagonist;
dopamine receptor D2 antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic
quetiapinedibenzothiazepine;
N-alkylpiperazine;
N-arylpiperazine
adrenergic antagonist;
dopaminergic antagonist;
histamine antagonist;
second generation antipsychotic;
serotonergic antagonist
rbi 257RBI 257: ligand for dopamine D4 receptors; structure in first source
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
ropiniroleindolones;
tertiary amine
antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
dopamine agonist
3-(3-cyanophenyl)-n-n-propylpiperidine3-(3-cyanophenyl)-N-n-propylpiperidine: a dopamine autoreceptor antagonist; RN given for (+-)-isomer
spiperonespiperone : An azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.

Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.
aromatic ketone;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound
alpha-adrenergic antagonist;
antipsychotic agent;
dopaminergic antagonist;
psychotropic drug;
serotonergic antagonist
sulpiridesulpiride : A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine.

Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)
benzamides;
N-alkylpyrrolidine;
sulfonamide
antidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
thioridazinethioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.

Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.
phenothiazines;
piperidines
alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamidepiperazines
zotepinezotepine: structuredibenzothiepine;
tertiary amino compound
alpha-adrenergic drug;
second generation antipsychotic;
serotonergic drug
lysergic acid diethylamidelysergic acid diethylamide : An ergoline alkaloid arising from formal condensation of lysergic acid with diethylamine.

Lysergic Acid Diethylamide: Semisynthetic derivative of ergot (Claviceps purpurea). It has complex effects on serotonergic systems including antagonism at some peripheral serotonin receptors, both agonist and antagonist actions at central nervous system serotonin receptors, and possibly effects on serotonin turnover. It is a potent hallucinogen, but the mechanisms of that effect are not well understood.
ergoline alkaloid;
monocarboxylic acid amide;
organic heterotetracyclic compound
dopamine agonist;
hallucinogen;
serotonergic agonist
apomorphineApomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
phenyltoloxaminephenyltoloxamine: RN given refers to parent cpd; structurediarylmethane
indopanalpha-methyltryptamine : A tryptamine derivative having a methyl substituent at the alpha-position.

indopan: RN given refers to parent cpd without isomeric designation
tryptamines
normethadonenormethadone: RN given refers to parent cpddiarylmethane
azaperoneazaperone : An N-arylpiperazine that is 2-(piperazin-1-yl)pyridine in which the amino hydrogen is replaced by a 3-(4-fluobenzoyl)propyl group. Used mainly as a tranquiliser for pigs and elephants.

Azaperone: A butyrophenone used in the treatment of PSYCHOSES.
aminopyridine;
aromatic ketone;
monofluorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
tertiary amino compound
antipsychotic agent;
dopaminergic antagonist
11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine: structure given in first source
2-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine2-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine: structure given in first source
benperidolBenperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It has been used in the treatment of aberrant sexual behavior. (From Martindale, The Extra Pharmacopoeia, 30th ed, p567)aromatic ketone
canadine, (s)-isomer(S)-canadine : The (S)-enantiomer of canadine.an (S)-7,8,13,14-tetrahydroprotoberberine;
canadine
plant metabolite
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
lisurideLisuride: An ergot derivative that acts as an agonist at dopamine D2 receptors (DOPAMINE AGONISTS). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (SEROTONIN RECEPTOR AGONISTS).monocarboxylic acid amideantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
serotonergic agonist
1-(3-chloro-5-benzo[b][1]benzoxepinyl)-4-methylpiperazineN-alkylpiperazine;
organic heterotricyclic compound
penfluridolPenfluridol: One of the long-acting ANTIPSYCHOTIC AGENTS used for maintenance or long-term therapy of SCHIZOPHRENIA and other PSYCHOTIC DISORDERS.diarylmethane
butaclamolamino alcohol;
organic heteropentacyclic compound;
tertiary alcohol;
tertiary amino compound
dopaminergic antagonist
haloperidol decanoateorganic molecular entity
remoxiprideRemoxipride: An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.dimethoxybenzene
quinpirolequinpirole : A pyrazoloquinoline that is (4aR,8aR)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrazolo[3,4-g]quinoline substituted by a propyl group at position 5. It acts as a dopamine agonist.

Quinpirole: A dopamine D2/D3 receptor agonist.
pyrazoloquinolinedopamine agonist
preclamolpiperidines
ipsapironeN-arylpiperazine
eticloprideeticlopride: blocks dopamine-D2 binding sites; structure given in first source; RN given refers to (S)-isomersalicylamides
n 0437, (-)-isomerrotigotine: Antiparkinson Agent and dopamine receptor agonist; structure given in first source; RN given refers to cpd without isomeric designationtetralins
sertindolesertindole : 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
fananserinfananserin: RN & structure given in first sourcenaphthalenes;
sulfonic acid derivative
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
dopamine hydrochlorideP 498: structure in first source; do not confuse with dopamine chloride, also known as P 498catecholamine
mezilaminemezilamine: RN given refers to parent cpd; synonym O 6553 refers to HCl; structure
tetrahydropalmatinean (S)-7,8,13,14-tetrahydroprotoberberine;
berberine alkaloid;
organic heterotetracyclic compound
adrenergic agent;
dopaminergic antagonist;
non-narcotic analgesic
tandospironetandospirone : A dicarboximide that is (3aR,4S,7R,7aS)-hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione which is substituted by a 4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl group at position 2. It is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM).

tandospirone: structure given in first source
bridged compound;
dicarboximide;
N-alkylpiperazine;
N-arylpiperazine;
pyrimidines
antidepressant;
anxiolytic drug
way 100635
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
ecopipamecopipam: structure given in first sourcebenzazepine
3-iodo-2-hydroxy-6-methoxy-n-((1-ethyl-2-pyrrolidinyl)methyl)benzamide3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide: a dopamine receptor imaging agent; RN refers to (S)-isomer; RN & structure given in first source
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
aj 76(1S,2R)-5-methoxy-1-methyl-2-(propylamino)tetralin : A secondary amino compound that consists of tetralin bearing methyl, propylamino and methoxy groups at positions 1, 2 and 5 respectively. Dopamine receptor antagonist with preferential action at presynaptic receptors (pKi values are 6.95, 6.67, 6.37, 6.21 and 6.07 at hD3. hD4, hD2S, hD2L and rD2 receptors respectively).

5-methoxy-1-methyl-2-(n-propylamino)tetralin: RN given refers to cis-(+)-isomer; structure given in first source
secondary amino compound;
tetralins
dopaminergic antagonist
1,2,3,6-tetrahydro-4-phenyl-1-((3-phenyl-3-cyclohexen-1-yl)methyl)pyridine1,2,3,6-tetrahydro-4-phenyl-1-((3-phenyl-3-cyclohexen-1-yl)methyl)pyridine: RN refers to (R)-isomer; a dopamine autoreceptor agonist; structure given in first source
n 0734N 0734: dopamine receptor agonist; structure given in first source
l 741742L 741742: selective toward D4 receptors; structure in first sourceprimary amine
sonepiprazole
l 7416263-(4-(4-chlorophenyl-4-hydroxypiperidino)methyl)indole: structure in first sourcepiperidines
sk&f 89124SK&F 89124: structure given in first source
chloroethylnorapomorphinechloroethylnorapomorphine: irreversible dopamine receptor antagonist; RN given refers to (R)-isomer; structure given in first source
harmalanharmalan: structure given in first sourceharmala alkaloid
corydalminecorydalmine: antagonizes dopamine receptors; structure given in first source; RN given refers to (S)-isomer
n-demethyllysergic acid diethylamideN-demethyllysergic acid diethylamide: RN given refers to (betaa)-isomer
nantenine, (+-)-isomer
ngd 94-1NGD 94-1: D(4) receptor antagonist; structure in first source
roxindoleindolesalpha-adrenergic antagonist;
serotonergic drug
1-methyl-6-methoxy-dihydro-beta-carboline
tetrahydrocolumbamine(S)-tetrahydrocolumbamine : A berberine alkaloid consisting of columbamine having four extra hydrogens at positions 5, 8, 13 and 13a and (S)-configuration.

tetrahydrocolumbamine: a dopamine receptor ligand; from Polygala tenuifolia; structure given in first source
berberine alkaloid;
organic heterotetracyclic compound
sb 243213SB 243213: a 5-HT2c inverse agonist; structure in first sourceindolyl carboxylic acid
levosulpiride(S)-(-)-sulpiride : An optically active form of sulpiride having (S)-configuration. The active enantiomer of the racemic drug sulpiride. Selective D2-like dopamine antagonist (Ki values are ~ 0.015. ~ 0.013, 1, ~ 45 and ~ 77 muM at D2, D3, D4, D1 and D5 receptors respectively).sulpirideantidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
tamoxifenstilbenoid;
tertiary amino compound
angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
racloprideRaclopride: A substituted benzamide that has antipsychotic properties. It is a dopamine D2 receptor (see RECEPTORS, DOPAMINE D2) antagonist.salicylamides
bp 897BP 897: a dopamine D3 receptor agonist; structure in first sourcenaphthalenecarboxamide
n-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamideN-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide: dopamine D4 ligand; structure in first source
pd 168,077N-((4-(2-cyanophenyl)-1-piperazinyl)methyl)-3-methylbenzamide: a D4 dopamine receptor agonistpiperazines
le 300indoles
abt724ABT724: dopamine D4 receptors agonist; structure in first sourcepiperazines;
pyridines
quercetin7-hydroxyflavonol;
pentahydroxyflavone
antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
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
preclamolpreclamol: centrally acting dopamine receptor agonist with selectivity for autoreceptors
l 7458703-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo(2,3-b)pyridine: selective for D(4) receptors; structure in first sourcepiperazines
pd 1289071-benzopyran
obelinobelin: calcium-sensitive photoprotein obtained from the hydroid Obelia geniculata
sb 271046SB 271046: 5-HT(6) receptor antagonist; structure in first source
jl 13 compoundJL 13 compound: structure given in first source
dihydrexidinephenanthridines
7-hydroxy-2-n,n-dipropylaminotetralin, (r)-isomer
l 750667L 750667: structure given in first sourcepiperazines
uh 232tetralins
stepholidinestepholidine: protoberberine alkaloid isolated from opium; dual D1 receptor agonist and D2 receptor antagonist
sarizotansarizotan: serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models
ms-245N,N-dimethyl-2-(1-(benzenesulfonyl)-5-methoxy-1H-indol-3-yl)ethylamine: a 5-HT(6) receptor ligand; structure in first source
armodafinilarmodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness.2-[(diphenylmethyl)sulfinyl]acetamidecentral nervous system stimulant;
eugeroic
n-demethylloperamidedesmethyl loperamide : A monocarboxylic acid amide that is the methylamide of 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylbutanoic acid.

N-demethylloperamide: loperamide metabolite; structure in first source
monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol
drug metabolite
cp 293019CP 293019: structure given in first source
f 13640befiradol: a selective serotonin 5-HT1A receptor agonist
slv 313
fauc 346FAUC 346: a D3 dopamine receptor antagonist; structure in first source
ngb 2904NGB 2904: a dopamine D3 receptor antagonist; structure in first sourcefluorenes
4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one: structure in first source
pnu 109291PNU 109291: 5-HT(1D) receptor agonist; structure in first source
pnu 96415epiperazines
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride
n-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamideN-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide: structure in first source
77-lh-28-177-LH-28-1: a CNS penetrant, selective M1 muscarinic receptor agonist, structure in first source
fauc 365FAUC 365: a dopamine D3 receptor antagonist; structure in first source
fauc 213
way-208466
fauc 113
desmethoxyfallypridedesmethoxyfallypride: structure given in first source
2-(3',4',5',6'-tetrahydro-2'h-(2,4') bipyridinyl-1'-yl)-n-m-tolyl-acetamide
cariprazinecariprazine : An N-alkylpiperazine that is N,N-dimethyl-N'-{trans-4-[2-(piperazin-1-yl)ethyl]cyclohexyl}urea substituted at position 4 on the piperazine ring by a 2,3-dichlorophenyl group. Used (as the hydrochloride salt) for treatment of schizophrenia and bipolar disorder.

cariprazine: Structure in first source
5-hydroxy-2-n,n-dipropylaminotetralin, (s)-isomer
naluzotannaluzotan: an antidepressant and anti-anxiety agent; structure in first source
pg 01037
le 404
lassbio-579LASSBio-579: structure in first source
gsk598809GSK598809: a dopamine D3 receptor antagonist
octoclothepine, (s)-isomer
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
nitd 609NITD 609: an antimalarial and coccidiostat; structure in first source
n,n-diallyl-5-methoxytryptamineN,N-diallyl-5-methoxytryptamine: structure in first sourcetryptamines
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