Page last updated: 2024-10-24

monoamine:proton antiporter activity

Definition

Target type: molecularfunction

Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: H+(out) + monoamine(in) = H+(in) + monoamine(out). [TC:2.A.1.2.11, TC:2.A.1.2.12]

Monoamine:proton antiporter activity describes a membrane transport protein that moves monoamines (e.g., dopamine, serotonin, norepinephrine) across a membrane against their concentration gradient, using the electrochemical gradient of protons (H+). This transport mechanism is essential for maintaining proper concentrations of these neurotransmitters within cells and synapses. The protein facilitates the movement of a monoamine molecule into the cell along with the movement of one or more protons out of the cell. This coupled movement of monoamines and protons is driven by the electrochemical potential difference across the membrane, which is generated by the proton gradient. Monoamine:proton antiporters play a crucial role in a variety of physiological processes, including:
- **Neurotransmission:** Regulation of neurotransmitter levels in synapses, influencing neuronal communication and behavior.
- **Cellular homeostasis:** Maintaining appropriate intracellular concentrations of monoamines, which are essential for various cellular functions.
- **Drug targeting:** Antiporters are targets for various drugs that act on the nervous system, such as antidepressants, antipsychotics, and psychostimulants. These drugs can modulate the activity of the antiporter, altering monoamine levels and affecting neurotransmission.
- **Disease pathogenesis:** Dysregulation of monoamine:proton antiporter activity can contribute to neurological disorders such as Parkinson's disease, depression, and schizophrenia.
In summary, monoamine:proton antiporter activity is a vital membrane transport process that ensures proper regulation of monoamine levels within cells and synapses, contributing to diverse physiological and pharmacological functions.'
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Proteins (4)

ProteinDefinitionTaxonomy
Synaptic vesicular amine transporterA synaptic vesicular amine transporter that is encoded in the genome of cow. [OMA:Q27963, PRO:DNx]Bos taurus (cattle)
Vesicular acetylcholine transporterA vesicular acetylcholine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16572]Homo sapiens (human)
Synaptic vesicular amine transporterA synaptic vesicular amine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q05940]Homo sapiens (human)
Chromaffin granule amine transporterA chromaffin granule amine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:P54219]Homo sapiens (human)

Compounds (15)

CompoundDefinitionClassesRoles
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
vesamicolvesamicol: RN given refers to parent cpd; structurepiperidines
reserpinereserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.

Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.
alkaloid ester;
methyl ester;
yohimban alkaloid
adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
tetrabenazine9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7.benzoquinolizine;
cyclic ketone;
tertiary amino compound
2h-benzo(a)quinolizin-2-ol, 2-ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-2H-Benzo(a)quinolizin-2-ol, 2-Ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-: Proposed catecholamine depletor.
hemicholinium 3Hemicholinium 3: A potent inhibitor of the high affinity uptake system for CHOLINE. It has less effect on the low affinity uptake system. Since choline is one of the components of ACETYLCHOLINE, treatment with hemicholinium can deplete acetylcholine from cholinergic terminals. Hemicholinium 3 is commonly used as a research tool in animal and in vitro experiments.
reserpic acidreserpic acid: inhibitor of norepinephrine transport into chromaffin vesicle ghosts; RN given refers to (3beta,16beta,17alpha,18beta,20alpha)-isomer parent cpd; structure given in first sourceyohimban alkaloid
4-phenylpiperidine
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
dihydrotetrabenazinedihydrotetrabenazine: RN given refers to cpd without isomeric designationisoquinolines
vesamicolpiperidines
lobeline
lobelanelobelane: structure in first source
mrk 560MRK 560: a gamma-secretase inhibitor; MRK-560 is the (cis)-isomer; structure in first source
benzovesamicolbenzovesamicol: structure in first source