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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| Protein | Definition | Taxonomy |
|---|---|---|
| Synaptic vesicular amine transporter | A synaptic vesicular amine transporter that is encoded in the genome of cow. [OMA:Q27963, PRO:DNx] | Bos taurus (cattle) |
| Vesicular acetylcholine transporter | A vesicular acetylcholine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16572] | Homo sapiens (human) |
| Synaptic vesicular amine transporter | A synaptic vesicular amine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q05940] | Homo sapiens (human) |
| Chromaffin granule amine transporter | A chromaffin granule amine transporter that is encoded in the genome of human. [PRO:DNx, UniProtKB:P54219] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| ketanserin | ketanserin : 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 |
| vesamicol | vesamicol: RN given refers to parent cpd; structure | piperidines | |
| reserpine | reserpine : 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 |
| tetrabenazine | 9,10-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 3 | Hemicholinium 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 acid | reserpic 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 source | yohimban 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 |
| dihydrotetrabenazine | dihydrotetrabenazine: RN given refers to cpd without isomeric designation | isoquinolines | |
| vesamicol | piperidines | ||
| lobeline | |||
| lobelane | lobelane: structure in first source | ||
| mrk 560 | MRK 560: a gamma-secretase inhibitor; MRK-560 is the (cis)-isomer; structure in first source | ||
| benzovesamicol | benzovesamicol: structure in first source |