ArticleProceedings of the National Academy of Sciences of the United States of America1996
Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter.
Article in Proceedings of the National Academy of Sciences of the United States of America, 1996. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 157 papers.
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157 citing papers in PubMed, 475 citations in OpenAlex.
- Chromogranin A mediates glucocorticoid-induced enhancement of vesicular dopamine storage and secretion in PC12 cells.The Journal of biological chemistry · 2026Article
- Associations between VMAT1 Polymorphisms and Obesity.Biochemical genetics · 2026Article
- History, pharmacology and therapeutic mechanisms of 3,4-methylenedioxymethamphetamine (MDMA).British journal of pharmacology · 2026Review
- Optogenetic-induced α-synuclein accumulation reveals early synaptic dysfunction in experimental models of Parkinson's disease.NPJ Parkinson's disease · 2025Article
- Peripheral catecholamine systems: an evolutionary perspective.American journal of physiology. Regulatory, integrative and comparative physiology · 2025Review
- Molecular basis of vesicular monoamine transport and neurological drug interactions.Cell reports · 2025Article
- Rapid generation of ventral A9-like dopaminergic neurons from patterned iPSCs.bioRxiv : the preprint server for biology · 2025Article
- VMAT2 inhibitors for the treatment of tardive dyskinesia: a narrative review.CNS spectrums · 2025Review
- Pathogenic mechanism underlying parkinsonism induced by neurotoxicants (MPTP and 6-hydroxydopamine) and α-synuclein: a unifying hypothesis.Journal of molecular cell biology · 2025Review
- Synaptic vesicle characterization of iPSC-derived dopaminergic neurons provides insight into distinct secretory vesicle pools.NPJ Parkinson's disease · 2025Article
- Dopamine-Glutamate and Dopamine-GABA Co-release.Advances in neurobiology · 2025Review
- Decoding serotonin: the molecular symphony behind depression.Frontiers in cellular neuroscience · 2025Review
- Neurotoxicology of dopamine: Victim or assailant?Neurotoxicology · 2024Review
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- Transport and inhibition mechanisms of human VMAT2.Nature · 2024Article
- Transport and inhibition mechanism for VMAT2-mediated synaptic vesicle loading of monoamines.Cell research · 2024Article
- Norepinephrine transporter and vesicular monoamine transporter 2 tumor expression as a predictor of response toPediatric blood & cancer · 2024Article
- Multifaceted modeling of small intestinal neuroendocrine tumors.Endocrine oncology (Bristol, England) · 2024Review
- Associations between methamphetamine use disorder andDialogues in clinical neuroscience · 2024Article
97 more citing papers are in PubMed but not listed here.
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A second isoform of the human vesicular monoamine transporter (hVMAT) has been cloned from a pheochromocytoma cDNA library. The contribution of the two transporter isoforms to monoamine storage in human neuroendocrine tissues was examined with isoform-specific polyclonal antibodies against hVMAT1 and hVMAT2. Central, peripheral, and enteric neurons express only VMAT2. VMAT1 is expressed exclusively in neuroendocrine, including chromaffin and enterochromaffin, cells. VMAT1 and VMAT2 are coexpressed in all chromaffin cells of the adrenal medulla. VMAT2 alone is expressed in histamine-storing enterochromaffin-like cells of the oxyntic mucosa of the stomach. The transport characteristics and pharmacology of each VMAT isoform have been directly compared after expression in digitonin-permeabilized fibroblastic (CV-1) cells, providing information about substrate feature recognition by each transporter and the role of vesicular monoamine storage in the mechanism of action of psychopharmacologic and neurotoxic agents in human. Serotonin has a similar affinity for both transporters. Catecholamines exhibit a 3-fold higher affinity, and histamine exhibits a 30-fold higher affinity, for VMAT2. Reserpine and ketanserin are slightly more potent inhibitors of VMAT2-mediated transport than of VMAT1-mediated transport, whereas tetrabenazine binds to and inhibits only VMAT2. N-methyl-4-phenylpyridinium, phenylethylamine, amphetamine, and methylenedioxymethamphetamine are all more potent inhibitors of VMAT2 than of VMAT1, whereas fenfluramine is a more potent inhibitor of VMAT1-mediated monamine transport than of VMAT2-mediated monoamine transport. The unique distributions of hVMAT1 and hVMAT2 provide new markers for multiple neuroendocrine lineages, and examination of their transport properties provides mechanistic insights into the pharmacology and physiology of amine storage in cardiovascular, endocrine, and central nervous system function.
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