Proteins > Synaptic vesicular amine transporter
Page last updated: 2024-08-07 23:45:41
Synaptic vesicular amine transporter
A synaptic vesicular amine transporter that is encoded in the genome of rat. [OMA:Q01827, PRO:DNx]
Synonyms
Monoamine transporter;
Solute carrier family 18 member 2;
Vesicular amine transporter 2;
VAT2
Research
Bioassay Publications (19)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 6 (31.58) | 29.6817 |
| 2010's | 11 (57.89) | 24.3611 |
| 2020's | 2 (10.53) | 2.80 |
Compounds (16)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| reserpine | Rattus norvegicus (Norway rat) | IC50 | 0.0177 | 1 | 10 |
| tetrabenazine | Rattus norvegicus (Norway rat) | IC50 | 0.1371 | 1 | 6 |
| tetrabenazine | Rattus norvegicus (Norway rat) | Ki | 0.0103 | 2 | 2 |
| 2h-benzo(a)quinolizin-2-ol, 2-ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy- | Rattus norvegicus (Norway rat) | IC50 | 0.5000 | 1 | 1 |
| 2h-benzo(a)quinolizin-2-ol, 2-ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy- | Rattus norvegicus (Norway rat) | Ki | 0.0280 | 1 | 1 |
| methamphetamine | Rattus norvegicus (Norway rat) | Ki | 41.2800 | 2 | 2 |
| lobeline | Rattus norvegicus (Norway rat) | Ki | 2.5023 | 6 | 6 |
| tadalafil | Rattus norvegicus (Norway rat) | IC50 | 0.0120 | 1 | 1 |
| gefitinib | Rattus norvegicus (Norway rat) | IC50 | 0.0010 | 1 | 1 |
| erlotinib | Rattus norvegicus (Norway rat) | IC50 | 0.0010 | 1 | 1 |
| lobeline | Rattus norvegicus (Norway rat) | Ki | 4.1100 | 2 | 2 |
| bosutinib | Rattus norvegicus (Norway rat) | IC50 | 0.1000 | 1 | 1 |
| lobelane | Rattus norvegicus (Norway rat) | Ki | 2.1582 | 10 | 10 |
| tetrabenazine | Rattus norvegicus (Norway rat) | IC50 | 0.0406 | 2 | 2 |
| tetrabenazine | Rattus norvegicus (Norway rat) | Ki | 36.4000 | 1 | 1 |
| 4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide | Rattus norvegicus (Norway rat) | Ki | 0.6960 | 2 | 2 |
| dihydrotetrabenazine, (2alpha,3beta,11bbeta)-isomer | Rattus norvegicus (Norway rat) | IC50 | 0.0174 | 2 | 2 |
| dihydrotetrabenazine, (2alpha,3beta,11bbeta)-isomer | Rattus norvegicus (Norway rat) | Ki | 0.0023 | 3 | 3 |
| acp-196 | Rattus norvegicus (Norway rat) | IC50 | 0.0031 | 1 | 1 |
| sildenafil | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tetrabenazine | Rattus norvegicus (Norway rat) | Kd | 0.0567 | 1 | 5 |
Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine.The Journal of biological chemistry, , Nov-08, Volume: 288, Issue:45, 2013
Preparation and evaluation of tetrabenazine enantiomers and all eight stereoisomers of dihydrotetrabenazine as VMAT2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011
Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Quinolyl analogues of norlobelane: novel potent inhibitors of [(3)H]dihydrotetrabenazine binding and [(3)H]dopamine uptake at the vesicular monoamine transporter-2.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 25, Issue:13, 2015
Synthesis and evaluation of novel azetidine analogs as potent inhibitors of vesicular [3H]dopamine uptake.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Exploring the effect of MedChemComm, , Volume: 4, Issue:3, 2013
Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 16, Issue:19, 2006
Fluoroethoxy-1,4-diphenethylpiperidine and piperazine derivatives: Potent and selective inhibitors of [Bioorganic & medicinal chemistry letters, , 12-15, Volume: 27, Issue:24, 2017
Lobelane analogues containing 4-hydroxy and 4-(2-fluoroethoxy) aromatic substituents: Potent and selective inhibitors of [(3)H]dopamine uptake at the vesicular monoamine transporter-2.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 26, Issue:10, 2016
Quinolyl analogues of norlobelane: novel potent inhibitors of [(3)H]dihydrotetrabenazine binding and [(3)H]dopamine uptake at the vesicular monoamine transporter-2.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 25, Issue:13, 2015
Synthesis and evaluation of novel azetidine analogs as potent inhibitors of vesicular [3H]dopamine uptake.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Exploring the effect of MedChemComm, , Volume: 4, Issue:3, 2013
Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Biotransformation: Impact and Application of Metabolism in Drug Discovery.ACS medicinal chemistry letters, , Nov-12, Volume: 11, Issue:11, 2020
Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligands.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 21, Issue:11, 2011
Preparation and evaluation of tetrabenazine enantiomers and all eight stereoisomers of dihydrotetrabenazine as VMAT2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011