A compound that inhibits the re-uptake of the neurotransmitter GABA from the synapse into the pre-synaptic neuron, so increasing the extracellular concentrations of the neurotransmitter and hence increasing neurotransmission.
ChEBI ID: 85384
| Member | Definition | Class |
|---|---|---|
| guvacine | A alpha,beta-unsaturated monocarboxylic acid that is nicotinic acid which has been hydrogenated at the 1-2 and 5-6 positions of the pyridine ring. | guvacine |
| tiagabine | A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy. | tiagabine |
| tiagabine hydrochloride | A hydrochloride resulting from the reaction of equimolar amounts of tiagabine and hydrogen chloride. A GABA reuptake inhibitor, it is used for the treatment of epilepsy. | tiagabine hydrochloride |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 11 (1.84) | 18.7374 |
| 1990's | 168 (28.14) | 18.2507 |
| 2000's | 265 (44.39) | 29.6817 |
| 2010's | 126 (21.11) | 24.3611 |
| 2020's | 27 (4.52) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 102 (15.81%) | 5.53% |
| Reviews | 110 (17.05%) | 6.00% |
| Case Studies | 56 (8.68%) | 4.05% |
| Observational | 1 (0.16%) | 0.25% |
| Other | 376 (58.29%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| arylsulfatase A | Homo sapiens (human) | Potency | 0.0135 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 37.9330 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 5.9728 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 38.9018 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 1.4580 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 21.1317 | 1 | 1 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 0.8913 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 1.2589 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 11.4239 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 0.3349 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 3.9811 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 31.6768 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 2 | 2 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 8.4120 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Sodium- and chloride-dependent GABA transporter 1 | Homo sapiens (human) | Kd | 0.0937 | 2 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Sodium- and chloride-dependent GABA transporter 1 | Homo sapiens (human) | INH | 0.0700 | 1 | 1 |
| Sodium- and chloride-dependent GABA transporter 1 | Homo sapiens (human) | Km | 24.5500 | 2 | 2 |