| + |
zolpidem | up-regulates activity 
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263802 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The BZ-sensitive GABAA-Rs can be further subdivided, in that receptors containing the alpha1 subunit have a higher sensitivity to a subpopulation of BZ site ligands, the benzodiazepines quazepam and cinolazepam (Sieghart, 1989) or nonbenzodiazepines such as zolpidem (an imidazopyridine) and a few others, including CL218-872 (triazolopyridazine), zaleplon, and indiplon, and abecarnil (β-carboline), (Olsen and Gordey, 2000; Korpi et al., 2002; Sieghart and Ernst, 2005). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
zaleplon | up-regulates activity
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263804 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The BZ-sensitive GABAA-Rs can be further subdivided, in that receptors containing the alpha1 subunit have a higher sensitivity to a subpopulation of BZ site ligands, the benzodiazepines quazepam and cinolazepam (Sieghart, 1989) or nonbenzodiazepines such as zolpidem (an imidazopyridine) and a few others, including CL218-872 (triazolopyridazine), zaleplon, and indiplon, and abecarnil (β-carboline), (Olsen and Gordey, 2000; Korpi et al., 2002; Sieghart and Ernst, 2005). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
Oxytocin | up-regulates 
|
GABA-A (a1-b1-g2) receptor |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268579 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 33536967 |
OT inhibits corticotropin-releasing factor (CRF) mRNA expression at the hypothalamus, resulting in antistress and anti-anxiety effects| It has been demonstrated that the inhibitory effect of OT on CRF mRNA expression is not a direct one on CRF neurons. GABAergic neurons are present in the surroundings of the PVN (peri-PVN). These GABA-projecting neurons into the PVN inhibits CRF expression via GABAA receptors |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
diazepam | up-regulates activity
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263796 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The traditional BZ site agonists (GABA-enhancing CNS depressants such as diazepam) are active on the GABAA-Rs containing a gamma2 subunit (Pritchett et al., 1989), a beta subunit, and one of the alpha subunits, alpha1, 2, 3, or 5. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
Quazepam | up-regulates activity
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263800 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The BZ-sensitive GABAA-Rs can be further subdivided, in that receptors containing the alpha1 subunit have a higher sensitivity to a subpopulation of BZ site ligands, the benzodiazepines quazepam and cinolazepam (Sieghart, 1989) or nonbenzodiazepines such as zolpidem (an imidazopyridine) and a few others, including CL218-872 (triazolopyridazine), zaleplon, and indiplon, and abecarnil (β-carboline), (Olsen and Gordey, 2000; Korpi et al., 2002; Sieghart and Ernst, 2005). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
GABRA1 | form complex 
binding
|
GABA-A (a1-b1-g2) receptor |
0.639 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263750 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The assembly of GABAA-R as heteropentamers produces complex subtype heterogeneity in structure, which is the major determinant of their pharmacological profile.|Evidence is greatly in favor of a pentameric receptor and most GABAA-R subtypes are formed from two copies of a single alpha, two copies of a single beta, and one copy of another subunit, such as gamma, delta, or epsilon. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
triazolopyridazine | up-regulates activity
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263803 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The BZ-sensitive GABAA-Rs can be further subdivided, in that receptors containing the alpha1 subunit have a higher sensitivity to a subpopulation of BZ site ligands, the benzodiazepines quazepam and cinolazepam (Sieghart, 1989) or nonbenzodiazepines such as zolpidem (an imidazopyridine) and a few others, including CL218-872 (triazolopyridazine), zaleplon, and indiplon, and abecarnil (β-carboline), (Olsen and Gordey, 2000; Korpi et al., 2002; Sieghart and Ernst, 2005). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
beta-carboline | up-regulates activity
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263805 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The BZ-sensitive GABAA-Rs can be further subdivided, in that receptors containing the alpha1 subunit have a higher sensitivity to a subpopulation of BZ site ligands, the benzodiazepines quazepam and cinolazepam (Sieghart, 1989) or nonbenzodiazepines such as zolpidem (an imidazopyridine) and a few others, including CL218-872 (triazolopyridazine), zaleplon, and indiplon, and abecarnil (β-carboline), (Olsen and Gordey, 2000; Korpi et al., 2002; Sieghart and Ernst, 2005). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
cinolazepam | up-regulates activity
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263801 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The BZ-sensitive GABAA-Rs can be further subdivided, in that receptors containing the alpha1 subunit have a higher sensitivity to a subpopulation of BZ site ligands, the benzodiazepines quazepam and cinolazepam (Sieghart, 1989) or nonbenzodiazepines such as zolpidem (an imidazopyridine) and a few others, including CL218-872 (triazolopyridazine), zaleplon, and indiplon, and abecarnil (β-carboline), (Olsen and Gordey, 2000; Korpi et al., 2002; Sieghart and Ernst, 2005). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
GABRG2 | form complex
binding
|
GABA-A (a1-b1-g2) receptor |
0.641 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263752 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The assembly of GABAA-R as heteropentamers produces complex subtype heterogeneity in structure, which is the major determinant of their pharmacological profile.|Evidence is greatly in favor of a pentameric receptor and most GABAA-R subtypes are formed from two copies of a single alpha, two copies of a single beta, and one copy of another subunit, such as gamma, delta, or epsilon. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
GABA-A (a1-b1-g2) receptor | down-regulates 
|
Excitatory_synaptic_transmission |
0.7 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263776 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
GABAA receptors (GABAA-Rs) are the major inhibitory receptors in the central nervous system (CNS). |Mammalian GABAA-Rs are all anion-selective channels. Increased chloride permeability generally reduces neuronal excitability (inhibition) |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| Pathways: | GABAergic synapse |
| + |
GABRB1 | form complex
binding
|
GABA-A (a1-b1-g2) receptor |
0.629 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263751 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
The assembly of GABAA-R as heteropentamers produces complex subtype heterogeneity in structure, which is the major determinant of their pharmacological profile.|Evidence is greatly in favor of a pentameric receptor and most GABAA-R subtypes are formed from two copies of a single alpha, two copies of a single beta, and one copy of another subunit, such as gamma, delta, or epsilon. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Central Nervous System |
| + |
DGC | up-regulates quantity
binding
|
GABA-A (a1-b1-g2) receptor |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-265432 |
|
|
Homo sapiens |
Neuron, Glial Cell |
| pmid |
sentence |
| 22626542 |
In brain, the DGC is involved in the organisation of GABA(A) receptors (GABA(A)Rs) and aquaporin-4 (AQP4)-containing protein complexes in neurons and glia, respectively. DGC-like complexes function in the postsynaptic clustering and stabilisation of GABAARs in a subset of inhibitory GABAergic synapses. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
gamma-aminobutyric acid | up-regulates activity
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263786 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
Gamma-Aminobutyric acid (GABA1), the major inhibitory neurotransmitter in the brain, exerts its action via ionotropic GABAA and metabotropic GABAB receptors. GABAA receptors (GABAA-Rs) are the major inhibitory receptors in the central nervous system (CNS). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | GABAergic synapse |
| + |
GABA-A (a1-b1-g2) receptor | down-regulates
|
CRHR2 |
0.253 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268589 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 33536967 |
OT inhibits corticotropin-releasing factor (CRF) mRNA expression at the hypothalamus, resulting in antistress and anti-anxiety effects| It has been demonstrated that the inhibitory effect of OT on CRF mRNA expression is not a direct one on CRF neurons. GABAergic neurons are present in the surroundings of the PVN (peri-PVN). These GABA-projecting neurons into the PVN inhibits CRF expression via GABAA receptors |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Hypothalamus |
| + |
hydrogencarbonate | up-regulates activity
chemical activation
|
GABA-A (a1-b1-g2) receptor |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-264920 |
|
|
Homo sapiens |
Neuron |
| pmid |
sentence |
| 26136660 |
The raise in the intracellular bicarbonate concentration may augment the depolarizing efflux of bicarbonate upon activation of GABAA receptors; however, both transporters also extrude chloride and thereby increase the gradient for a hyperpolarizing chloride current. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
GABA-A (a1-b1-g2) receptor | up-regulates quantity
relocalization
|
chloride |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-263810 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18790874 |
GABAA receptors (GABAA-Rs) are the major inhibitory receptors in the central nervous system (CNS). |Mammalian GABAA-Rs are all anion-selective channels. Increased chloride permeability generally reduces neuronal excitability (inhibition) |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | GABAergic synapse |
| + |
GABA-A (a1-b1-g2) receptor | down-regulates
|
CRHR1 |
0.249 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-268600 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 33536967 |
OT inhibits corticotropin-releasing factor (CRF) mRNA expression at the hypothalamus, resulting in antistress and anti-anxiety effects| It has been demonstrated that the inhibitory effect of OT on CRF mRNA expression is not a direct one on CRF neurons. GABAergic neurons are present in the surroundings of the PVN (peri-PVN). These GABA-projecting neurons into the PVN inhibits CRF expression via GABAA receptors |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Hypothalamus |
3.0
GABA-A (a1-b1-g2) receptor