GABA Receptor Agonist

DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic agent (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin.

Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR.

Ginsenoside Rc (Standard) is the analytical standard of Ginsenoside Rc. This product is intended for research and analytical applications. Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.

Bamaluzole is a GABA receptor agonist extracted from patent WO 2012064642 A1.

Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.

Bodipy TMR-X muscimol is a Bodipy labeled Muscimol (HY-N2313) (Ex=543 nm, Em=572 nm). Muscimol is a GABAA agonist. Bodipy TMR-X muscimol can be used for imaging the spread of reversible brain inactivations.

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABA_A receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABA_A receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.

T-2000 (DMMDPB) is an orally active GABA receptor agonist with anticonvulsant activities.

Suriclone (RP31264) is a GABA receptor agonist. Suriclone is an anxiolytic agent with a high affinity for the benzodiazepine receptors. Suriclone has oral activity.

CGS-9896 is an orally active benzodiazepine receptor agonist that targets the benzodiazepine receptor allosterically coupled to the GABA_A receptor and chloride ion carrier channel. The K_i value of CGS-9896 for benzodiazepine receptors in rats is 0.83 nM. CGS-9896 inhibits pentylenetetrazol-induced convulsions in mice and exerts an anticonvulsant effect.

Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid (HY-113413). This product is intended for research and analytical applications. Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABA_A receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity.

GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression.

NAP-1 is a compound with agent that can suppress or relieve pain. effects. NAP-1 enhances the inhibitory current by binding to a specific site of GABAaR, resulting in a narcotic effect. NAP-1 can be used in research to develop clinical agent that can suppress or relieve pain.

Fletazepam is a benzodiazepine derivative with sedative, anxiolytic and muscle relaxant effects. Fletazepam can be utilized in neurological research.

Timelotem (KC-7507 free base) is a representative of a class of 1, 2-cyclo1, 4-benzodiazepines. Timelotem shows significant antipsychotic properties. Timelotem produces sedative, anti-anxiety and anti-convulsant effects by enhancing the action of the neurotransmitter gamma-aminobutyric acid (GABA). Timelotem can be used in studies of schizophrenia and other mental disorders.

(S)-Baclofen hydrochloride is a GABAB receptor agonist that crosses the blood-brain barrier and is orally active, with IC₅₀ values ​​of 1.77 μM for GABAB and 1564 μM for GABAA. (S)-Baclofen hydrochloride can be used in research on muscle disorders such as spasticity.

Ro 17-1812 is a benzodiazepine receptor partial agonist with anticonvulsant effect.

SKF 97541 (CGP 35024) is a potent and selective GABA_B agonist that can induce hyperpotential. SKF 97541 has antiepileptic activity.

Anxiolytic/nonsedative agent-1 (compound 2b) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with K_is of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.

CGP44532 is a GABA_B receptor agonist with a pEC₅₀ (geometric mean of the half-maximal effective concentration) value of 5.63 μM.