Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase[1][2][3].
Arbaclofen placarbil is a novel transported prodrug of the active R-isomer of baclofen. Baclofen is a racemic GABAB receptor agonist
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity[1][2].
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells[1][2][3].
AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
L-663581 (FG-8205) is an agonist of benzodiazepine receptor, acting as a partial agonist at GABA A receptor[1].
CGP11952 is a triazolyl-Benzaphenon resembling the benzodiazepines in its pharmacological action. CGP11952 is an experimental benzodiazepine derivative.
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research[1][2][3].
Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase.IC50 value:Target: GABA transaminaseClinical studies have shown that vigabatrin is superior to placebo in decreasing the frequency of infantile spasms. In tuberous sclerosis, vigabatrin may be considered the first-line treatment for IS. The mode of action is increasing concentrations of the inhibitory neurotransmitter GABA in the brain.A significant increase in seizure threshold was observed following systemic (i.p.) administration of high (600 or 1200 mg/kg) doses of vigabatrin. Bilateral microinjection of vigabatrin (10 μg) into either the anterior or posterior SNr also increased seizure threshold, but less markedly than systemic treatment.
CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC50 of 6 nM. CGP55845 hydrochloride can be used for neurological research[1][2].
NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site[1].
Remimazolam (CNS-7056) is a short-acting GABA(A) receptor agonist[1].
Inaperisone is a centrally acting muscle relaxant. Inaperisone inhibits the micturition reflex by acting indirectly on GABAB receptors in the brainstem[1].
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy[1][2][3].
Alpha-Asarone is one of the main psychoactive compounds, and possesses an antidepressant-like activity in mice.IC50 value:Target:In vitro: The results indicated that α-asarone significantly attenuated the LPS-stimulated increase in neuroinflammatory responses and suppressed pro-inflammatory cytokine production in BV-2 cells. Mechanistic study revealed that α-asarone?inhibited the LPS-stimulated activation via regulation of nuclear factor kappa-B by blocking degradation of inhibitor kappa B-alpha signaling in BV-2 microglial cells. [2]In vivo: The present results reveal that the acute treatment of α-asarone elicited biphasic responses on immobility such that the duration of the immobility time is significantly reduced at lower doses (15 and 20 mg/kg, i.p.) but increased at higher doses (50 and 100 mg/kg, i.p.) in the TST. Besides, α-asarone at higher doses (50 and 100 mg/kg, i.p.) significantly decreased the spontaneous locomotor activity.[1]
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[1].
17-PA is a selective antagonist of neurosteroid potentiation and direct gating of GABAA receptors[1].
Homocarnosine is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects[1].Homocarnosine has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation[2].
CGP 64213 is a GABAb receptor agonist.
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties[1][2][3].
CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC50 of 32 μM. CGP 36742 is useful in treatment of depression[1].
Carburazepam is a drug which derives from benzodiazepine. Benzodiazepines (BZD, BZs) are a class of psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring.
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors[1].
Chlormezanone resembles benzodiazepine. The action of Chlormezanone is similar to benzodiazepine-type agents. Chlormezanone is used as an anxiolytic and a muscle relaxant.
CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures[1].
L-DABA (L-2,4-Diaminobutyric acid) hydrobromide is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
MIDD0301 is a potent, positive allosteric, α5β3γ2 selective, GABAA receptor (GABAAR) ligand with EC50 of 17 nM, shows no significant binding at the peripheral GABAAR at 10 uM; causes amplification of GABA induced current mediated by α1-3,5β3γ2 GABAARs in the presence of MIDD0301 in automated patch clamp test; relaxes airway smooth muscle at single micromolar concentrations as demonstrated with ex vivo guinea pig tracheal rings, also attenuates airway hyperresponsiveness (AHR) in an ovalbumin murine model of asthma by oral administration, with low brain distribution; reduces lung cytokine expression of IL-17A, IL-4, and TNF-α, as wells as the number of CD4+ T cells.
N-Arachidonoyl-GABA is one member of a new class of lipoamino acids related to anandamide identified in bovine brain. N-Arachidonoyl-GABA displays analgesic activity[1].
Ru-32514 is an agonist of benzodiazepine receptor.