Agonists

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B5399 (±)-Baclofen ≥98% (TLC), solid GABAB receptor agonist; skeletal muscle relaxant; antispastic agent.
T1694 (E)-4-Amino-2-butenoic acid  
A4147 3-Amino-1-propanesulfonic acid sodium salt ≥98% GABAA receptor agonist.
268615 3-Aminopropylphosphonic acid 98% GABAB receptor agonist; antagonist of basal prolactin secretion.
D1444   6,2′-Dihydroxyflavone ≥98% (HPLC), powder 6,2′-Dihydroxyflavone is a partial inverse agonist at GABAA receptors with α-subunit selectivity.
A6981 Acamprosate calcium ≥98% (HPLC), powder Acamprosate calcium is a GABA γ-aminobutyric acid agonist.
SML0376 CGS 9895 ≥98% (HPLC) CGS 9895 is a GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors. CGS 9895 is the only known compound that can specifically enhance GABA-induced currents in ab subunit containing receptors, and acts at the extracellular a1+b3- subunit interface.
SML1584 CMPPE ≥95% (HPLC) CMPPE is a GABAB receptor positive allosteric modulator (PAM). GABAB receptor positive allosteric modulators have potential for treatment of many neuro-psychiatric disorders as well as drug dependence and seizures. The receptor is a GPCR expressed throughout the CNS; it acts as both an auto-receptor and heteroreceptor to mudulate GABA release and regulate K+ channels and Ca++ channels. CMPPE has the highest hypoactivity/anticonvulsant ratio.
C1240 Chlormethiazole hydrochloride ≥98% (HPLC), powder GABAA agonist; glycine receptor modulator.
D0446 DS1 ≥98% (HPLC) δ-GABAA receptors are emerging as an important pharmacological target. DS1 potently (low nM) enhances GABA-evoked currents mediated by α4β3δ receptors. It had little effect on GABA responses mediated by α4β3γ2 receptors. At similar concentrations DS1 directly activates this receptor and is the most potent known agonist of α4β3δ receptors. This compound has an opportunity to be become an agonist golden stardard for δ-GABAA receptors.
DS1 potently (low nM) enhances GABA-evoked currents mediated by GABAA α4β3δ receptor subtype. At similar concentrations, it acts as a direct agonist at this receptor and is the most potent agonist known. It has little effect on GABA responses mediated by α4β3γ2 receptors.
E6530 Etomidate >98% (HPLC), powder Etomidate is a general anesthetic; potentiates GABAA transmission. The possible neuroprotective effect of etomidate against streptozotocin-induced (STZ-induced) hyperglycaemia were investigated in the rat brain and spinal cord. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage
SML1520 GS39783 ≥98% (HPLC) GS39783 is a positive allosteric modulator (PAM) of GABA-B receptors. GABAB receptor positive allosteric modulators have potential for treatment of many neuro-psychiatric disorders as well as drug dependence and seizures. The receptor is a GPCR expressed throughout the CNS; it acts as both an auto-receptor and heteroreceptor to modulate GABA release and regulate K+ channels and Ca++ channels. GS39783 has been shown to inhibit alcohol self-administration and to have an antipsychotic-like effect in animal models of addiction and schizophrenia, respectively.
T101 Gaboxadol hydrochloride solid, ≥98% (HPLC) GABAA receptor agonist.
G002 Isoguvacine hydrochloride solid GABAA receptor agonist.
SML0565 MK-0343 ≥98% (HPLC) MK-0343 (MRK-409) is a partial agonist for GABAA receptors with comparable Ki values for α1, α2, α3 and α5 containing receptors (0.2 – 0.4 nM). The compound has the greatest agonist activity against α3 receptors, and is brain penatrant, and displays anxiolytic activity in rodent and primate models.
G019   Muscimol hydrobromide ≥98% (HPLC), solid Muscimol hydrobromide is a GABAA receptor agonist.
M1523 Muscimol powder GABAA receptor agonist.
SML0647   Phenazepam ≥97% (HPLC) Phenazepam is the benzodiazepine that exhibit anticonvulsive, anxiolytic, sedative and hypnotic effects in humans and experimental animals. Phenazepam is an agonist of the γ-Aminobutyric acid A (GABAA)-benzodiazepine receptor chloride channel complex.
P9159 Piperidine-4-sulfonic acid GABAA receptor agonist.
G013 R(+)-Baclofen hydrochloride solid R(+)-Baclofen is a GABAB receptor agonist; more active enantiomer; skeletal muscle relaxant.
G014 S(−)-Baclofen hydrochloride ≥98% (HPLC), solid S(−)-Baclofen hydrochloride is a less active enantiomer of baclofen.
S7936 SB 205384 solid GABAA receptor modulator selective for the α3β2γ2 subunit combination.
SB 205384 is a selective and positive allosteric modulator of non-benzodiazepine site of the GABAA receptor.3 It affects the extrasynaptic GABAA receptors in rat cortical neurons4 and enhances the GABAergic transmission onto pro-opiomelanocortin neurons in mice.5
SML1476 Thiocolchicoside ≥98% (HPLC) Thiocolchicoside is a potent competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist with muscle relaxant, anti-inflammatory, and analgesic activity. Thiocolchicoside has also been found to suppress nuclear factor kappa B ligand (RANKL) activation of NF-KB resulting in suppression of osteoclastogenesis.
A2734 α5IA ≥98% (HPLC) α5IA is a selective inverse agonist for Α5 subtype of GABAA receptor with a higher intrinsic activity at the A5 subtype than other drugs. α5IA enhances cognition in laboratory animals without being proconvulsant or anxiogenic. α5IA acts as an "alcohol antagonist," markedly reducing the amnesic effect of alcohol and partially attenuating sedation, similar to Ro15-4513, but without the anxiogenic effect. α5IA offers promise as a tool to study cognitive disorders, memory function, and treatment of alcohol-related disorders.
SML0249 βCCt ≥98% (HPLC) βCCt has been characterized as an α1selective antagonist and benzodiazepine mixed agonist/antagonist.. A recent study found Ki values for the GABA-A subtypes were 0.72, 15, 18.9, 110.8, and >5,000 nM at five recombinant GABAA/BzR subtypes α1, α2, α3, α5, and α6 respectively. βCCt was a near ‘neutral’ antagonist (i.e., little or no efficacy) at all these 5 recombnant GABAA/BzR receptor subtypes. βCCt has been shown to reduce alcohol self-administration in alcohol preferring (P) and high alcohol drinking (HAD) rats.
A2129 γ-Aminobutyric acid ≥99% GABA (γ-Aminobutyric acid) is an amino acid that functions as an inhibitory neurotransmitter in the central nervous system and also functions as a neuromodulator in some peripheral tissues. It binds to GABAA receptor and inhibits the activity of signal-receiving neurons. The GABAA receptors are found to form a channel in the cell membranes of neurons. Upon binding of GABA, the receptor is activated to allow the passage of negatively charged molecules, such as chloride ions, into the cell. This results in lowering of excitability of the cell.
GABAergic neurons are involved in myorelaxation, anxiolytic treatment, sedation, and anaesthetics. GABA can also influence heart rate and blood pressure.
Major inhibitory neurotransmitter in brain; GABAA and GABAB receptor agonist; increases Cl conductance.