GABA Receptor Modulator

TET-13 is a positive allosteric modulator of GABA_A receptor with an EC₅₀ of 5.65 μM, lower than that of Etomidate (EC₅₀: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED₅₀: 0.48 mg/kg and 0.69 mg/kg, respectively).

Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.

MmTx1 toxin (Micrurotoxin 1) is an allosteric GABA_A receptor modulator that increases GABA_A receptor susceptibility to agonist.

GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.

TG 41 is positive modulator of GABAA receptor. TG 41 enhances the binding both of GABA and of Flunitrazepam to rat cerebral cortical membranes.

Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form.

Californidine perchlorate is an orally active γ-aminobutyric acid (GABA) receptor and serotonin receptor modulator. Californidine perchlorate enhances GABA-mediated chloride influx and inhibits cytochrome P450 enzymes. Californidine perchlorate is promising for research of anxiety.

ZL006-05 is an orally active, brain-penetrant nNOS–PSD-95 and α2-containing GABA_A dual-target inhibitor. ZL006-05 blocks the nNOS-PSD-95 protein-protein interaction and selectively potentiatesα2-containing GABA_A receptors. ZL006-05 attenuates central sensitization and strengthens inhibitory GABAergic synaptic transmission. ZL006-05 can be used for the study of neuropathic pain, cancer pain, chemotherapy-induced peripheral neuropathic pain, ischemic stroke, poststroke depression and anxiety.

NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.

α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the GABA_A receptor, suitable for research into central nervous system (CNS) disorders.

GABAA receptor modulator-5 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC₅₀ of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modulator-5 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modulator-5 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression.

GABAA receptor modulator-11 (Compound 4) is a GABA_A receptor modulator. GABAA receptor modulator-11 inhibits anesthetic-induced desensitization of GABAA α1β3γ2 and α1β3 receptors, with IC₅₀ values of 5.1 μM and 3.1 μM, respectively. GABAA receptor modulator-11 can be used for research on central nervous system diseases.

Cimbuterol (Standard) is the analytical standard of Cimbuterol. This product is intended for research and analytical applications. Cimbuterol is a β-adrenergic receptor agonist.

CMPPE is a GABAB receptor positive allosteric modulator (PAM) that inhibits alcohol self-administration and reinstatement behavior in rats.

CGP 54626 is a GABAB receptor modulator, which is essential in the central and peripheral nervous systems. It is used as a tool to identify and characterize GABAB receptor agonists and antagonists, which will aid in the development of drugs targeting diseases related to these systems. This discovery involves purified GABAB receptors, receptor proteins and their encoding nucleic acids, facilitating the study of new members of the GABAB receptor family through DNA cloning technology and sequence-derived probes.

GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABA_AR negative allosteric modulator (NAM) with a K_i of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety.

GABAA receptor modulator-1 (9eey) is a GABAA receptor modulator that can be used in the study of central nervous system diseases.

5-Deoxykievitone, an isoflavanone found in Phaseolus species, is a GABA receptor modulator. 5-Deoxykievitone potentiates GABA-induced chloride current through α₁β₂γ_2s GABA_A receptors. 5-Deoxykievitone can be used for the research of epilepsy and anxiety.

Etazolate (hydrochloride) (Standard) is the analytical standard of Etazolate (hydrochloride). This product is intended for research and analytical applications. Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.

(S)-Padsevonil (Standard) is the analytical standard of (S)-Padsevonil (HY-109009A). This product is intended for research and analytical applications. (S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.