GABA Receptor Modulator

GABA Receptor Modulators (87):

Cat. No.	Product Name	Effect	Purity

HY-108223

Necopidem	Modulator
Necopidem (Compound 6) is a GABA A receptor modulator. Necopidem can be used in research on neurological disorders such as anxiety.

HY-N0662

Amentoflavone	Modulator	99.66%
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.

HY-B0504

Creatinine	Modulator	99.92%
Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.

HY-B0504S

Creatinine-d₃	Modulator	99.90%
Creatinine-d₃ is a deuterium labeled Creatinine. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.

HY-113320

Etiocholanolone	Modulator	99.49%
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 GABA_A receptor than its enantiomer form.

HY-10233

Gaboxadol hydrochloride	Modulator	99.85%
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABA_A receptor and an antagonist of GABA_C receptors (IC₅₀=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED₅₀ value of 143 μM, a full agonist efficacy at α5 subunit (ED₅₀=28-129 μM) and a superagonist efficacy at α4β3δ (ED₅₀=6 μM). Gaboxadol hydrochloride is a non-opioid agent.

HY-B0504S2

Creatinine-d₅	Modulator	99.93%
Creatinine-d₅ is the deuterium labeled Creatinine. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.

HY-B0504R

Creatinine (Standard)	Modulator
Creatinine (Standard) is the analytical standard of Creatinine. This product is intended for research and analytical applications. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.

HY-B0799

Dihydroergotoxine mesylate	Modulator	99.61%
Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABA_A receptor associated Cl^- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABA_A receptor associated Cl^- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.

HY-19505

TPA-023B	Modulator	98.45%
TPA-023B is a high-affinity and orally active GABA_A receptor α2/α3 subtype (K_is of 0.73 nM/2 nM) partial agonist and a α1 subtype (K_i of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.

HY-105042

Selank	Modulator	99.58%
Selank (Selanc; TP-7) is a GABAA receptor modulator with anxiolytic activity. Selank allosterically modulates the specific binding of GABA to GABAA receptors and alters the affinity of endogenous ligands for these receptors. Selank reduces elevated anxiety levels, attenuates stress-induced exacerbation of anxiety, and produces a synergistic anxiolytic effect with diazepam. Selank can be used in the research of anxiety disorders.

HY-100936

Etazolate hydrochloride	Modulator	98.00%
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 (GABA_A) 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.

HY-121618

α-Thujone	Modulator	98.07%
α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC₅₀ for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and can cross the blood-brain barrier.

HY-B0504S1

Creatinine-¹³C	Modulator	99.93%
Creatinine-¹³C is the ¹³C-labeled Creatinine. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.

HY-N0449

Nordihydrocapsaicin	Modulator	99.82%
Nordihydrocapsaicin, an analog of Capsaicin (HY-10448), is an orally active compound with pungent properties and anti-cancer activities, which is found in fresh and processed peppers. Nordihydrocapsaicin can cause a burning sensation when consumed.

HY-153584

MRK-898	Modulator	99.48%
MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with K_i values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s).

HY-W009009

L-838417	Modulator	98.73%
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABA_A receptor and an antagonist at the α1, with binding K_i values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2. L-838417 has anti-anxiety activity.

HY-B1803A

Tracazolate hydrochloride	Modulator	99.24%
Tracazolate (ICI 136753) hydrochloride is a potent GABA_A receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC₅₀=13.2 μM), α1β3γ2 (EC₅₀=1.5 μM). Tracazolate hydrochloride has the potency (EC₅₀) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.

HY-N8852

6-Methoxyflavanone	Modulator	98.95%
6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABA_A receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABA_A receptors, and is relatively inactive on the α1β2 GABA_A receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain.

HY-19371

Lorediplon	Modulator	99.88%
Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.

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