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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
102 Results for "
GABAA agonist
" in MedChemExpress (MCE) Product Catalog:
Products (102)
102 Results for "GABAA agonist" in MCE Product Catalog:
5
Category:
Natural Products Other disease Disease markers Metabolic Disease Endogenous metabolite Disease Research Fields
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4
4 Cited Publications
Synonyms: DHEA sulfate; Prasterone sulfate
Category:
Human Gut Microbiota Metabolites Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Steroids
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4
4 Cited Publications
Synonyms: DHEA sulfate sodium; Prasterone sulfate sodium
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Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
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4 Cited Publications
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L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).
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Clomethiazole hydrochloride is a potent and orally active GABAA agonist . Clomethiazole hydrochloride inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Clomethiazole hydrochloride is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
2
2 Cited Publications
Synonyms: Imidazolyl-4-acetic acid
Category:
Human Gut Microbiota Metabolites Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields
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2
2 Cited Publications
Synonyms: (-)-Valerenic Acid
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Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
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2 Cited Publications
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MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
1
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THIP (Gaboxadol) is a blood-brain barrier-penetrant, orally active selective GABAA receptor agonist. THIP exhibits EC50 values of 33 μM and 130 μM for α4β2δ and α4β1δ receptors, respectively. THIP activates extrasynaptic GABAA receptors to produce tonic inhibition and inhibits GABAergic interneurons to cause disinhibition. THIP is used in research on insomnia, sleep disorders, and addictive behaviors .
1
1 Cited Publications
Synonyms: Lu 02-030 hydrochloride; THIP hydrochloride
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Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC 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 .
1
1 Cited Publications
Cat. No.: HY-19945
CAS No.: 220551-92-8
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DAA1106 is a peripheral benzodiazepine receptor (PBR) agonist that is permeable to the blood-brain barrier, but has no affinity for GABAA receptors.
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(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
1 Cited Publications
Cat. No.: HY-113416R
CAS No.: 651-48-9
Synonyms: DHEA sulfate (Standard); Prasterone sulfate (Standard)
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Isonipecotic acid is a GABAA receptor partial agonist .
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Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .
Synonyms: RG-7816; RO-7017773
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Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction .
Synonyms: L-822179
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α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential .
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TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.
Synonyms: trans-4-Aminocrotonic acid
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TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
