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カタログ番号 | 製品名 | 別名 | ターゲット |
---|---|---|---|
T11349 | GABAA receptor agent 1 | GABA Receptor | |
GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor. | |||
T61668 | GABAA receptor agent 5 | ||
GABAA Receptor Agent 5 (compound 018) serves as a potent γ-GABAAR antagonist, possessing a Ki of 0.020 μM. This compound exhibits γ-GABAAR antagonist properties, yet it demonstrates low cellular membrane permeability [1]... | |||
T60842 | GABAA receptor agonist 1 | ||
GABAA receptor agonist 1 (compound 3e) is a potent agonist of GABAA receptor that binds at the GABA binding site of GABAA receptor to produce GABAergic effects. GABAA receptor agonist 1 has anti-depression activities in ... | |||
T60481 | GABAA receptor agent 4 | ||
GABAA receptor agent 4 (compound 1e) is a potent antagonist of γ-GABAAR with Ki of 0.18 µM. GABAA receptor agent 4 has immunomodulatory potential which was shown to efficiently rescue the inhibition of T cell proliferati... | |||
T60817 | GABAA receptor agent 6 | ||
GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with low cellular membrane permeability (Ki = 0.56 μM) [1]. | |||
T61625 | GABAA receptor agonist 2 | ||
GABAA receptor agonist 2 (compound 4c) is a highly potent GABAA receptor agonist which exhibits anti-depressive properties in classical mouse models of depression, such as the FST and TST. By binding to the GABA binding ... | |||
T61052 | GABAA receptor agent 7 | ||
GABAA receptor agent 7 (compoud 5c) has anticonvulsant activity both in vitro and in vivo with low neurotoxicity which can be used in epilepsy research. GABAA receptor agent 7 is a potent positive modulator of GABAA rece... | |||
T60826 | GABAA receptor agent 8 | ||
GABAA receptor agent 8 (compoud 5e) has the potential in epilepsy research. GABAA receptor agent 8 is a potent positive modulator of GABAA receptor with anticonvulsant activity both in vitro and in vivo as well as low ne... | |||
T62885 | GABAA receptor modulator-2 | ||
GABAA receptor modulator-2 (Compound 20) is a selective, orally active α5-GABAAR negative conformation modulator (Ki: 4.1 nM). gABAA receptor modulator-2 exhibits high metabolic stability and a good central nervous syste... | |||
T62426 | GABAA receptor agent 2 TFA | ||
GABAA receptor agent 2 TFA is a potent, high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptor). GABAA receptor agent 2 TFA has no ... | |||
T8887 | 2'MeO6MF | GABA Receptor | |
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.It offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response... | |||
T7165 | Basmisanil | RG1662,RO5186582 | GABA Receptor |
Basmisanil (RG1662) is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndro... | |||
T11277 | FG 7142 | ZK 39106,LSU-65 | GABA Receptor |
FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cereb... | |||
T7794 | Zuranolone | GABA Receptor | |
Zuranolone is an agonist of GABAA receptor. | |||
T17144 | TPA 023 | GABA Receptor | |
TPA 023 is an agonist of the GABAA α2/α3 subtype-selective (Ki: 0.19-0.41 nM). | |||
T23339 | SCS | GABA Receptor | |
SCS is a GABAA receptor antagonist. | |||
T7622 | Gabazine | SR95531 | GABA Receptor |
Gabazine (SR95531) is an antagonist of GABAA receptors (Ki : 74-150 nM) | |||
TQ0151 | L-655708 | GABA Receptor | |
T3644 | U93631 | GABA Receptor | |
GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude... | |||
T11061 | DMCM hydrochloride | GABA Receptor | |
DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA αxβ3γ2 receptor subtypes. For α1, α2, α3, and α5 receptors, their Kis were 10 ... | |||
T22655 | CGS 20625 | Others | |
partial agonist for the benzodiazepine binding site of the GABAA receptor | |||
T28479 | PZ-II-029 | PZ-II029,PZ II-029,PZII-029,PZII029,PZ II029 | GABA Receptor |
PZ-II-029 is a modulator of α6β3γ2-selective GABAA channel. | |||
TQ0040 | ONO-8590580 | CS-2894 | GABA Receptor |
ONO-8590580 (CS-2894) is a negative allosteric modulator of GABAA α5. | |||
T35336 | Furosemide sodium | Frusemide Sodium,Lasix | Na-K-Cl cotransporter |
Furosemide sodium (Frusemide Sodium) is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity ... | |||
T50048 | 4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one | Others | |
4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one is a benzodiazepine derivative. It is an orthosteric modulator of the GABAA receptor and selectively binds to the benzodiazepine site of the GABAA receptor. It h... | |||
T27838 | Lirequinil | RO413696,RO-413696,RO41-3696,RO 413696,Ro 41-3696,Ro-41-3696 | GABA Receptor |
Lirequinil (Ro 41-3696) is a small molecule GABAA receptor agonist used to study neurological disorders. | |||
T20657 | Muscimol HBr | Agarin hydrobromide,Muscimol Hydrobromide,Agarin HBr | GABA Receptor |
Muscimol HBr (Agarin HBr) is an agonist of GABAA receptor. | |||
T28303 | Pazinaclone | A-77000,DN-2327,DN2327,DN 2327,A 77000,A77000 | GABA Receptor |
Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity. | |||
T7793 | 6-(4-Methoxyphenyl)-3-pyridazinamine | GABA Receptor | |
6-(4-Methoxyphenyl)-3-pyridazinamine is a GABAA receptor antagonist | |||
T23104 | Ocinaplon | DOV 273547 | GABA Receptor |
Ocinaplon (DOV 273547) is a GABAA receptors modulator. | |||
T8568 | Suritozole | MDL-26479 | GABA Receptor |
Suritozole (MDL-26479) is a negative modulator at the gamma-aminobutyric acidA (GABAA) receptor | |||
T19418L | Methionine | D-Methionine,MRX-1024 | Endogenous Metabolite |
Methionine (D-Methionine) (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation. | |||
T5375 | Loreclezole | GABA Receptor | |
Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors. | |||
TNU0685 | Dipropofol | 4,4-Bis(2,6-di-isopropylphenol) | GABA Receptor |
Dipropofol (4,4-Bis(2,6-di-isopropylphenol)) is a small molecule GABAA receptor agonist that can be used to study epilepsy. | |||
T22348 | Isonipecotic acid | 4-Piperidinecarboxylic acid,Hexahydroisonicotinic acid,4-Carboxypiperidine | GABA Receptor |
Isonipecotic acid (4-Piperidinecarboxylic acid) is a heterocyclic compound. Isonipecotic acid mainly characterized as a GABAA receptor partial agonist. | |||
T34146 | Propanidid | FBA 1420,Epontol,Sombrevin,Fabontal,Fabantol | GABA Receptor |
Propanidid (Sombrevin) is a gamma-aminobutyric acid type A receptor (GABAA) agonist and a fast-acting intravenous anesthetic that lowers arterial blood pressure. | |||
T11684 | Isoguvacine hydrochloride | 1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride | GABA Receptor |
Isoguvacine hydrochloride (1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride) is a GABA receptor agonist. Isoguvacine hydrochloride binds to rat synaptic cortical membranes and activates α1β2γ2S, α2β2γ2S, α3β2γ2... | |||
TQ0023 | Lorediplon | GABA Receptor | |
Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep. | |||
T24381 | L-822179 | L822179,L 822,179,L 822179,L822,179,L-822,179 | GABA Receptor |
L-822179 (α5IA) is a selective inverse agonist for the Α5 subtype of GABAA receptor with higher intrinsic activity at the A5 subtype than other drugs. | |||
T23466 | TP003 | GABA Receptor | |
TP003 is a novel non-selective GABAA receptor benzodiazepine site agonist with affinity for α1β2gam2, α2β3gam2, α3β3gam2, α5β2gam2, EC50 of 20.3, 10.6, 3.24, 5.64 nM, respectively. TP003 has antianxiety and partial antic... | |||
T23470 | Tracazolate hydrochloride | Tracazolate (hydrochloride) | GABA Receptor |
Tracazolate hydrochloride (Tracazolate (hydrochloride)) is a modulator of the GABAA receptor with anxiolytic and anticonvulsant activity. Tracazolate hydrochloride potentiates α1β1γ2s and α1β3γ2 with EC50s of 13.2 μM and... | |||
T22301 | L-838417 D9 | CTP354,CTP354 (C-21191),C-21191 | GABA Receptor |
L-838417 D9 (C-21191) is a novel deuterated subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1]. | |||
T8572 | CL 218872 | GABA Receptor | |
CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 nM for α1, α2, α3, α4, α5 and α6-subunit containing receptor... | |||
T15775 | Lotilaner | GABA Receptor , Parasite | |
Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA receptor). It also has no effect on a dog GABAA receptor. | |||
T23444 | TCS 1105 | N-(4-fluorobenzyl)-2-(1H-indol-3-yl)-2-oxoacetamide | Others |
TCS 1105 is a GABAA benzodiazepine receptor (BZR) ligand. TCS 1105 blocks Sema3A induced axonal growth cones collapse. TCS 1105 reduces anxiety-like behavior and enhances offensive behavior and social dominance in mice. | |||
T12492 | Pivagabine | CXB-722 | GABA Receptor |
Pivagabine (CXB-722), a hydrophobic 4-aminobutyric acid derivative, exhibits neuromodulatory activity and successfully penetrates the blood-brain barrier in rats. It counteracts the impact of foot shock on GABAA receptor... | |||
T26834 | BL-1020 Mesylate | CYP-1020 Mesylate | Dopamine Receptor , GABA Receptor |
BL-1020 Mesylate (CYP-1020 Mesylate) is an orally available GABA A receptor agonist and D2 antagonist that decreases dopamine activity and enhances GABAA activity.BL-1020 Mesylate has been used in the study of schizophre... | |||
T14983 | Clomethiazole | Distraneurin,Chlormethiazole,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE | P450 , GABA Receptor |
Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: C... | |||
T4993 | Afloqualone | HQ-495 | GABA Receptor |
Afloqualone (HQ-495) is a agonist of GABA Receptor . Target: GABA Receptor in vitro: Afloqualone is a quinazolinone family GABAergic drug. It has sedative and muscle-relaxant effects, resulting from its agonist activity ... | |||
T16489 | Darigabat | CVL-865,PF-6372865,PF-06372865 | GABA Receptor |
Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2... |
カタログ番号 | 製品名 | 別名 | ターゲット |
---|---|---|---|
T4S1999 | Valepotriate | Valtrate | Apoptosis , HIV Protease |
Valepotriate (Valtrate) fraction can have sedative effects and affect behavioral parameters related to recognition memory. Valepotriates, a new class of cytotoxic and antitumor agents, they are very potent cytotoxic agen... | |||
T5S1882 | Songorine | Napellonine,Zongorine,Bullatine G | Others , GABA Receptor |
Songorine (Napellonine) shows favorable anti-tumor activity in preliminary pharmacological verification trials including cell proliferation and molecular docking assays. | |||
T2S1464 | Thiocolchicoside | Thiocolchicine 2-glucoside analog,Coltramyl | Others , GABA Receptor |
Thiocolchicoside (Thiocolchicine 2-glucoside analog) (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABAA receptor antagonist and also glycine rece... | |||
TN1325 | (2S)-6-Prenylnaringenin | 6-Prenylnaringenin,6-PN | GABA Receptor |
(2S)-6-Prenylnaringenin (6-Prenylnaringenin) is an isomer of the potent phytoestrogen, 8-prenylnaringenin. (2S)-6-Prenylnaringenin is the most potent compound in the forebrain and acts as a positive allosteric modulator ... | |||
T2850 | Bicuculline | (+)-Bicuculline,d-Bicuculline | GABA Receptor |
Bicuculline ((+)-Bicuculline) is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungos... | |||
T8268 | 6,2'-Dihydroxyflavone | GABA Receptor | |
6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor. | |||
T3S2100 | (-)-Securinine | Securinine | GABA Receptor |
(-)-Securinine (Securinine) is plant-derived alkaloid and also a GABAA receptor antagonist. | |||
T16535 | Picrotoxinin | Chloride channel , GABA Receptor | |
Picrotoxinin is a blocker of chloride channel and a noncompetitive antagonist of GABAA with an IC50 of 1.15 μM for α1β2γ2L GABAA. Picrotoxinin shows convulsant properties. | |||
TN1202 | (-)-α-Pinene | (1S)-(-)-Alpha-Pinene | Virus Protease , GABA Receptor , Endogenous Metabolite , Antibacterial |
(-)-α-Pinene ((1S)-(-)-Alpha-Pinene) enhances the quantity of NREMS without affecting the intensity of NREMS by prolonging GABAergic synaptic transmission, acting as a partial modulator of GABAA-BZD receptors and directl... | |||
TN6773 | Acetoxyvalerensre | acetylvalerenolic acid | GABA Receptor |
Acetoxyvalerensre (acetylvalerenolic acid) (acetylvalerenolic acid) is a derivative of valerenic acid, which is a a GABAA receptor modulator. | |||
T8036 | 6-Methylflavone | GABA Receptor | |
6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors. | |||
TQ0119 | Cirsimaritin | GABA Receptor | |
T3318 | Wogonoside | Glychionide B,Wogonin 7-O-glucuronide,Oroxindin | GABA Receptor , Autophagy |
Wogonoside (Wogonin 7-O-glucuronide) acts as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor. | |||
T2983 | 3,4,5-Trimethoxycinnamic acid | 3-(3,4,5-Trimethoxyphenyl)acrylic Acid,O-Methylsinapic acid | GABA Receptor , Endogenous Metabolite |
3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex. | |||
T8040 | Cholesterol myristate | Cholesteryl myristate,Cholesteryl tetradecanoate | Others , Potassium Channel , GABA Receptor , Endogenous Metabolite , AChR |
Cholesterol Myristate (Cholesteryl Myristate) is a natural steroid found in traditional Chinese medicine that interacts with various ion channels, including the GABAA receptor, nicotinic acetylcholine receptor, and the i... | |||
T8162 | Cannabidivarin | Cannabidivarin,GWP-42006,GWP42006,GWP 42006 | GABA Receptor |
Cannabidivarin (GWP42006) is a potent inhibitor against gamma 2 subunit of GABAA receptors. it may serve as a novel drug with definite control over childhood absence epilepsy. | |||
T4S1616 | Sanggenon D | Sanggenone D | NOS , COX , GABA Receptor |
Sanggenone D represents a new scaffold of positive GABAA receptor modulators, it also inhibits COX-2 activity (IC 50 = 73-100 μM). Sanggenone D has anti-inflammatory activity, it can inhibit NO production from lipopolysa... | |||
T3836 | Eudesmin | MAPK , S6 Kinase | |
Eudesmin shows antiinflammatory, neuritogenic, anticonvulsant and sedative effects, the mechanism of eudesmin may be related to up-regulation of GABAA and GAD65 expressions, and anti-apoptosis of neuron the in brain.50 m... | |||
T7033 | Rosmanol | Antioxidant , COX | |
Rosmanol has antioxidant activity, it can activate the antioxidant response element. Rosmanol has biphasic modulation of GABAA receptors, demonstrates CNS activity in mouse models of antinociception, antidepressant and a... | |||
T0508 | γ-Aminobutyric acid | Gamma-aminobutyric acid,4-Aminobutyric acid,GABA,4-Aminobutanoic acid,Piperidic acid | GABA Receptor , Endogenous Metabolite |
γ-Aminobutyric acid (4-Aminobutyric acid) is the most common inhibitory neurotransmitter in the central nervous system. | |||
T6S2227 | Spinosin | Flavoayamenin | Others |
1. Spinosin (Flavoayamenin) ameliorated memory impairment induced through AβO, the serotonergic neurotransmitter system, and these effects were regulated, in part, through neuroprotective activity via the anti-inflammato... | |||
TMS0418 | Dihydroergotoxine mesylate | Ergoloid mesylates | GABA Receptor |
Dihydroergotoxine mesylate (Ergoloid mesylates) is mainly used to improve symptoms and physical symptoms of mental degeneration related to aging. | |||
TCS0102 | Pulegone | (+)-Pulegone | Calcium Channel , Endogenous Metabolite , TRP/TRPV Channel |
1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect t... | |||
T5754 | Kavain | NF-κB , GABA Receptor | |
Kavain, a compound extracted from the Kava plant, Piper methysticum, is found to be involved in TNF-α expression in human and mouse cells via regulation of transcriptional factors such as NF-kB and LITAF. | |||
T8193 | α-Thujone | Thujone,ALPHA-(-)-THUJONE | Apoptosis , Reactive Oxygen Species , GABA Receptor , AChR , Parasite , Autophagy |
α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM. | |||
T3343 | 5-methoxyflavone | 5-methoxy-2-phenylchromen-4-one | DNA/RNA Synthesis |
5-methoxyflavone (5-methoxy-2-phenylchromen-4-one) is a naturally occurring, low molecular weight flavonoids compound that associated with a wide wariety of biological activities. | |||
T4590 | (+)-Kavain | Kavain,L-KAWAIN,(R)-KAWAIN | Calcium Channel , GABA Receptor , Sodium Channel , Monoamine Transporter |
(+)-Kavain ((R)-KAWAIN) is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B. | |||
T3403 | Glabridin | Q-100692,KB-289522,LS-176045 | Reactive Oxygen Species , Tyrosinase , GABA Receptor , Antibacterial , PPAR |
Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on... | |||
T2979 | DL-Menthol | Hexahydrothymol,(±)-Menthol | GABA Receptor , AChE |
DL-Menthol ((±)-Menthol) is a racemic mixture of the monoterpene alcohols (–)-menthol and (+)-menthod, which have been found in Cannabis. (–)-Menthol is more common than (+)-menthol in nature and exhibits analgesic, anti... | |||
T80776 | Withasomniferolide A | ||
Withasomniferolide A, a withanolide extracted from the roots of Withania somnifera, has been identified as a positive activator of the GABAA receptor, isolated using a methanol extract [1]. | |||
TN5608 | Paspalinine | ||
Paspalinine can inhibit binding of [125I]charybdotoxin (ChTX) to maxi-K channels in bovine aortic smooth muscle sarcolemmal membranes. Paspalinine shows tremorgenic action, which may be due in part to their inhibition of... | |||
TN3868 | Dihydroxyaflavinine | GABA Receptor | |
Dihydroxyaflavinine is a fungal toxin, it inhibits non-competitively GABAA receptor channel expressed in Xenopus oocytes.Dihydroxyaflavinine shows oral toxicity to the fall armyworm (Spodoptera frugiperda) and corn earwo... | |||
TN1842 | Kushenol I | GABA Receptor , Antifection | |
Kushenol I is a GABAA receptor modulator, it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).Kushenol I is shown to be active against the plant pathogenic fungus Cladosporium cucumeri... | |||
TN4322 | Isopulegol | ATPase , Potassium Channel , GABA Receptor | |
Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly related to positive modulation of benzodiazepine-sensitive GA... | |||
T0051 | Urethane | Ethyl carbamate,Ethylurethane,Carbamic acid ethyl ester | Chloride channel , GABA Receptor , Antibacterial , GluR , NMDAR , AChR , Parasite |
Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes. | |||
TN3351 | Aflatrem | GABA Receptor | |
Aflatrem is a tremorgenic mycotoxin with acute neurotoxic effects, a single low dose of aflatrem is able to induce degeneration of neuronal processes in hippocampal neurotransmitter systems. Aflatrem potentiates the gamm... | |||
T75557 | Withasomniferolide B | ||
Withasomniferolide B, a withanolide, can be obtained through isolation from a methanol extract of Withania somnifera roots, which acts as a positive activator of the GABA(A) receptor [1]. |
カタログ番号 | 製品名 | Species | Expression System |
---|---|---|---|
TMPY-03991 | DBI Protein, Human, Recombinant (His) | Human | E. coli |
The diazepam binding inhibitor (DBI), alternatively known as the acyl-CoA binding protein (ACBP), is involved in multiple biological actions. The polypeptide binds to the peripheral, or mitochondrial, benzodiazepine rece... |