Search Result
Results for "
Anticonvulsant effect
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-101392
-
Harmane
1 Publications Verification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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-
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- HY-B0184
-
|
W-554; ADD-03055
|
iGluR
|
Neurological Disease
|
|
Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).
|
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- HY-B1302
-
|
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P-glycoprotein
PARP
Caspase
Apoptosis
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures .
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- HY-W090292
-
|
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Drug Intermediate
|
Neurological Disease
|
|
Olivetolic acid is a biosynthetic precursor of cannabinol acid (CBGA). Olivetolic acid exhibits a modest anticonvulsant effect in a mouse model of Dravet syndrome. Olivetolic acid can be used for the study of convulsion .
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-
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- HY-B1199
-
-
-
- HY-103234A
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research .
|
-
-
- HY-P3960
-
|
|
Thyroid Hormone Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mouse brain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS .
|
-
-
- HY-103230
-
-
-
- HY-136591
-
|
|
Drug Metabolite
|
Neurological Disease
Cancer
|
|
Demoxepam is a major metabolite of Chlordiazepoxide. Demoxepam exhibits cytotoxicity activity against cancer cell lines. Demoxepam has anticonvulsant and anxiolytic effects. Demoxepam has an inhibitory effect on in vitro [ 3H]tryptophan binding to rat hepatic nuclei .
|
-
-
- HY-N8303
-
|
|
ERK
PAK
|
Neurological Disease
Inflammation/Immunology
|
|
Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects .
|
-
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- HY-123335A
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
L-796778 acetate is a selective agonist of the sst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796778 acetate is a partial agonist that inhibits Forskolin (HY-15371)-stimulated cAMP production with an IC50 value of 18 nM. L-796778 acetate has anticonvulsant effect .
|
-
-
- HY-103506
-
|
NO-711 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC50 values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity .
|
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-
- HY-101392A
-
|
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
-
- HY-P1132A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galanin (1-29)(rat, mouse) TFA is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3, respectively. Anticonvulsant effect .
|
-
-
- HY-141795
-
|
Co 134444
|
Drug Derivative
|
Neurological Disease
|
|
Posovolone (Co 134444) is an orally active, neuroactive steroid. Posovolone has anticonvulsant and anxiolytic-like activity as well as ataxic effects .
|
-
-
- HY-N4267
-
|
|
Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
|
-
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- HY-P1132
-
-
-
- HY-116944
-
-
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- HY-B0184A
-
|
W-554 hydrate; ADD-03055 hydrate
|
iGluR
|
Neurological Disease
|
|
Felbamate hydrate (W-554 hydrate) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .
|
-
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- HY-177986
-
|
|
Drug Derivative
|
Neurological Disease
|
|
NCR 631 is a 3-HAO inhibitor and 3-hydroxyanthranilic acid (HY-W001171) analogue. NCR-631 has anticonvulsant properties. NCR-631shows a concentration-dependent protective effect against the anoxia .
|
-
-
- HY-W013378S
-
|
|
Endogenous Metabolite
Isotope-Labeled Compounds
|
Others
|
|
Carbamazepine 10,11 epoxide-d2 is the deuterium labeled Carbamazepine 10,11 epoxide . Carbamazepine 10,11-epoxide is an orally active metabolite of Carbamazepine (HY-B0246). Carbamazepine has anticonvulsant effect. Carbamazepine can be used for the research of seizures .
|
-
-
- HY-176065
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Nav1.2-IN-1 (compound 5i), a 3-(1,2,3,6-tetrahydropyridine)-4-azaindole derivative, is a potent and selective Nav1.2 inhibitor. Nav1.2-IN-1 induces a reduction in the peak amplitude of Nav1.2 currents with an IC50 value of 7.79 μM. Nav1.2-IN-1 exhibits antiepileptic activity. Nav1.2-IN-1 shows high anticonvulsant effect and low neurotoxicity in subcutaneous Pentetrazole (sc-PTZ)-induced epilepsy mode .
|
-
-
- HY-133773
-
-
-
- HY-125555
-
-
-
- HY-U00315S
-
|
Gidasepam-d5; Hidazepam-d5; Hydazepam-d5
|
GABA Receptor
|
Neurological Disease
|
|
Gidazepam-d5 is a deuterium labeled Gidazepam. Gidazepam is an agonist of GABA receptor channels (GABA RCs), and has anticonvulsant effect .
|
-
-
- HY-107323
-
|
QM 6008; Thiadipone; Tiadipone
|
GABA Receptor
|
Neurological Disease
|
|
Bentazepam (Thiadipone) is a compound with short-action anxiolytic effect. Bentazepam shows anticonvulsant and sedative properties. Bentazepam can be used for the research of depressive disorder and anxiety .
|
-
-
- HY-107323A
-
|
QM 6008 hydrochloride; Thiadipone hydrochloride; Tiadipone hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Bentazepam (QM 6008, Thiadipone) hydrocholide is a compound with short-action anxiolytic effect. Bentazepam hydrocholide shows anticonvulsant and sedative properties. Bentazepam hydrocholide can be used for the research of depressive disorder and anxiety .
|
-
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- HY-B0184S1
-
|
Felbamyl-d5; Felbatol-d5; Taloxa-d5
|
iGluR
|
Neurological Disease
|
|
Felbamate-d5 is the deuterium labeled Felbamate . Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .
|
-
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- HY-B0184R
-
|
W-554 (Standard); ADD-03055 (Standard)
|
Reference Standards
iGluR
|
Neurological Disease
|
|
Felbamate (Standard) is the analytical standard of Felbamate. This product is intended for research and analytical applications. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).
|
-
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- HY-B1199A
-
|
|
Monoamine Oxidase
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Nialamide hydrochloride is a non-selective monoamine oxidase (MAO) inhibitor. Nialamide hydrochloride inhibits MAO and regulates ROS production. Nialamide hydrochloride induces hyperkinesis in animals, enhances the anticonvulsant effect of Diphenylhydantoin in mice, increases rectal temperature, and enhances the pressor effect of Norepinephrine. Nialamide hydrochloride can be used in the research of depression, inflammatory diseases, neurodegenerative diseases, and hypertension .
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- HY-B0184S
-
|
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iGluR
|
Neurological Disease
|
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Felbamate-d4 (W-554-d4) is the deuterium labeled Felbamate. Felbamate (W-554) is a potent anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).
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- HY-W097106
-
|
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Drug Isomer
|
Neurological Disease
|
|
(S)-3-N-Cbz-Amino-succinimide (Compound 1d) is an antiepileptic agent that can inhibit pentylenetetrazole (PTZ) and maximal electroshock (MES)-induced tonic convulsions in mice .
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- HY-147377
-
-
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- HY-103234
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research .
|
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- HY-103234B
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 hydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 hydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 hydrochloride can be used in Parkinson's disease research .
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- HY-177302
-
|
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mGluR
|
Neurological Disease
|
|
mGluR2 modulator 6 (Compound 25-a) is a mGluR2 modulator. mGluR2 modulator 6 has anticonvulsant activity in the 6Hz epilepsy model, and the effect is better when combined with Levetiracetam (HY-B0106). mGluR2 modulator 6 can be used in the research of epilepsy .
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-
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- HY-103234AR
-
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Reference Standards
iGluR
|
Neurological Disease
|
|
GYKI 52466 (dihydrochloride) (Standard) is the analytical standard of GYKI 52466 (dihydrochloride). This product is intended for research and analytical applications. GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research .
|
-
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- HY-W013378S2
-
|
|
Endogenous Metabolite
|
Others
|
|
Carbamazepine 10,11-epoxide- 13C,d2 is the deuterium labeled Carbamazepine 10,11-epoxide-C13. Carbamazepine 10,11-epoxide-C13 is a 13C-labled Carbamazepine 10,11-epoxide. Carbamazepine 10,11-epoxide is an orally active metabolite of Carbamazepine (HY-B0246). Carbamazepine has anticonvulsant effect. Carbamazepine can be used for the research of seizures .
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-
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- HY-17032
-
|
(rac)-AS1069562 free base; YM-08054 free base
|
Endogenous Metabolite
|
Neurological Disease
|
|
Indeloxazine ((rac)-AS1069562 free base) is a brain active compound with anti-amnesic activity. Indeloxazine significantly prolonged the step latency in senescence accelerated mice (SAM-P/8/Ta), indicating that it has a promoting effect on brain function. Indeloxazine has a broader pharmacology than piracetam and exhibits stronger anti-amnesic activity. Indeloxazine has also been used as an anticonvulsant compound, further supporting its potential use in neuroprotection and behavioral improvement .
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- HY-W777360
-
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Isotope-Labeled Compounds
Adrenergic Receptor
Monoamine Oxidase
nAChR
Opioid Receptor
Imidazoline Receptor
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Harman- 13C2, 15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
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- HY-105340
-
|
|
iGluR
|
Neurological Disease
|
|
MDL 27266 is an orally active NMDA receptor antagonist with neuroprotective effect. MDL 27266 is a broad-spectrum anticonvulsant agent .
|
-
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- HY-103230R
-
|
|
Reference Standards
iGluR
|
Neurological Disease
|
|
IEM-1460 (Standard) is the analytical standard of IEM-1460 (HY-103230). This product is intended for research and analytical applications. IEM-1460 blocks both AMPA and NMDA glutamate receptor with anticonvulsant effect in vivo .
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-
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- HY-182548
-
|
|
GABA Receptor
Sodium Channel
iGluR
|
Cardiovascular Disease
Neurological Disease
|
|
BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABAA receptor (GABAA receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na + channels (Ki = 350 μM) and NMDA receptors (NMDA receptor) (IC50 = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine .
|
-
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- HY-136591R
-
|
|
Drug Metabolite
Reference Standards
|
Neurological Disease
Cancer
|
|
Demoxepam (Standard) is the analytical standard of Demoxepam. This product is intended for research and analytical applications. Demoxepam is a major metabolite of Chlordiazepoxide. Demoxepam exhibits cytotoxicity activity against cancer cell lines. Demoxepam has anticonvulsant and anxiolytic effects. Demoxepam has an inhibitory effect on in vitro [ 3H]tryptophan binding to rat hepatic nuclei .
|
-
-
- HY-N16538
-
|
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Drug Derivative
|
Cardiovascular Disease
Neurological Disease
|
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4-(Acetoxymethyl)phenyl glucoside is a type of gastrodin derivative that can cross the blood-brain barrier. 4-(Acetoxymethyl)phenyl glucoside exhibits sedative, anticonvulsant and analgesic effects in mouse models. 4-(Acetoxymethyl)phenyl glucoside can be used for research on senile cardiovascular and cerebrovascular diseases as well as brain nerve disorders .
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-
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- HY-103566R
-
|
|
Reference Standards
mGluR
EGFR
p38 MAPK
Apoptosis
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
LY456236 (Standard) is the analytical standard of LY456236 (HY-103566). This product is intended for research and analytical applications. LY456236 is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC50 of 0.145 μM. LY456236 can also inhibit EGFR, with an IC50 of 0.918 μM. LY456236 has anticonvulsant effects and blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 can be used in epilepsy research .
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- HY-W115674
-
|
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P-glycoprotein
PARP
Caspase
Apoptosis
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Quinidine hydrochloride is an orally active antiarrhythmic agent. Quinidine hydrochloride reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride can be used in studies related to uterine sarcoma and seizures .
|
-
-
- HY-15080
-
|
LY 293606
|
iGluR
|
Cardiovascular Disease
Neurological Disease
|
|
GYKI 53405 is a non-competitive, orally active AMPA receptor antagonist. GYKI 53405 shows no significant binding affinity for GABAA, GABAB or benzodiazepine receptors. GYKI 53405 increases self-grooming behavior, induces wet dog-like shakes, reduces spontaneous activity, produces anxiolytic-like behavior, reverses the anxiogenic effect induced by mCPP, inhibits locomotor activity, suppresses sound-induced and maximal electroshock-induced seizures, prolongs survival in global cerebral ischemia models, and exhibits sustained anticonvulsant effects at doses below the sedation threshold. GYKI 53405 can be used in research related to absence epilepsy, anxiety disorders and global cerebral ischemia .
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- HY-103506R
-
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NO-711 hydrochloride (Standard)
|
Reference Standards
GABA Receptor
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Neurological Disease
|
|
NNC-711 (Standard) is the analytical standard of NNC-711 (HY-103506). This product is intended for research and analytical applications. NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC50 values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity .
|
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- HY-W700834
-
|
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Isotope-Labeled Compounds
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Neurological Disease
Inflammation/Immunology
|
|
Harman-d3 is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3960
-
|
|
Thyroid Hormone Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mouse brain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS .
|
-
- HY-P1132A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galanin (1-29)(rat, mouse) TFA is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3, respectively. Anticonvulsant effect .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-101392
-
Harmane
1 Publications Verification
|
Alkaloids
other families
Pyridine Alkaloids
Plants
Indole Alkaloids
Source Classification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
|
Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
-
- HY-B1302
-
-
-
- HY-P3960
-
-
-
- HY-N8303
-
|
|
Flavonoids
Flavones
Rutaceae
Plants
Citrus reticulata Blanco
Source Classification
|
ERK
PAK
|
|
Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects .
|
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- HY-101392A
-
|
|
Apocynaceae
Alkaloids
Other Alkaloids
Plants
Rauwolfia canescens
Source Classification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
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Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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- HY-N4267
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Cardiovascular Disease
Structural Classification
other families
Classification of Application Fields
Lignans
Phenylpropanoids
Plants
Disease Research Fields
Source Classification
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Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
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Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
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- HY-N16538
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Product Name |
Chemical Structure |
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- HY-W013378S
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Carbamazepine 10,11 epoxide-d2 is the deuterium labeled Carbamazepine 10,11 epoxide . Carbamazepine 10,11-epoxide is an orally active metabolite of Carbamazepine (HY-B0246). Carbamazepine has anticonvulsant effect. Carbamazepine can be used for the research of seizures .
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- HY-U00315S
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Gidazepam-d5 is a deuterium labeled Gidazepam. Gidazepam is an agonist of GABA receptor channels (GABA RCs), and has anticonvulsant effect .
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- HY-B0184S1
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Felbamate-d5 is the deuterium labeled Felbamate . Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .
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- HY-B0184S
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Felbamate-d4 (W-554-d4) is the deuterium labeled Felbamate. Felbamate (W-554) is a potent anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).
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- HY-W013378S2
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Carbamazepine 10,11-epoxide- 13C,d2 is the deuterium labeled Carbamazepine 10,11-epoxide-C13. Carbamazepine 10,11-epoxide-C13 is a 13C-labled Carbamazepine 10,11-epoxide. Carbamazepine 10,11-epoxide is an orally active metabolite of Carbamazepine (HY-B0246). Carbamazepine has anticonvulsant effect. Carbamazepine can be used for the research of seizures .
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- HY-W777360
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Harman- 13C2, 15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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- HY-W700834
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Harman-d3 is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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