Search Result
Results for "
synaptosomes
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N10772
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- HY-N2326
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nAChR
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Neurological Disease
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(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM) .
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- HY-108973
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5-HT Receptor
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Neurological Disease
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CGP 15210G is an inhibitor of 5-HT reuptake. CGP 15210G inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo .
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- HY-123199
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SABA
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Serotonin Transporter
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Neurological Disease
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Serotonin azidobenzamidine is an arylazido derivative of 5-hydroxytryptamine (HY-B1473A). Serotonin azidobenzamide competitively inhibits [3H]5-hydroxytryptamine uptake by rat cortical synaptosomes in the dark with a Ki of 130 nM .
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- HY-16923A
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BIII-890 hydrochloride; BIII-890 CL
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Sodium Channel
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Neurological Disease
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Crobenetine hydrochloride (BIII-890 hydrochloride) is the hydrochloride form of Crobenetine (HY-16923). Crobenetine hydrochloride is a selective inhibitor for Na + channel. Crobenetine hydrochloride displaces 3HBTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, exhibits only low binding affinity for other receptors and ion channels. Crobenetine hydrochloride protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
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- HY-16923
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BIII-890; BIII-890 CL free acid
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Sodium Channel
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Neurological Disease
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Crobenetine (BIII-890), a benzomorphan derivative, is a potent, selective, and highly use-dependent Na + channel blocker. Crobenetine displaces [3H]BTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, yet exhibits only low binding affinity for other receptors and ion channels. Crobenetine protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
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- HY-129682
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- HY-101334
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GlyT
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Neurological Disease
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MPDC is a potent and competitive inhibitor of the Na +-dependent high-affinity glutamate transporter in forebrain synaptosomes .
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- HY-101334A
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GlyT
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Neurological Disease
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MPDC hydrochloride is a potent and competitive inhibitor of the Na +-dependent high-affinity glutamate transporter in forebrain synaptosomes .
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- HY-101753A
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Cyanimipramine hydrochloride; Ro 11-2465 hydrochloride
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5-HT Receptor
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Neurological Disease
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Cianopramine hydrochloride (Cyanimipramine hydrochloride; Ro 11-2465 hydrochloride) is the hydrochloride form of Cianopramine (HY-101753). Cianopramine hydrochloride is an antidepressant, which selectively inhibits the serotonin uptake into synaptosomes .
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- HY-145577
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Monoamine Oxidase
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Neurological Disease
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Lafadofensine is the monoamines reuptake inhibitor. Lafadofensine has th sufficient effects after short-term administration (extracted from patent WO2006121218A1, compound 1) .
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- HY-145577A
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Monoamine Transporter
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Neurological Disease
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Lafadofensine D-(-)-Mandelic acid is the monoamines reuptake inhibitor. Lafadofensine D-(-)-Mandelic acid has sufficient effects after short-term administration .
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- HY-16934
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Cholinesterase (ChE)
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Neurological Disease
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ML352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki
values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively .
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- HY-B1237A
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Na+/K+ ATPase
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Cardiovascular Disease
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Suloctidil hydrochloride hydrochloride is an active agent against on Na+/K+ ATPase activity and on membrane fluidity in rat brain synaptosomes. Suloctidil hydrochloride is currently being evaluated in many clinical trials for use in dementia and thrombotic disorders.
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- HY-B1237
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Na+/K+ ATPase
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Cardiovascular Disease
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Suloctidil is a new drug that is currently being evaluated in many clinical trials for use in dementia and thrombotic disorders
Target:
Effect of suloctidil on Na+/K+ ATPase activity and on membrane fluidity in rat brain synaptosomes.
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- HY-B0696B
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NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrate
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GABA Receptor
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Neurological Disease
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Tiagabine hydrochloride hydrate is a potent and selective GABA uptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
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- HY-131556
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p-Iodoamphetamine hydrochloride
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5-HT Receptor
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Neurological Disease
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4-Iodoamphetamine (p-Iodoamphetamine) hydrochloride is a halogenated amphetamine featuring an iodine atom at the para position of the phenyl group. 4-Iodoamphetamine hydrochloride selectively induces serotonin release and inhibits reuptake by rat brain synaptosomes.
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- HY-18610
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Ro 8-4650 hydrochloride
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Dopamine Transporter
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Neurological Disease
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Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
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- HY-W708023
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5-HT Receptor
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Neurological Disease
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5-APDI hydrochloride is an indane with an amphetamine-like aminopropane group. 5-APDI hydrochloride inhibits the uptake of serotonin, dopamine, and norepinephrine by crude synaptosomes (IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively) .
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- HY-18610A
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Ro 8-4650
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Dopamine Transporter
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Neurological Disease
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Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
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- HY-B0696
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NO050328; NO328; TGB
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GABA Receptor
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Neurological Disease
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Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
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- HY-B1287
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(±)-Citalopram hydrobromide; Lu 10-171
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Serotonin Transporter
Autophagy
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Neurological Disease
Cancer
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Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
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- HY-158252S
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NO050328-d5 hydrochloride; NO328-d5 hydrochloride; TGB-d5 hydrochloride
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Isotope-Labeled Compounds
GABA Receptor
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Neurological Disease
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Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
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- HY-79635R
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Bacterial
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Infection
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Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
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- HY-B0696AR
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GABA Receptor
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Neurological Disease
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Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
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- HY-113273B
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Endogenous Metabolite
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Metabolic Disease
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Diadenosine pentaphosphate pentaammonium is an endogenous vasoactive purine dinucleotide which has been isolated from thrombocytes. Diadenosine polyphosphates (ApnA, n=2–7) have been identified as constituents of secretory vesicles such as in platelets, chromaffin cells, Torpedo synaptic terminals and brain synaptosomes .
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- HY-113273C
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Endogenous Metabolite
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Metabolic Disease
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Diadenosine pentaphosphate pentalithium is an endogenous vasoactive purine dinucleotide which has been isolated from thrombocytes. Diadenosine polyphosphates (ApnA, n=2–7) have been identified as constituents of secretory vesicles such as in platelets, chromaffin cells, Torpedo synaptic terminals and brain synaptosomes .
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- HY-B0696AS
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NO050328-dd4 hydrochloride; NO328-d4 hydrochloride; TGB-d4 hydrochloride
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GABA Receptor
Isotope-Labeled Compounds
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Neurological Disease
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Tiagabine-d4 hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
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- HY-113273A
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Endogenous Metabolite
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Metabolic Disease
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Diadenosine pentaphosphate pentasodium is an endogenous vasoactive purine dinucleotide which has been isolated from thrombocytes. Diadenosine polyphosphates (ApnA, n=2–7) have been identified as constituents of secretory vesicles such as in platelets, chromaffin cells, Torpedo synaptic terminals and brain synaptosomes .
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- HY-W008610
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Dopamine Receptor
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Neurological Disease
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GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats .
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- HY-N6776
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Potassium Channel
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Neurological Disease
Cancer
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Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals .
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- HY-100968
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Dopamine Receptor
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Neurological Disease
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GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats .
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- HY-120170
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ASCT
Adrenergic Receptor
Dopamine Transporter
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Neurological Disease
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BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [ 3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research .
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- HY-B1287R
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(±)-Citalopram hydrobromide(Standard); Lu 10-171 (Standard)
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Serotonin Transporter
Autophagy
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Neurological Disease
Cancer
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Citalopram (hydrobromide) (Standard) is the analytical standard of Citalopram (hydrobromide). This product is intended for research and analytical applications. Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
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- HY-B0696A
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NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride
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GABA Receptor
Trk Receptor
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Neurological Disease
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Tiagabine hydrochloride is an anticonvulsant agent and a selective inhibitor of the GAT-1 GABA transporter with a Ki of ∼0.1 μM. Tiagabine hydrochloride potently and selectively inhibits GABA reuptake with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in synaptosomes, neurons and glia, respectively. Tiagabine hydrochloride has neuroprotective properties .
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- HY-B1287S
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(±)-Citalopram hydrobromide-d3; Lu 10-171-d3
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Isotope-Labeled Compounds
Serotonin Transporter
Autophagy
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Neurological Disease
Cancer
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Citalopram-d3 ((±)-Citalopram-d3) hydrobromide is deuterium labeled Citalopram (hydrobromide). Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
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- HY-100838
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L-CCG III
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EAAT
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Neurological Disease
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cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
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- HY-103509
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GABA Receptor
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Neurological Disease
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NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .
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- HY-B1110
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(±)-Nomifensine; Nomifensin
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Dopamine Receptor
Adrenergic Receptor
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Neurological Disease
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Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine has antidepressive effects .
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- HY-B1110A
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(±)-Nomifensine maleate; Nomifensin maleate
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Dopamine Receptor
Adrenergic Receptor
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Neurological Disease
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Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine maleate has antidepressive effects .
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- HY-100769
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YL0919
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5-HT Receptor
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Neurological Disease
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Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A?receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder .
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- HY-100928
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Calcium Channel
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Neurological Disease
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YS 035 hydrochloride is a Ca 2+ antagonist on cellular uptake and mitochondrial efflux of calcium ions. YS 035 hydrochloride inhibits Ca 2+ uptake by muscle cells and inhibits Na +/Ca 2+ exchange (Ki=28 µM). YS 035 hydrochloride is a useful tool for research on the mitochondrial Ca 2+ transport .
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- HY-117160
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4-trans-hydroxycyclohexyl Glyburide; 4-trans-hydroxy Glibenclamide
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Potassium Channel
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Neurological Disease
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rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide (HY-15206). It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9. rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50 values of 0.95 and 100 nM, respectively.
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- HY-B1110S
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(±)-Nomifensine-d3 maleate; Nomifensin-d3 maleate
|
Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
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Neurological Disease
|
Nomifensine-d3 ((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine has antidepressive effects .
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- HY-160959
-
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nAChR
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Neurological Disease
|
AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-100838
-
L-CCG III
|
EAAT
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Neurological Disease
|
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-158252S
-
|
Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
|
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- HY-B0696AS
-
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Tiagabine-d4 hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
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- HY-B1287S
-
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Citalopram-d3 ((±)-Citalopram-d3) hydrobromide is deuterium labeled Citalopram (hydrobromide). Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
|
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- HY-B1110S
-
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Nomifensine-d3 ((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine has antidepressive effects .
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Cat. No. |
Product Name |
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Classification |
-
- HY-123199
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SABA
|
|
Azide
|
Serotonin azidobenzamidine is an arylazido derivative of 5-hydroxytryptamine (HY-B1473A). Serotonin azidobenzamide competitively inhibits [3H]5-hydroxytryptamine uptake by rat cortical synaptosomes in the dark with a Ki of 130 nM .
|
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