Search Result
Results for "
norepinephrine+transporter
" in MedChemExpress (MCE) Product Catalog:
11
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B1272
-
-
-
- HY-14258
-
|
(S)-Citalopram; (S)-(+)-Citalopram
|
Serotonin Transporter
|
Neurological Disease
|
|
Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram is an antidepressant for the research of major depression .
|
-
-
- HY-14258A
-
|
(S)-Citalopram oxalate; (S)-(+)-Citalopram oxalate
|
Serotonin Transporter
|
Neurological Disease
Cancer
|
|
Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
|
-
-
- HY-B0168A
-
|
|
Serotonin Transporter
PERK
|
Neurological Disease
|
|
Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
|
-
-
- HY-12798
-
|
AR-13324
|
Monoamine Transporter
ROCK
|
Cardiovascular Disease
Neurological Disease
|
|
Netarsudil (AR-13324) is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil reduces intraocular pressure by inhibiting ROCK, causing relaxation of trabecular meshwork cells and dilation of episcleral veins, thereby increasing the ease of aqueous humor outflow, while inhibiting NET to reduce aqueous humor production. Netarsudil is mainly used in the study of ocular hypertension and primary open-angle glaucoma .
|
-
-
- HY-12798B
-
|
AR-13324 hydrochloride
|
ROCK
|
Cardiovascular Disease
Neurological Disease
|
|
Netarsudil (AR-13324) hydrochloride is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil hydrochloride reduces intraocular pressure by inhibiting ROCK, causing relaxation of trabecular meshwork cells and dilation of episcleral veins, thereby increasing the ease of aqueous humor outflow, while inhibiting NET to reduce aqueous humor production. Netarsudil hydrochloride is mainly used in the study of ocular hypertension and primary open-angle glaucoma .
|
-
-
- HY-W380450
-
|
Viloxazin; Emovit
|
5-HT Receptor
|
Neurological Disease
|
|
Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
|
-
-
- HY-125784
-
|
Viloxazin hydrochloride; Emovit hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Viloxazine hydrochloride is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50=0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50=32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
|
-
-
- HY-B0952
-
|
Tuaminoheptane
|
Adrenergic Receptor
|
Neurological Disease
|
|
2-Aminoheptane (Tuaminoheptane) is a norepinephrine transporter inhibitor. 2-Aminoheptane binds to norepinephrine transporter via ionic and hydrophobic interactions to block norepinephrine uptake. 2-Aminoheptane deactivates ω-TAmla enzyme, reduces recombinant whole cell stability, and acts as an amino group donor substrate for ω-TA and ω-TAmla enzymes. 2-Aminoheptane can be used in research on depression and Alzheimer's disease .
|
-
-
- HY-12798A
-
|
AR-13324 dimesylate
|
ROCK
|
Cardiovascular Disease
Neurological Disease
|
|
Netarsudil (AR-13324) dimesylate is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil dimesylate reduces intraocular pressure by inhibiting ROCK, causing relaxation of trabecular meshwork cells and dilation of episcleral veins, thereby increasing the ease of aqueous humor outflow, while inhibiting NET to reduce aqueous humor production. Netarsudil dimesylate is mainly used in the study of ocular hypertension and primary open-angle glaucoma .
|
-
-
- HY-B0168B
-
|
(1S,2R)-Milnacipran hydrochloride; F-2695 hydrochloride
|
Serotonin Transporter
Trk Receptor
PI3K
Akt
mTOR
P-glycoprotein
|
Neurological Disease
Inflammation/Immunology
|
|
Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
|
-
-
- HY-12766S
-
|
|
Isotope-Labeled Compounds
nAChR
Dopamine Transporter
|
Neurological Disease
|
|
Bupropion morpholinol-d6 is the deuterated form of Bupropion morpholinol. Bupropion morpholinol is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .
|
-
-
- HY-135615A
-
|
N-Desmethylsibutramine hydrochloride
|
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
|
Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant .
|
-
-
- HY-79722
-
|
trans-4-Aminocyclohexan-1-ol
|
Drug Intermediate
|
Neurological Disease
|
|
4-trans-Hydroxycyclohexylamine (trans-4-Aminocyclohexan-1-ol) is an intermediate. 4-trans-Hydroxycyclohexylamine can be used in the synthesis of norepinephrine transporter inhibitors. 4-trans-Hydroxycyclohexylamine can be used in the research of mood and behavior-related diseases .
|
-
-
- HY-14258AR
-
|
(S)-Citalopram oxalate (Standard); (S)-(+)-Citalopram oxalate (Standard)
|
Reference Standards
Serotonin Transporter
|
Neurological Disease
Cancer
|
|
Escitalopram (oxalate) (Standard) is the analytical standard of Escitalopram (oxalate). This product is intended for research and analytical applications. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
|
-
-
- HY-B0168
-
|
|
Serotonin Transporter
PERK
|
Neurological Disease
|
|
Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
|
-
-
- HY-B1272A
-
-
-
- HY-N7506
-
|
Delta3,2-Hydroxylbakuchiol
|
Monoamine Transporter
Dopamine Transporter
|
Neurological Disease
|
|
13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) that can be isolated from Psoralea corylifolia (L.), is a potent selective monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50 = 0.58 μM) and norepinephrine transporter (NET) (IC50 = 0.69 μM) than for the serotonin transporter (SERT) (IC50 = 312.02 μM). 13-Hydroxyisobakuchiol increases the activity of intact mice and improves the decreased activity of reserpinized mice in vivo. 13-Hydroxyisobakuchiol can be used for the research of disorders such as Parkinson's disease and depression .
|
-
-
- HY-17590
-
|
(S,S)-Hydroxybupropion hydrochloride; GW-353162A; BW-306U
|
Monoamine Transporter
|
Neurological Disease
|
|
Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
|
-
-
- HY-12766
-
|
|
Dopamine Transporter
nAChR
|
Neurological Disease
|
|
Bupropion morpholinol (Hydroxy Bupropion) is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .
|
-
-
- HY-118796
-
|
4-HO-MET; 4-Hydroxy-N-methyl-N-ethyltryptamine
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
|
4-Hydroxy MET (4-HO-MET; 4-Hydroxy-N-methyl-N-ethyltryptamine) is a synthetic tryptamine psychoactive substance. 4-Hydroxy MET is a partial 5-HT2A receptor agonist, a serotonin transporter inhibitor and weak norepinephrine transporter inhibitor. 4-Hydroxy MET affects emotional, motoric, and cognitive functions via serotonergic hallucinogenic activity .
|
-
-
- HY-14790
-
|
(S,S)-(+)-Reboxetine
|
Adrenergic Receptor
|
Neurological Disease
|
|
Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine reuptake inhibitor with activity in increasing urethral resistance. Esreboxetine has been reported to be effective in patients with stress urinary incontinence in a Phase IIa clinical study, achieving this effect by increasing urethral closure. The mechanism of action of esreboxetine involves inhibition of norepinephrine transporters in the central and peripheral nervous systems. The peripheral selectivity of esreboxetine helps it significantly increase urethral resistance without penetrating the brain .
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-
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- HY-14258AS
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
Escitalopram-d6 (oxalate) is the deuterium labeled Escitalopram oxalate. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ~30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
|
-
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- HY-B1272R
-
|
|
Reference Standards
Adrenergic Receptor
ERK
JNK
p38 MAPK
NF-κB
AP-1
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Desipramine hydrochloride (Standard) is the analytical standard of Desipramine hydrochloride (HY-B1272). This product is intended for research and analytical applications. Desipramine hydrochloride is a first-generation tricyclic antidepressant. Desipramine hydrochloride selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine hydrochloride activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine hydrochloride also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine hydrochloride can be used for the research of hepatocellular cancer, inflammation, and neurological diseases .
|
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- HY-156807
-
|
|
Serotonin Transporter
5-HT Receptor
|
Neurological Disease
|
LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .
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- HY-107128
-
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TD-9855 hydrochloride
|
Serotonin Transporter
|
Neurological Disease
|
|
Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .
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-
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- HY-172421
-
-
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- HY-B0457S
-
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Chlorimipramine-d3 hydrochloride; G-34586-d3 hydrochloride; NSC-169865-d3 hydrochloride
|
Serotonin Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Clomipramine-d3 (hydrochloride) is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
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- HY-B0457AS
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-
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- HY-129040
-
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MIBG; Iobenguane
|
Monoamine Transporter
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Neurological Disease
Endocrinology
Cancer
|
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m-Iodobenzylguanidine (Iobenguane) is a ligand with high affinity against norepinephrine transporter (NET). m-Iodobenzylguanidine is used as an imaging agent in the diagnostic imaging and radionuclide studies of neuroendocrine tumors, such as neuroblastoma, pheochromocytoma and carcinoid tumor .
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- HY-B1308
-
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
|
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Adrenalone hydrochloride is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Adrenalone hydrochloride is an inhibitor of dopamine β oxidase. Adrenalone hydrochloride is chemically similar to known norepinephrine transporter (NET) ligands with an IC50 of 36.9 μM .
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-
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- HY-B1308A
-
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Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
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Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Adrenalone is an inhibitor of dopamine β oxidase. Adrenalone is chemically similar to known norepinephrine transporter (NET) ligands with an IC50 of 36.9 μM .
|
-
-
- HY-14258AS1
-
|
(S)-Citalopram-d4 oxalate; (S)-(+)-Citalopram-d4 oxalate
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
|
|
Escitalopram-d4 (oxalate) is deuterium labeled Escitalopram (oxalate). Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ~30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
|
-
-
- HY-14794A
-
|
(1S,2R)-Milnacipran; F2695
|
Serotonin Transporter
Trk Receptor
PI3K
mTOR
P-glycoprotein
Akt
|
Neurological Disease
Inflammation/Immunology
|
|
Levomilnacipran ((1S,2R)-Milnacipran) is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
|
-
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- HY-B0168S
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
PERK
|
Neurological Disease
|
|
Milnacipran-d10 (hydrochloride) is the deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
|
-
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- HY-W052508R
-
|
N-Desalkylquetiapine (Standard)
|
5-HT Receptor
Reference Standards
|
Neurological Disease
|
|
Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .
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-
-
- HY-148863
-
|
|
Calcium Channel
Monoamine Transporter
|
Inflammation/Immunology
|
|
Cavα2δ1&NET-IN-2 (Compound 45CS) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-2 inhibits Cavα2δ-1 with a Ki of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a Ki of 59 nM and IC50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain .
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-
-
- HY-103217
-
-
-
- HY-103218
-
|
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Adrenergic Receptor
|
Neurological Disease
|
|
Talsupram (hydrochloride) is a selective norepinephrine inhibitor with high affinity for norepinephrine transporter (NET) and can be used in the study of neuropathic pain .
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-
-
- HY-19346
-
|
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ROCK
|
Others
|
|
AR-13324 analog mesylate is an analog of AR-13324. AR-13324 is an ROCK and norepinephrine transporter (NET) inhibitor .
|
-
-
- HY-172029
-
|
|
Monoamine Transporter
|
Neurological Disease
|
|
3,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride is an analog of Pyrovalerone. Pyrovalerone inhibits the dopamine transporter (DAT),serotonin transporter (SERT),and the norepinephrine transporter (NET) .
|
-
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- HY-135615
-
|
N-Desmethylsibutramine
|
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
|
Desmethyl Sibutramine, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine can be used in the research of obesity and appetite suppressant .
|
-
-
- HY-B1308R
-
|
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Adrenalone (hydrochloride) (Standard) is the analytical standard of Adrenalone (hydrochloride). This product is intended for research and analytical applications. Adrenalone hydrochloride is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Adrenalone hydrochloride is an inhibitor of dopamine β oxidase. Adrenalone hydrochloride is chemically similar to known norepinephrine transporter (NET) ligands with an IC50 of 36.9 μM .
|
-
-
- HY-B0932R
-
|
L-Propionylcarnitine chloride (Standard); ST-261 (Standard)
|
Integrin
NADPH Oxidase
Reference Standards
Others
|
Others
|
|
Adrenalone (hydrochloride) (Standard) is the analytical standard of Adrenalone (hydrochloride). This product is intended for research and analytical applications. Adrenalone hydrochloride is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Adrenalone hydrochloride is an inhibitor of dopamine β oxidase. Adrenalone hydrochloride is chemically similar to known norepinephrine transporter (NET) ligands with an IC50 of 36.9 μM .
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-
-
- HY-135615AR
-
|
N-Desmethylsibutramine hydrochloride (Standard)
|
Reference Standards
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
|
Desmethyl Sibutramine (hydrochloride) (Standard) is the analytical standard of Desmethyl Sibutramine (hydrochloride). This product is intended for research and analytical applications. Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant .
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-
-
- HY-121212R
-
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Aminotransferases (Transaminases)
Reference Standards
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Desmethyl Sibutramine (hydrochloride) (Standard) is the analytical standard of Desmethyl Sibutramine (hydrochloride). This product is intended for research and analytical applications. Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant .
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-
-
- HY-126158
-
|
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Dopamine Transporter
Serotonin Transporter
|
Neurological Disease
|
|
SRI-29574 is an allosteric modulator of the dopamine transporter (DAT). SRI-29574 partially inhibits the uptake of the DAT (IC50=2.3 nM) and also partially inhibits the uptake of the serotonin transporter (SERT) and norepinephrine transporter (NET). SRI-29574 may serve as a useful probe to study the function and regulatory mechanisms of DAT .
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-
-
- HY-133858
-
|
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5-HT Receptor
|
Neurological Disease
|
|
25N-NBOMe hydrochloride, a 2C-N derivative, is a 5-HT2A and 5-HT2C receptors agonist with Ki values of 0.144 nM and 1.06 nM, respectively. 25N-NBOMe hydrochloride has little to no efficacy at inducing release of preloaded neurotransmitter from recombinant dopamine, serotonin and norepinephrine transporters .
|
-
-
- HY-14258R
-
|
(S)-Citalopram (Standard); (S)-(+)-Citalopram (Standard)
|
Serotonin Transporter
Reference Standards
|
Neurological Disease
Cancer
|
|
Escitalopram (Standard) is the analytical standard of Escitalopram. This product is intended for research and analytical applications. Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram has ~30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram is an antidepressant for the research of major depression .
|
-
-
- HY-117542
-
|
|
Histone Methyltransferase
|
Neurological Disease
|
|
D595 is a phenylethylamine calcium channel blocker with potent negative inotropic activity. D595 has shown significant efficacy in its corresponding pharmacological studies, especially in inhibiting the uptake of monoamine neurotransmitters. D595 has high affinity in binding to the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET). Structural adjustments of D595, especially changes in the hydroxyl stereochemistry, significantly affect its interaction with the transporters, showing a specific preference for stereoisomers .
|
-
- HY-10427A
-
|
iso-NRI-022
|
Serotonin Transporter
Dopamine Transporter
|
Cardiovascular Disease
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iso-WAY-260022 (Compound 13R) is an orally active, brain-penetrant and selective norepinephrine transporter (hNET) inhibitor with an IC50 value of 140 nM. iso-WAY-260022 also shows inhibitory effects on human serotonin (hSERT) and dopamine transporters (hDAT). iso-WAY-260022 inhibits norepinephrine reuptake and increases hypothalamic norepinephrine levels to regulate thermoregulatory center function. iso-WAY-260022 is promising for research of vasomotor symptoms, such as menopausal hot flushes, night sweats .
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- HY-B1272AS
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- HY-B1272AS1
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- HY-B0168AS
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Isotope-Labeled Compounds
Serotonin Transporter
PERK
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Neurological Disease
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Milnacipran-d5 hydrochloride is deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
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- HY-B0168BS
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(1S,2R)-Milnacipran-d5 hydrochloride; F-2695-d5 hydrochloride
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Isotope-Labeled Compounds
Serotonin Transporter
Trk Receptor
PI3K
Akt
mTOR
P-glycoprotein
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Neurological Disease
Inflammation/Immunology
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Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
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- HY-B0168AR
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Reference Standards
Serotonin Transporter
PERK
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Neurological Disease
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Milnacipran (hydrochloride) (Standard) is the analytical standard of Milnacipran hydrochloride (HY-B0168A). This product is intended for research and analytical applications. Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
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- HY-14794AS
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(1S,2R)-Milnacipran-d10 hydrochloride; F2695-d10 hydrochloride
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Isotope-Labeled Compounds
Serotonin Transporter
Trk Receptor
PI3K
mTOR
P-glycoprotein
Akt
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Neurological Disease
Inflammation/Immunology
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Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
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- HY-W380450R
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Viloxazin (Standard); Emovit (Standard)
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Reference Standards
5-HT Receptor
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Neurological Disease
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Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .
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- HY-116062A
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Histone Methyltransferase
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Neurological Disease
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JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
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- HY-148862
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Calcium Channel
Monoamine Transporter
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Inflammation/Immunology
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Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain .
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- HY-186093
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Drug Intermediate
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Others
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(S,S)-Reboxetine-OH is a phenol compound. (S,S)-Reboxetine-OH can be used to synthesize norepinephrine transporter ligand .
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- HY-107128R
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TD-9855 hydrochloride (Standard)
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Reference Standards
Serotonin Transporter
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Neurological Disease
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Ampreloxetine hydrochloride (Standard) (TD-9855 hydrochloride (Standard)) is the analytical standard of Ampreloxetine (hydrochloride) (HY-107128). This product is intended for research and analytical applications. Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .
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- HY-U00069
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Monoamine Transporter
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Neurological Disease
Inflammation/Immunology
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Thionisoxetine is a norepinephrine transporter inhibitor with a Ki value of 0.2 nM in rats, and exhibits anti-hyperalgesic and analgesic activities. Thionisoxetine reverses thermal hyperalgesia and mechanical allodynia in rats. Thionisoxetine can be used in studies related to persistent inflammatory pain .
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- HY-106604
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LM 1404
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Monoamine Transporter
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Neurological Disease
Metabolic Disease
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Lortalamine (LM 1404) is a selective norepinephrine transporter inhibitor with an IC50 of <1 nM. Lortalamine is a non-tricyclic antidepressant. Lortalamine antagonises Reserpine (HY-N0480)-induced ptosis and hypothermia. Lortalamine inhibits norepinephrine uptake .
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- HY-172763
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Drug Derivative
Serotonin Transporter
Dopamine Transporter
5-HT Receptor
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Neurological Disease
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EDMA hydrochloride is a derivative of MDMA. EDMA hydrochloride is a substrate for multiple neurotransmitter transporters, including serotonin transporter (SERT), dopamine transporter (DAT), and norepinephrine transporter (NET). EDMA hydrochloride has 5-HT releasing activity at SERT (EC50 = 117 nM) and MPP + releasing activity at DAT (EC50 = 597 nM) and NET (EC50 = 325 nM) .
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- HY-182247
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Serotonin Transporter
Dopamine Transporter
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Neurological Disease
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D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder .
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- HY-186094
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Drug Derivative
Drug Intermediate
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Neurological Disease
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(S,S)-Demethyl-reboxetine is a key phenolic precursor for the preparation of the PET tracer (S,S)-[ 11C]-MeNER. (S,S)-Demethyl-reboxetine is also the demethylated derivative of Reboxetine (HY-14560). Efficient synthesis of the norepinephrine transporter (NET)-targeted tracer is achieved through 11C methylation of (S,S)-Demethyl-reboxetine. (S,S)-Demethyl-reboxetine serves as a core raw material for the synthesis of radiopharmaceuticals related to NET imaging .
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- HY-179568
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Monoamine Transporter
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Neurological Disease
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F3288-0031 is a brain-penetrant norepinephrine transporter (NET) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of NET, stabilizing the inward-open state and has a preferential NET/SERT inhibition with pIC50 = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions .
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HY-L906
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647 compounds
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On May 15, 2024, "Dimerization and antidepressant recognition at noradrenaline transporter" was published online by Nature. The research findings were an effort from Shanghai Institute of Materia Medica, Chinese Academy of Sciences. This study unraveled the important neural system target - the noradrenaline transporter (NET), obtaining the binding modes of human NET homodimers with the natural substrate norepinephrine (NE) and six selective antidepressants. It laid an important theoretical foundation for understanding the physiological regulation mechanisms of NET and other monoamine transporters.
The Norepinephrine Transporter (NET) Compound Library is obtained by computer-aided virtual screening based on the HY-L901 compound library . The specific screening process includes molecular docking screening, key pharmacophore screening, and CNS-MPO screening, which can be used for new drug discovery targeting the noradrenaline transporter.
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-14258
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(S)-Citalopram; (S)-(+)-Citalopram
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Natural Products
Endogenous metabolite
Source Classification
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Serotonin Transporter
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Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram is an antidepressant for the research of major depression .
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- HY-N7506
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Delta3,2-Hydroxylbakuchiol
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Structural Classification
Monophenols
Leguminosae
Phenols
Psoralea corylifolia L.
Plants
Source Classification
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Monoamine Transporter
Dopamine Transporter
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13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) that can be isolated from Psoralea corylifolia (L.), is a potent selective monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50 = 0.58 μM) and norepinephrine transporter (NET) (IC50 = 0.69 μM) than for the serotonin transporter (SERT) (IC50 = 312.02 μM). 13-Hydroxyisobakuchiol increases the activity of intact mice and improves the decreased activity of reserpinized mice in vivo. 13-Hydroxyisobakuchiol can be used for the research of disorders such as Parkinson's disease and depression .
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- HY-14258R
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(S)-Citalopram (Standard); (S)-(+)-Citalopram (Standard)
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Structural Classification
Natural Products
Endogenous metabolite
Source Classification
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Serotonin Transporter
Reference Standards
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Escitalopram (Standard) is the analytical standard of Escitalopram. This product is intended for research and analytical applications. Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram has ~30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram is an antidepressant for the research of major depression .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-12766S
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Bupropion morpholinol-d6 is the deuterated form of Bupropion morpholinol. Bupropion morpholinol is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .
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- HY-14258AS
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Escitalopram-d6 (oxalate) is the deuterium labeled Escitalopram oxalate. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ~30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
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- HY-B0457S
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Clomipramine-d3 (hydrochloride) is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
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- HY-B0457AS
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Clomipramine-d3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
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- HY-14258AS1
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Escitalopram-d4 (oxalate) is deuterium labeled Escitalopram (oxalate). Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ~30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
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-
- HY-B0168S
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Milnacipran-d10 (hydrochloride) is the deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
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- HY-B1272AS
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Desipramine-d4 is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases .
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- HY-B1272AS1
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Desipramine-d3 is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases .
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- HY-B0168AS
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Milnacipran-d5 hydrochloride is deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
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- HY-B0168BS
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Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
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- HY-14794AS
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Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
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