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Request The Product List ofDepression Depression

    Major depressive disorder, often referred to as major depression, is a heterogenous condition with complex and diverse neurobiological etiologies. Depression is characterized by a triad of symptoms: low or depressed mood, anhedonia and low energy or fatigue. Approximately 15% of the population in developed countries has been affected by depression in their lifetime and the chance of developing depression is twice as high in women. 40-50% of depressive causes are inheritable (genes as yet unidentified) and the remaining 50-60% of causes are caused by environmental stressors.


   Pathogenesis of Depression

   Traditionally, depression has been described as a disease of decreased monoamine function within the brain (also known as the monoamine hypothesis). Brain areas specifically involved are thought to include the hippocampus, prefrontal and cingulate cortex, and the amygdala. In addition the dopaminergic reward pathway, in particular the nucleus accumbens, and the hypothalamus may also be involved, and have been identified due to the symptoms of anhedonia, and abnormalities in sleep, appetite and circadian rhythms respectively, which are prevalent in depressed patients.

    Depression may also be caused by an enhancement of biological stress-response mechanisms, especially the hypothalamic-pituitary-adrenal (HPA) axis, is a common feature of depression, which is manifested by increased corticotrophin releasing factor (CRF) expression in the hypothalamus and cerebrospinal fluid (CSF).


    Pharmacological Intervention

    The main obstacle for depression research has been the lack of animal models for some depressive symptoms, such as guilt and suicidal ideology. This has hampered efforts to fully understand the disease and it remains an area of intense research.

    Current pharmacological interventions for depression focus on potentiation of the monoamine system. Tricyclic antidepressants act by inhibiting serotonin and/or noradrenalin uptake and monoamine oxidase (MAO) inhibitors reduce the enzymatic breakdown of serotonin, noradrenalin and dopamine. Novel pharmacological targets focusing on non-monoamine systems, such as CRF antagonists, GR antagonists, cytokines, melatonin receptoragonists, TrkB agonists, histone deacetylase (HDAC) inhibitors and κ-opioid receptor antagonists, are currently being developed.

Cat. No. Product Name CAS No. Information
GY02457

ACY-738

1375465-91-0

ACY-738 (ACY738) is a potent and specific HDAC6 inhibitor (IC50=1.7 nM) with improved brain bioavailability; displays 60-1500 fold selectivity over class I HDACs; induces dramatic increase in α-tubulin acetylation in brain and stimulates mouse exploratory behaviors; increases the innervation of the neuromuscular junctions in the gastrocnemius muscle and improves the motor and sensory nerve conduction in the mutant HSPB1-induced CMT2 mouse model.

GY10522

SAGE-217

1632051-40-1

SAGE-217 (Zuranolone, SAGE217) is a potent, orally active GABAA receptor positive allosteric modulator with EC50 of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA r eceptors, respectively; effectively reduces pentylenetretazol (PTZ)-induced seizures in mice, abolishes both behavioral and electrographic seizure activity.

GY05216

Rislenemdaz mesylate

1893392-76-1

Rislenemdaz (MK 0657;CERC 301) is a potent, orally bioavailable, brain‐penetrant, NR2B-selective NMDA receptor (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM respectively, with no off-target activity; inhibits calcium influx into agonist‐stimulated NMDA‐GluN1a/GluN2B L(tk‐) cells with IC50 of 3.6 nM, with no effect on GluN2A up to 30 uM; significantly decreases immobility frequency and increases swimming behavior in acute depression models.

GY04112

CERC-501

1174130-61-0

LY 2456302 (CERC-501, JSPA 0658, Aticaprant) is a potent, selective, short-acting antagonist of κ-opioid receptor (KOR) with Ki of 0.81 nM; displays >30-fold selectivity over MOR and DOR; selectively and potently occupies central kappa opioid receptors in vivo (ED50=0.33 mg/kg); produces antidepressant-like effects in the mouse forced swim test and enhanced the effects of imipramine and citalopram; orally-bioavailable and excellent pharmacokinetic properties.

GY03571

Nelotanserin

839713-36-9

A potent, selective 5-HT2A inverse agonist with pKi of 9.2; displays >30- and 5000-fold selectivity compared with 5-HT2C and 5-HT2B receptors; prevents DOI-induced hypolocomotion and increases sleep consolidation; orally active.

GY05377

Org-26576

1026791-61-6

A potent AMPA receptor positive allosteric modulator; displays 10-30 fold greater potency in potentiating AMPA-mediated electrophysiological responses with an EC50 of 8-16 uM in rat hippocampal primary cultured neurons, compared to CX516; increases neuronal cell proliferation and survival in adult rodent hippocampus; produces nootropic effects in vivo.

GY05370

Radafaxine HCl

106083-71-0

A potent metabolite of bupropion; selectivly inhibits the reuptake of norepinephrine over dopamine; DAT and NET transporters inhibitor, and nAChR family modulator.

GY05364

Paroxetine HCl hemihydrate

110429-35-1

Piperidine, 3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)-, hydrochloride, hydrate (2:2:1), (3S,4R)-

GY05350

Edivoxetine HCl

1194374-05-4

Edivoxetine (LY2216684) is a novel potent, selective norepinephrine reuptake inhibitor (NERI) being evaluated as adjunctive treatment for major depressive disorder (MDD).

GY05349

Edivoxetine

1194508-25-2

Edivoxetine (LY2216684) is a novel potent, selective norepinephrine reuptake inhibitor (NERI) being evaluated as adjunctive treatment for major depressive disorder (MDD).

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