Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
Serotonin reuptake inhibitor
Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%). -
serotonin transporter (SER) inhibitor
Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist. -
norepinephrine (NE) transporter inhibitor
Atomoxetine hydrochloride is a competitive and specific inhibitor of SLC6A2 while demonstrating weak ST and DAT inhibition as studied in synaptosomes of rat hypothalamus. -
serotonin uptake inhibitor
Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively). -
norepinephrine reuptake inhibitor
Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor -
serotonin/NE reuptake inhibitor
Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor. -
adrenergic receptor/5-HT receptor inhibitor
Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. -
serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI). -
5-HT3 receptor inhibitor
Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β. -
5-HT1A receptor agonist/serotonin reuptake inhibitor
YL0919, a novel antidepressant candidate with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells were 1.78??0.34 nM and 1.93??0.18 nM respectively. -
Serotonin reuptake inhibitor
Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM. -
5-HT1A receptor antagonist/COMT inhibitor
Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. -
5-HT2 receptors inhibitor
Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test. -
triple reuptake inhibitor/5-HT2A/5-HT2C/5-HT3/α1A-adrenergic receptor antagonis
Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist. -
5-HT1A/5-HT1B/5-HT3A/5-HT7 receptor/SERT inhibitor
Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. -
SSR inhibitor / 5-HT1A receptor partial agonist
Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist. -
serotonin reuptake inhibitor/5-HT2A receptor antagonist
Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1. -
norepinephrine reuptake inhibitor
(R)-Viloxazine Hydrochloride is the R-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant. -
norepinephrine reuptake inhibitor
(S)-Viloxazine Hydrochloride is the S-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant. -
5-HT Receptor Inhibitor
BF-1 is a potent antagonist of the 5-HT2B receptor, exhibiting a pKi value of 10.05 and an IC50 of 2.6 nM. This compound demonstrates significant inhibitory activity, making it valuable for research applications in neurobiology and pharmacology. Its specificity for the 5-HT2B receptor allows for detailed investigation into serotonin signaling pathways and related physiological processes. -
5-HT Receptor Inhibitor
5-APDI hydrochloride is a selective inhibitor of the 5-HT receptor, exhibiting significant biological activity in modulating neurotransmitter uptake. It effectively inhibits the reuptake of serotonin, dopamine, and norepinephrine in crude synaptosomes, with IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively. This compound is valuable in research applications related to neuropharmacology and the study of mood disorders. -
5-HT Uptake Inhibitor
Litoxetine is a selective 5-HT uptake inhibitor that functions primarily through its action on serotonin transporters. It also acts as a 5-HT3 receptor antagonist, exhibiting a Ki value of 85 nM for cerebral 5-HT3 receptors. This compound is utilized in research related to depression and nausea, showcasing its potential as an antidepressant and antiemetic agent. -
5-HT6 Receptor Modulator/Lp-PLA2 Inhibitor
Goxalapladib is a selective modulator of the 5-HT6 receptor that also serves as an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Its mechanism of action suggests potential applications in the investigation of atherosclerosis-related cardiovascular diseases. This compound facilitates research into the modulation of lipid metabolism and inflammation, making it a valuable tool for studies focused on cardiovascular health. -
5-HT2 Inhibitor
Cloroperone is a potent 5-HT2 receptor inhibitor with a Ki value of 4.5 nM. It demonstrates significant biological activity in modulating serotonin signaling pathways, making it useful in the study of psychiatric disorders. Cloroperone's inhibitory effects on the 5-HT2 receptor can aid in research focused on understanding the mechanisms underlying various neuropsychiatric conditions. -
5-HT Receptor Inhibitor
4-CAB hydrochloride is a potent 5-HT receptor inhibitor that acts as an analog of p-chloroamphetamine. It demonstrates significant inhibition of serotonin reuptake with an IC50 value of 330 nM, alongside dopamine reuptake inhibition with an IC50 of 2.3 μM. This compound is valuable for research focusing on serotonergic and dopaminergic neurotransmission, as well as investigations into the neuropharmacology of psychoactive substances. -
5-HT/NE Inhibitor
(R)-Indeloxazine benzenesulfonate is a potent inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake, exhibiting IC50 values of 0.35 μM and 3.3 μM, respectively. This compound demonstrates notable analgesic effects reminiscent of curative outcomes and may enhance nerve function by improving neurotrophic support. It is valuable for research applications focusing on pain management and the exploration of neurological disorders. -
5-HT Inhibitor
Femoxetine functions as a serotonin (5-HT) inhibitor, exhibiting potential antidepressant properties. By blocking the reabsorption of serotonin in nerve cells, it elevates serotonin concentrations in the synaptic cleft, thereby enhancing serotonin signaling. This compound is instrumental in researching the involvement of serotonin in depression and other affective disorders, as well as examining the effects of 5-HT reuptake inhibitors on mood regulation and behavioral responses. -
5-HT Receptor Inhibitor
5-IAI hydrochloride is a selective 5-HT receptor inhibitor that modulates serotonin signaling. This compound has been shown to significantly reduce serotonin uptake sites and decrease hippocampal serotonin levels in rat models. It serves as an important tool for research into serotonin-related pathways and their implications in neuropharmacology. -
5-HT Receptor Inhibitor
PF-05212377 is a selective inhibitor of the serotonin receptor 5-HT6. This compound serves as a substrate for the P-glycoprotein non-BCRP human transporter and demonstrates blood-brain barrier permeability in non-human primates. PF-05212377 holds potential for research applications related to Alzheimer's Disease, enabling exploration of its role in neurodegenerative mechanisms and therapeutic strategies. -
5-HT Receptor Inhibitor
DSP-6745 is a potent and orally active inhibitor of the 5-HT receptor. This compound exhibits significant biological activity in modulating serotonergic signaling, making it a valuable tool for research into depressive disorders. Its ability to selectively target 5-HT receptors enables the investigation of their role in mood regulation and related pathologies. -
5-HT/NA reuptake Inhibitor
5-HT/NA Reuptake Inhibitor-1 is a selective dual inhibitor of serotonin (5-HT) and norepinephrine (NA) reuptake, exhibiting IC50 values of 660 nM and 70 nM, respectively. This compound demonstrates favorable in vitro metabolic stability in humans, along with high hERG selectivity and passive membrane permeability. It is primarily utilized in research focused on mood disorders and neuropharmacology, providing valuable insights into the modulation of neurotransmitter systems. -
5-HT6R/MAO-B Inhibitor
5-HT6R/MAO-B modulator 1 is a selective antagonist of the 5-HT6 receptor with Gs signaling activity and serves as an irreversible inhibitor of monoamine oxidase B (MAO-B). This compound demonstrates glioprotective effects and has the capability to reverse memory deficits induced by scopolamine. Additionally, it features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a versatile tool for chemical biology applications. -
5-HT Inhibitor
Femoxetine hydrochloride is a selective serotonin (5-HT) inhibitor known for its antidepressant properties. By inhibiting the reuptake of serotonin, it elevates serotonin levels within the synaptic cleft, thereby enhancing serotonergic signaling. This compound is valuable in research focusing on the role of serotonin in mood regulation and its implications in depression and related emotional disorders. -
5-HT Receptor Inhibitor
Org 6582 is a competitive and selective inhibitor of the 5-HT receptor, demonstrating a Ki value of 89 nM. This compound exhibits a long-lasting inhibitory effect on serotonin uptake, persisting for over 48 hours. Org 6582 is primarily utilized in research focusing on depressive disorders, providing valuable insights into serotonergic modulation in various neuropsychological studies. -
5-HT Receptor Inhibitor
5-HT3-In-1 is a selective inhibitor of the 5-HT3 receptor, effectively blocking serotonin's action at this target. This compound demonstrates notable efficacy in inhibiting 5-HT3-mediated signaling pathways, making it valuable for research focused on neuropharmacology and gastrointestinal function. Its use extends to studying various conditions, including anxiety, depression, and nausea-related disorders. -
5-HT Reuptake Inhibitor
Ifoxetine hemisulfate is a selective inhibitor of the serotonin (5-HT) reuptake process in the central nervous system. By specifically targeting 5-HT transporters, it effectively blocks serotonin reuptake in the brain while sparing peripheral uptake in blood platelets. This compound shows promise for its antidepressant properties and is utilized in research focused on mood regulation and neuropharmacology. Additionally, Ifoxetine hemisulfate has been demonstrated to inhibit the uptake of radiolabeled 5-HT in rat brain synaptosomes, providing valuable insights into serotonin dynamics and receptor interactions. -
5-HT2C Inhibitor
SB 242084 monohydrochloride is a selective and high-affinity antagonist of the 5-HT2C receptor with a pKi value of 9.0. This compound effectively enhances the basal activity of dopaminergic neurons in the ventral tegmental area, stimulating dopamine release in the vomeronasal nucleus. Additionally, SB 242084 promotes mitochondrial gene expression and oxidative metabolism through 5-HT2A receptor interactions. Its potential applications in research include the investigation of negative symptoms associated with anxiety, depression, and schizophrenia, as well as the study of acute organ damage. -
Dopamine/5-HT Receptor Inhibitor
Loxapine hydrochloride is an orally active inhibitor of dopamine receptors and an antagonist of 5-HT receptors. This dibenzoxazepine compound exhibits significant antipsychotic properties, making it valuable for research into psychotropic effects and therapeutic interventions for schizophrenia and other psychiatric disorders. Its dual receptor activity contributes to its efficacy in modulating dopaminergic and serotonergic pathways. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole is a potent α2-adrenoceptor antagonist and 5-HT receptor reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is primarily utilized in research related to depression, facilitating studies on the modulation of serotonergic and adrenergic signaling pathways. Its unique pharmacological profile makes it a valuable tool for investigating potential therapeutic approaches in mood disorders. -
5-HT1A Receptor Inhibitor
LY 178210 is a selective partial agonist of the 5-HT1A receptor, exhibiting Ki values of 0.67 nM for 5-HT1A and 380 nM for 5-HT1D receptors, thereby demonstrating its specificity. Its minimal activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors makes it a valuable tool in neuropharmacology. Additionally, LY 178210 effectively inhibits forskolin-stimulated cyclase activity, though with lower potency compared to full agonists like 8-OH-DPAT. This compound is significant for studies on serotonergic modulation, as it markedly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the hypothalamus while increasing serum corticosterone concentrations. -
5-HT2A Receptor Inhibitor
Belaperidone is a selective 5-HT2A receptor inhibitor, demonstrating significant antidopaminergic and antiserotonergic properties. This compound is primarily employed in research related to neuropsychiatric disorders and may provide insight into therapeutic strategies for conditions such as schizophrenia and depression. Its mechanism of action makes Belaperidone a valuable tool in studying serotonin and dopamine receptor interactions within the central nervous system. -
5-HT2AR Inhibitor
5-HT2AR-IN-1 is a potent inhibitor of the 5-hydroxytryptamine 2A receptor (5-HT2AR) with demonstrated antidepressant activity. It effectively reduces both 5-HT2AR expression and serotonin transporter (SERT) protein levels. This compound is suitable for research into central nervous system disorders, including depression and addiction-related conditions, highlighting its potential in investigating therapeutic strategies for these ailments. -
5-HT Receptor Inhibitor
Citalopram hydrochloride is an orally active inhibitor of the 5-HT receptor, primarily functioning as a selective serotonin reuptake inhibitor (SSRI). This compound exhibits significant antidepressant activity and is widely utilized in research focused on depression and related mood disorders. Its mechanism aids in increasing serotonin levels in the synaptic cleft, making it a valuable tool for studying serotonin-related pathways and therapeutic interventions in psychiatric conditions. -
5-HT Reuptake Inhibitor
Ifoxetine is a selective inhibitor of the serotonin (5-HT) reuptake process, primarily targeting the central nervous system while sparing peripheral uptake in blood platelets. This compound effectively inhibits the uptake of radiolabeled 5-HT in rat brain synaptosomes, both in vitro and ex vivo. Due to its mechanism of action, Ifoxetine demonstrates potential antidepressant properties and can be utilized in research related to mood disorders and serotonin signaling. -
SERT Inhibitor/5-HT₂A receptor Antagonist
LY 367265 is a potent inhibitor of the serotonin transporter (SERT) with an IC₅₀ value of 3.1 nM and also serves as a selective antagonist for the 5-HT₂A receptor (Kᵢ = 0.81 nM). It displays minimal activity on the norepinephrine transporter (NET) and low affinity for other serotonin receptor subtypes, reinforcing its selectivity. LY 367265 enhances the efflux of [³H]5-HT in a concentration-dependent manner (EC₅₀ = 250 nM) and can counteract the contraction induced by Sumatriptan, indicating its antagonistic effects on 5-HT₁D-like receptors. This compound is valuable for research into neurological disorders, including anxiety and post-traumatic stress disorder. -
5-HT Deamination Inhibitor
RS 2232 is a competitive inhibitor of 5-hydroxytryptamine (5-HT) deamination, demonstrating a Ki of 0.054 μM. This compound selectively and reversibly inhibits type A monoamine oxidase, making it a valuable tool in neurological research. RS 2232 is utilized to gain insights into the role of serotonin metabolism in various brain functions and disorders. -
5-HT Receptor Inhibitor
Proxibarbal is a barbiturate derivative that acts as a selective inhibitor of the 5-HT receptor. It demonstrates notable anti-anxiety properties and is utilized in research focused on migraine headache mechanisms. This compound serves as a valuable tool for understanding serotonergic pathways and their implications in anxiety and migraine disorders.
