Serotonin Transporter Inhibitor

Fluoxetine (LY-110140 free base) is a selective serotonin reuptake inhibitor (SSRI) class used for antidepressant research.

Fluoxetine hydrochloride (LY 110140) is an antidepressant and a selective serotonin reuptake inhibitor.

Sertraline hydrochloride is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. Sertraline hydrochloride is researched for a number of diseases, such as major depressive disorder and obsessive.

Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial agonist of 5-HT_1B (K_i: 15 nM, 33 nM).

Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

RPI-GLYT2-82 is a reversible, blood-brain barrier-permeable allosteric inhibitor of GlyT2 with an IC₅₀ value of 554 nM. RPI-GLYT2-82 also exhibits inhibitory activity against 5-HT2AR and SERT, with IC₅₀ values of 1.9 μM and 4.7 μM, respectively. RPI-GLYT2-82 inhibits pain signals and alleviates allodynia, shows no target-related side effects at the maximum analgesic dose, and has no addictive potential. RPI-GLYT2-82 can be used for the research of neuropathic pain.

SERT-IN-4 is a brain-penetrant and orally active SERT inhibitor and ERβ agonist with human SERT IC₅₀ of 16.92 nM and human ERβ EC₅₀ of 3.66 nM. SERT-IN-4 inhibits SERT-mediated substrate transport, increases hippocampal serotonin levels, modulates p-CREB and BDNF expression.SERT-IN-4 reduces immobility in CUMS mice, improves social interaction and reduces inactivity in CSDS mice.SERT-IN-4 can be used for the research of major depressive disorder.

nNOS-PDZ-IN-1 is an orally active, blood-brain barrier-penetrant inhibitor of neuronal nitric oxide synthase-PDZ domain (nNOS-PDZ), with an IC₅₀ of 0.76 μM and a K_D of 0.55 μM. nNOS-PDZ-IN-1 binds to the nNOS-PDZ domain, occupies its binding site and disrupts its interaction with the serotonin transporter. nNOS-PDZ-IN-1 exhibits antidepressant activity without addiction potential or movement-related side effects. nNOS-PDZ-IN-1 can be used in research related to major depressive disorder.

Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC₅₀ value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects.

Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC₅₀ value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects.

Paroxetine (BRL29060) hydrochloride is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine hydrochloride inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine hydrochloride is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine hydrochloride is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a K_i of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).

Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT₁A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.

Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM).

Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission.

Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K_i = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a K_i 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.

Fluvoxamine (DU-23000) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.

Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a K_i 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.

Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.