Serotonin Transporter

Fluoxetine (LY-110140) is a highly specific serotonin uptake inhibitor and selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. Fluoxetine has antidepressant activity.

Fluoxetine hydrochloride (Lilly110140) is the first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist that binds to DREADD receptor subtypes [hM3Dq] and [hM4Di] with Ki values of 6.3 nM and 4.2 nM, respectively.

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

WAY-260022 is an orally available and selective norepinephrine transporter protein inhibitor that displays inhibitory effects on serotonin and dopamine transporter proteins.

Clovoxamine (DU 23811) is a 5-hydroxytryptamine reuptake, serotonin and norepinephrine inhibitor with antidepressant and anticonvulsant activity.

Sertraline hydrochloride (Sertraline HCl) is a selective serotonin uptake inhibitor that is used in the treatment of depression.

Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.

Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a thiophene derivative and selective neurotransmitter uptake inhibitor for serotonin and noradrenaline (SNRI). It is an antidepressant agent and anxiolytic, also used for treating pain in patients with diabetes mellitus and fibromyalgia.

Dextromilnacipran (Levomilnacipran) is a selective serotonin and norepinephrine reuptake inhibitor.

Duloxetine is an inhibitor of serotonin-norepinephrine reuptake(Ki of 4.6 nM),with treatment of major depressive disorder and generalized anxiety disorder.

Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.

Paroxetine is a inhibitor of serotonin uptake that is effective in the treatment of depression.

Vortioxetine (Lu AA 21004) is a serotonergic antidepressant used for major depression disorders. Vortioxetine has been associated with a low rate of minor serum aminotransferase elevations during treatment.

Venlafaxine (Wy 45030), an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), is used to treat major generalised anxiety disorder (GAD), depressive disorder (MDD), panic disorder and social phobia.

Fluvoxamine maleate (DU-23000 (maleate)) is a selective serotonin reuptake inhibitor that is used in the treatment of depression and a variety of anxiety disorders.

Imipramine hydrochloride (Imipramine HCl) is a first generation tricyclic antidepressant that acts primarily as an inhibitor of serotonin and norepinephrine transporters (Kds = 1.4 and 37 nM, respectively).Imipramine hydrochloride is reported to prevent the translocation of aSMase, inhibiting MV and exosomes secretion

Desipramine hydrochloride (Norimipramine) ,a secondary amine tricyclic antidepressant (TCA), is the hydrochloride salt form of desipramine. In the central nervous system (CNS), Desipramine hydrochloride blocks the re-uptake of neurotransmitters, including norepinephrine and serotonin. This leads to an increase in the amount of these neurotransmitters in the synaptic cleft and prolongs their activities postsynaptically.

Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that inhibits dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

Vilazodone Hydrochloride (EMD 68843) , a partial agonist of 5-HT1A receptors and specific serotonin reuptake inhibitor (SSRI), is utilized in treating of the major depressive disorder.

Escitalopram Oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Venlafaxine hydrochloride (Wy 45030 hydrochloride) is a cyclohexanol and phenylethylamine derivative functioning as a serotonin and noradrenaline reuptake inhibitor (SNRI) used as an antidepressive agent.

Nitroxazepine (CIBA 2330Go) is a serotonin-norepinephrine reuptake inhibitor, and treatment depression. Nitroxazepine is a tricyclic antidepressant (TCA) for the research of depression

Amitifadine hydrochloride (EB-1010 hydrochloride) is a triple reuptake inhibitor (TRI) or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).

Vortioxetine hydrobromide (Lu AA21004 hydrobromide) is a serotonin (5-HT) modulator and stimulator (SMS), inhibits 5-HT1A 1B 3A 7 receptor and SERT (IC50: 15 33 3.7 19 1.6 nM).

Citalopram hydrobromide (XU-62-320) , a selective serotonin reuptake inhibitor (SSRI), selectively inhibits the CNS neuronal reuptake of serotonin, thereby potentiating serotonergic activity in the central nervous system (CNS). Citalopram hydrobromide is the orally bioavailable hydrobromide salt of the racemic bicyclic phthalene derivative citalopram with antidepressant activity. This agent has minimal effects on the CNS neuronal reuptake of norepinephrine (NE) and dopamine (DA).

Clomipramine hydrochloride (Anafranil) is a tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.

Centanafadine hydrochloride (EB-1020 hydrochloride) is a dual inhibitor of norepinephrine (NE) dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter).

Ketanserin tartrate (KJK-945 tartrate) is a 5-HT2A receptor and α1-adrenergic receptor antagonist with antihypertensive activity, inhibits serotonin-induced vasoconstriction and platelet activation, and can be used in the study of systemic sclerosis.

Gentisein (NSC-329491), a primary metabolite of Mangiferin, exhibits significant inhibition of serotonin uptake, demonstrating potency with an IC50 value of 4.7 µM[1][2].

(Z)-Thiothixene (Thiothixene) is an antagonist of serotonergic receptor.

Milnacipran hydrochloride (Savella) is a serotonin and norepinephrine reuptake inhibitor used to treat major depressive disorders. Milnacipran hydrochloride is an enantiomer of milnacipran, which is used to treat fibromyalgia. Milnacipran hydrochloride and milnacipran have been associated with a low rate of transient elevations in serum aminotransferase levels during treatment and with rare instances of clinically apparent acute liver injury with jaundice.

Dapoxetine hydrochloride (LY-210448 hydrochloride) is a selectivity short-acting serotonin reuptake inhibitor, used for the therapy of premature ejaculation.

Desvenlafaxine (O-Desmethylvenlafaxine) is a cyclohexanol and phenol derivative and metabolite of venlafaxine that functions as a serotonin and noradrenaline reuptake inhibitor (SNRI) and is used as an antidepressive agent.

Desvenlafaxine succinate hydrate (WY 45233 Succinate) is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).

ZZL-7 is a fast-onset antidepressant agent that disrupts the interaction between neuronal nitric oxide synthase (nNOS) and the serotonin transporter (SERT) in the dorsal raphe nucleus (DRN). It easily crosses the blood-brain barrier and has research value in major depressive disorder (MDD).

PF-00217830 is a serotonin 1A receptor agonist, dopamine D2 receptor agonist, and serotonin 2A receptor antagonist.PF-00217830 may be used in the study of schizophrenia.

Milnacipran (1S-cis) hydrochloride (Levomilnacipran Hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (SNRI), treatment of fibromyalgia.

MAO-B-IN-9 is a monoamine oxidase B MAO-B inhibitor (IC50: 0.18 μM) that crosses the blood-brain barrier with potency, selectivity and time-dependence. MAO-B-IN-9 has neuroprotective effects against Aβ1-42-induced neuronal cell death, which may be related to the anti-aggregation effect of Aβ1-42.

Tedatioxetine (Lu AA24530) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) with antidepressant properties.Tedatioxetine acts as a CYP2D6 substrate.

Azaphen (Pipofezin hydrochloride) is the reuptake of serotonin inhibitor.with antidepressant action and has sedative effects, suggesting antihistamine activity.

DOV-216,303 Free Base (DOV-216303) is an inhibitor of serotonin, norepinephrine, and dopamine reuptake with with IC50s of 14, 20 and 78 nM. DOV-216,303 Free Base exhibits antidepressant effects.

Phenelzine is an antidepressant and mania drug, which is a monoamine oxidase inhibitor. Its antidepressant effect is similar to that of niacinamide. It can reduce the degradation of catecholamines (norepinephrine, dopamine, and serotonin) in the brain and increase the content of catecholamines. , and play an antidepressant effect. It has a good effect on endogenous depression but has a poor effect on exogenous and reactive depression.

MAO-A SERT-IN-1 acts as an inhibitor for both MAO-A and the serotonin transporter (SERT). It decreases the SERT-mediated reuptake of 5-HT and demonstrates neuroprotective properties in cellular inhibition models. Additionally, this compound has shown to alleviate depressive behaviors in both zebrafish and mice.