Biogenic Amine Transport Inhibitors
Mechanism of Action of Selective Monoaminergic Reuptake Inhibitors. During neurotransmission, monoamine neurotransmitters such as serotonin, dopamine or norepinephrine, are released into the synaptic cleft from storage vesicles present in the pre-synaptic neuron (A). The neurotransmitters then bind to their respective receptors on the post-synaptic neuron, thereby transferring the signal. The actions of the neurotransmitters are terminated via their reuptake into the pre-synaptic neuron via specific transporter proteins following which the neurotransmitter is taken up into the vesicles for re-release. When a monoaminergic reuptake inhibitor is present (B), it binds to the monoamine transporter and blocks the reuptake of the neurotransmitter whose levels increase in the synaptic cleft thereby enhancing neurotransmission.

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H3167 (2S,3S)-Hydroxybupropion hydrochloride ≥98% (HPLC) (2S,3S)-hydroxybupropion is a dopamine transporter (DAT) and norepinephrine transporter (NET) transporters inhibitor and nicotinic acetylcholine receptor (nAChR) family modulator. Hydroxybupropions were reported to contribute to antidepressant and perhaps smoking cessation activities. Both (2S,3S) and (2R,3R) metabolites reverse affective and somatic withdrawal signs in nicotine-dependent mice, but (2S,3S)-hydroxybupropion is more potent. (2S,3S)-hydroxybupropion significantly decreases the development of nicotine reward in mice.
    • T7947 (R)-Tomoxetine hydrochloride solid Norepinephrine uptake blocker.
    • SML0474 (S)-Duloxetine hydrochloride ≥98% (HPLC) Duloxetine hydrochloride is a dual serotonin/norepinephrine reuptake inhibitor (SNRI), widely used clinically as an antidepressant and anxiolytic.
    • SML0194   3,4-Methylenedioxypyrovalerone hydrochloride ≥98% (HPLC) 3,4-Methylenedioxypyrovalerone is a norepinephrine-dopamine reuptake inhibitor (NDRI) that acts as a CNS stimulant.
    3,4-Methylenedioxypyrovalerone is a norepinephrine-dopamine reuptake inhibitor (NDRI); CNS stimulant.
    3,4-Methylenedioxypyrovalerone is a derivative of pyrovalerone, a rapidly-absorbed psychostimulant. It belongs to the class of synthetic cathinones often used as performance-enhancing agent by athletes before being banned.
    • Q109 6-Nitroquipazine maleate salt solid Potent and selective serotonin transport blocker.
    • A8404 Amitriptyline hydrochloride ≥98% (TLC), powder Tricyclic antidepressant; inhibits the norepinephrine and serotonin transporters with Kis of 100 nM and 14.7 nM, respectively; high in vitro affinity for α1-adrenoceptors, serotonin and muscarinic acetylcholine receptors.
    • A129 Amoxapine Tricyclic antidepressant; inhibits uptake of norepinephrine; inhibits 5-HT2 serotonergic receptors.
    • B138 BTCP hydrochloride BTCP is a potent and selective blocker of dopamine transport with little affinity for phencyclidine sites.
    • SML0847 Benztropine mesylate ≥98% (HPLC) Benztropine mesylate is a centrally acting muscarinic acetylcholine receptor antagonist and dopamine transporter (DAT) inhibitor (IC50 = 118 nM). Benztropine mesylate has been used to treat the symptoms of Parkinson′s disease and is currently in clincial trials for chronic back pain.
    Benztropine mesylate serves as an inhibitor of breast cancer stem cells (BCSCs) in vitro and in vivo. It can help in improving the efficacy of chemotherapy in vitro. It is considered as an anti-cancer stem cell (CSC) drug, which can modify tumorigenic properties.
    • B102 Bupropion hydrochloride ≥98% (HPLC), solid Bupropion possesses antidepressant and anxiolytic properties. It serves as a good auxiliary for people who makes an effort to give up smoking. It may also be used in the treatment for attention-deficit hyperactivity disorder.
    Inhibits the dopamine and norepinephrine transporters with Kis of 2.8 μM and 1.4 μM, respectively. Does not inhibit the serotonin transporter (Ki = 45 μM). Antidepressant.
    • PZ0125 CP-53631 ≥98% (HPLC) CP-53631 is a selective serotonin reuptake inhibitor (SSRI); antidepressant.
    • C7861 Citalopram hydrobromide ≥98% (HPLC) Potent and selective serotonin uptake inhibitor (Ki = 5.4 nM); antidepressant
    • C7291 Clomipramine hydrochloride ≥98% (HPLC), powder Clomipramine hydrochloride (CLP) is a amphiphilic drug, with two benzene rings in its structure. It exhibits anti-depressant property by restoring the equilibrium of certain natural materials in the human being. CLP acts as a potential therapeutic for obsessive compulsive disorder.
    Tricyclic antidepressant; inhibits serotonin and norepinephrine transporters.
    • D3900 Desipramine hydrochloride ≥98% (TLC), powder Desipramine is used to treat depression. It is also used to manage enuresis in children. Desipramine helps to eliminate the pain triggered by diabetic neuropathy.
    Tricyclic antidepressant that is a more potent inhibitor of the norepinephrine transporter (Ki = 4 nM) than the serotonin transporter (Ki = 61 nM).
    • D2069 Desvenlafaxine hydrochloride ≥98% (HPLC), powder Desvenlafaxine hydrochloride is a dual SERT/NET reuptake inhibitor. It is a major active metabolite of venlafaxine (#542); brain penetrant; Ki = 40 nM and 122 nM for hSERT and hNET, respectively (weak binding at the hDAT). Inhibition of [3H]5-HT or [3H]NE uptake for the hSERT or hNET produced IC50 values of 47 and 531 nM.
    Desvenlafaxine hydrochloride is a psychoactive drug. Incidence of this drug in environmental samples might induce in vitro gene expression associated with neurological disorders.
    • D4526 Doxepin hydrochloride ~85% E-isomer basis, ≥98% (GC), 15% Z-isomer basis, powder Tricyclic antidepressant that is a more potent inhibitor of norepinephrine uptake than of serotonin uptake; antagonist at H1 histamine, muscarinic cholinergic, and α-adrenoreceptors.
    • E4786 Escitalopram oxalate ≥98% (HPLC), powder Escitalopram is a selective serotonin reuptake inhibitor (SSRI), the S-enantiomer and eutomer of citalopram.
    • F132 Fluoxetine hydrochloride solid Fluoxetine hydrochloride is a selective serotonin reuptake inhibitor and functions as an antidepressant. This drug works at presynaptic terminals where it prevents the reuptake of serotonin, resulting in the accumulation of serotonin in extracellular fluid at synapses.
    Selective serotonin reuptake inhibitor; antidepressant.
    • F2802 Fluvoxamine maleate solid Fluvoxamine maleate is a selective neuronal serotonin reuptake inhibitor. It functions as an antidepressant and anti-obsessive agent. It is useful in treating obsessive compulsive disorder and panic disorder.
    • D052 GBR 12909 dihydrochloride solid, ≥98% (HPLC) Highly selective dopamine reuptake inhibitor with behavioral effects similar to cocaine.
    • G9659 GBR 12935 dihydrochloride ≥98% (TLC), powder GBR 12935 inhibits the dopamine and norepinephrine transporters with Kis of 21.5 nM and 225 nM, respectively. It does not inhibit the serotonin transporter (Ki = 6.5 mM). GBR 12935 binds to a nondopaminergic piperazine site in blood platelets and brain that has been identified as cytochrome P450.
    • SML0851   GZ-793A ≥98% (HPLC) GZ-793A is a selective inhibitor of vesicular monoamine transporter 2 (VMAT2), which transports the monoamine neurotransmitters from cellular cytosol into synaptic vesicles. GZ-793A is 50-fold selective for VMAT over the serotonin or dopamine transporters. VMAT2 has recently been considered a target for the treatment of methamphetamine abuse. In rat studies, GZ-793A decreased self-administration of methamphetamine with no development of tolerance.
    • I7379 Imipramine hydrochloride ≥99% (TLC) Tricyclic antidepressant; inhibits the serotonin and norepinephrine transporters with Kis of 7.7 nM and 67 nM, respectively. Has little effect on the dopamine transporter (Ki = 25 μM).
    • I119 Indatraline hydrochloride solid Indatraline is a non-selective monoamine transport inhibitor. It inhibits the reuptake of neurotransmitters, such as serotonin, norepinephrine and dopamine. It exhibits anti-depressant and anti-angiogenic effects. Indatraline also plays a role in inducing autophagy.
    • M9651 Maprotiline hydrochloride >99% (HPLC), powder Maprotiline is a tetracyclic agent. It possesses inhibitory effects against the uptake of norepinephrine by nerve cells. Maprotiline exhibits anti-depressant and sedative activity.
    • M2017 Mazindol ≥98% (TLC), powder Anorectic agent; inhibits the dopamine, norepinephrine and serotonin transporters with Kis of 27.6 nM, 3.2 nM, and 153 nM, respectively.
    • M0443 Mirtazapine ≥98% (HPLC) Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA). Mirtazapine agonizes selective adrenergic and serotonergic receptors so that both NE release and 5-HT1A mediated serotonergic signaling are increased.
    • N5536 Nefazodone hydrochloride ≥98% (HPLC), solid Novel antidepressant; mixed 5-HT2A serotonin receptor antagonist/serotonin uptake inhibitor.
    • SML0909 Nefopam hydrochloride ≥98% (HPLC) Nefopam is a centrally-acting analgesic drug of the benzoxazocine chemical class. Nefopam is a non-opioid, but has a potentiating effect on morphine and other opioids. Its mechanism of action is not certain, but may involve its action as a dopamine/serotonin/norepinephrine reuptake inhibitor.
    • N151 Nisoxetine hydrochloride solid, ≥98% (HPLC) Potent and selective inhibitor of the norepinephrine transporter (Ki = 5.1 nM).
    • N1530 Nomifensine maleate salt Nomifensine maleate is a selective dopamine uptake inhibitor interacting with the dopamine transporter, at a site different from that of cocaine; antidepressant. Nomifensine serves as an antidepressant and is known to cause frequent hemolytic anemia. The aniline group in this compound results in blood and liver toxicities.
    • N7261 Nortriptyline hydrochloride ≥98% (TLC), powder Tricyclic antidepressant that is a more potent inhibitor of the norepinephrine transporter (Ki = 3.4 nM) than the serotonin transporter (Ki = 161 nM). 5-HT2 serotonin receptor antagonist.
    • P9623 Paroxetine hydrochloride hemihydrate ≥98% (HPLC), powder Paroxetine hydrochloride hemihydrate is one of the most potent and selective of the selective serotonin reuptake inhibitors (SSRI); antidepressant
    Paroxetine is a phenylpiperidine derivative. It has the ability to cross placenta. Paroxetine is known to increase the risk of congenital cardiac malformations. It might be useful in hormone replacement therapy for treating vasomotor symptoms during menopause. It is known to ameliorate the effects of panic disorder, obsessive‐compulsive disorder and social phobia.
    • P8813 Protriptyline hydrochloride ≥99% (TLC), powder Norepinephrine uptake blocker.
    • F1678 R-(−)-Fluoxetine hydrochloride >98% (HPLC), solid Selective serotonin reuptake inhibitor.
    • R6527 Reboxetine mesylate hydrate >96% (HPLC), solid Reboxetine mesylate hydrate is a selective noradrenaline uptake inhibitor.
    • F1553 S-(+)-Fluoxetine hydrochloride ≥98% (HPLC), solid Fluoxetine hcl (hydrochloride) is a selective serotonin reuptake inhibitor and functions as an antidepressant. This drug works at presynaptic terminals where it prevents the reuptake of serotonin, resulting in the accumulation of serotonin in extracellular fluid at synapses.
    Selective serotonin reuptake inhibitor.
    • SML1597   SRI-29574 ≥98% (HPLC) DAT is crucial for regulating the levels of DA (dopamine). It is also responsible for the reuptake of 1-methyl-4-phenylpyridinium (MPP+), neurotoxin which mediates symptoms similar to Parkinson’s disease. Changes in DAT activity is associated with attention-deficit/hyperactivity and autism spectrum disorders.
    SRI-29574 is a potent DAT (dopamine transporter) allosteric modulator that partially inhibits DAT uptake without affecting binding to DAT. SRI-29574 is a noncompetitive inhibitor of [3H]DA uptake. Also SRI-29574 partially inhibits SERT and NET uptake.
    • S9944 Sibutramine hydrochloride monohydrate ≥98% (HPLC), solid Sibutramine is a serotonin and noradrenaline reuptake inhibitor (SNRI). It is an antiobesity drug, which decreases calorie intake and increases energy expanditure. Sibutramine antagonizes MPTP-induced dopamine depletion in mouse brain.
    • T1692 Tianeptine sodium salt hydrate ≥98% (HPLC), powder Tianeptine is a tricyclic antidepressant that enhances serotonin uptake. This drug can affect neuroprotection, neuronal excitability, memory and anxiety. However, tianeptine is not linked to adverse psychomotor, cognitive, cardiovascular, sleep and bodyweight effects. The drug has a low tendency for abuse and has a positive pharmacokinetic profile.
    Tianeptine is least involved in drug interaction as it is not metabolized by cytochrome P450 system in the liver. In hippocampus and amygdala, tianeptine is involved in glutamatergic transmission processes and elicits neuroplasticity.
    • T6154 Trazodone hydrochloride ≥99% (HPLC), powder Antidepressant that potentiates the activity of serotonin uptake blockers and has full 5-HT2C serotonin receptor agonist activity. It is metabolized to the 5-HT1 serotonin receptor agonist 1-(3-Chlorophenyl)piperazine.
    • T3146 Trimipramine maleate salt ≥98% (TLC), powder Antidepressant; serotonin transport blocker that also blocks norepinephrine uptake.
    • V7264 Venlafaxine hydrochloride ≥98% (HPLC), powder Venlafaxine is an antidepressant. The mechanism of the antidepresant action of venlafaxine in humans is associated with its potentiation of neurotransmitter activity in the CNS. Venlafaxine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and weak inhibitor of dopamine reuptake. Venlafaxine has no significant activity for muscarinic, histaminergic, or α-1 adrenergic receptors in vitro. Venlafaxine does not possess MAO inhibitor activity.
    • SML1098 Vilazodone hydrochloride ≥98% (HPLC) Vilazodone is a serotonin 5-HT1A partial agonist and serotonin-selective reuptake inhibitor (SPARI) that is used clinically as an antidepressant for major depressive disorder.
    • Z101 Zimelidine dihydrochloride solid Serotonin transport blocker; antidepressant.
    • C124 β-CFT naphthalenedisulfonate monohydrate solid Cocaine analog that inhibits the dopamine, norepinephrine, and serotonin transporters with Kis of 26.1 nM, 31.9 nM, and 127 nM, respectively. [11C]-β-CFT and [18F]-β-CFT are ligands for PET imaging of the dopamine transporter in vivo.