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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C155 (−)-2β-Carbomethoxy-3β-(4-iodophenyl)nortropane crystalline 5-HT serotonin transporter inhibitor; precursor of [123I]nor-β-CIT, a radioligand for SPECT imaging of the 5-HT transporter.
    • H3167 (2S,3S)-Hydroxybupropion hydrochloride ≥98% (HPLC) (2S,3S)-hydroxybupropion is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator. (2S,3S)-hydroxybupropion is a major metabolite of bupropion. 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) New 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.
    • Q109 6-Nitroquipazine maleate salt solid Potent and selective serotonin transport blocker.
    • A164 Alaproclate hydrochloride Potent and selective serotonin uptake inhibitor.
    • 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 solid Potent and selective blocker of dopamine transport with little affinity for phencyclidine sites.
    • B102 Bupropion hydrochloride ≥98% (HPLC), solid 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 solid Potent and selective serotonin uptake inhibitor (Ki = 5.4 nM); antidepressant
    • C7291 Clomipramine hydrochloride ≥98% (HPLC), powder Tricyclic antidepressant; inhibits serotonin and norepinephrine transporters.
    • D3900 Desipramine hydrochloride ≥98% (TLC), powder 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.
    • 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 Selective serotonin reuptake inhibitor; antidepressant.
    • F2802 Fluvoxamine maleate solid Selective serotonin reuptake inhibitor; antidepressant.
    • 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 Inhibits the dopamine and norepinephrine transporters with Kis of 21.5 nM and 225 nM, respectively. Does not inhibit the serotonin transporter (Ki = 6.5 μM). Binds to a nondopaminergic piperazine site in blood platelets and brain that has been identified as cytochrome P450.
    • G120 GYKI 52895 solid Selective dopamine uptake inhibitor; antiparkinsonian; antidepressant.
    • I7379 Imipramine hydrochloride ≥99% (TLC), crystalline 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 Potent inhibitor of dopamine, norepinephrine and serotonin uptake.
    • L8792 Lofepramine hydrochloride ≥98% (HPLC), solid Lofepramine is an antidepressant; serotonin and norepinephrine re-uptake inhibitor (SNRI).
    • M9651 Maprotiline hydrochloride >99% (HPLC), powder Selective norepinephrine uptake inhibitor.
    • 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.
    • N151 Nisoxetine hydrochloride solid, ≥98% (HPLC) Potent and selective inhibitor of the norepinephrine transporter (Ki = 5.1 nM).
    • N1530 Nomifensine maleate salt Selective dopamine uptake inhibitor interacting with the dopamine transporter at a site different from that of cocaine; antidepressant.
    • F133 Norfluoxetine hydrochloride ≥97%, solid Fluoxetine metabolite; more potent inhibitor of serotonin uptake than fluoxetine with a half-life in vivo of 5-7 days.
    • 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
    • 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 Selective serotonin reuptake inhibitor.
    • 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 Tricyclic antidepressant; enhances serotonin uptake.
    • 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.
    • 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.