Monoamine Transporter

Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.

Reserpine (Serpalan) is an alkaloid isolated from the root of Rauwolfia serpentina. As an inhibitor of vesicular monoamine transporter 2 (VMAT2), it suppresses the uptake of norepinephrine into storage vesicles, leading to depletion of catecholamines and serotonin in central and peripheral nerve terminals. It has antihypertensive and antipsychotic effects and can be used to induce gastric ulcer and depression models.

FFN 206 dihydrochloride is a fluorescent VMAT2 substrate that can be used to detect VMAT2 subcellular sites in cell culture and shows no detectable inhibition of DAT.

Tetrabenazine Metabolite ((-)-β-HTBZ), a vesicles monoamine transporter 2 (VMAT2) inhibitor, is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite has a high affinity for VMAT2 with a Ki of 13.4 nM. Tetrabenazine Metabolite is often used to study chorea associated with Huntington's disease and other hyperactivity disorders.

NBI-98782 ((+)-α-DHTBZ) is an inhibtior of vesicular monoamine transporter (VMAT2) (Ki: 0.97 nM)

Liafensine(BMS-820836) is a novel and selective triple monoamine reuptake inhibitor with inhibitory effects on the reuptake of serotonin, norepinephrine, and dopamine for the study of major depressive disorder and central nervous system disorders.

Xanthoangelol, which can be extracted from Angelica keiskei, inhibits obesity-induced inflammatory responses.Xanthoangelol has antimicrobial activity, inhibits monoamine oxidase, and induces apoptosis in neuroblastoma and leukemia cells.

Diclofensine (Ro 8-4650) is a monoamine reuptake inhibitor that blocks dopamine (IC50=0.74 nM), norepinephrine (IC50=2.3 nM), and 5-hydroxytryptophan (IC50=3.7 nM) in synaptosomes of the rat brain. dAURK-4 hydrochloride is an inhibitor of dopamine (IC50=0.74 nM), norepinephrine (IC50=2.3 nM) and 5-hydroxytryptophan (IC50=3.7 nM).

Valbenazine (NBI-98854), a highly selective vesicular monoamine transporter 2(VMAT2) inhibitor, is approved for the treatment of tardive dyskinesia.

Tetrabenazine (Ro 1-9569) is a former antipsychotic drug used to treat various movement disorders. It inhibits neurotransmitter uptake into adrenergic storage vesicles and serves as a high-affinity label for the vesicle transport system.

Rose Bengal sodium is a potent inhibitor of VGlut and vesicular monoamine transporter (VMAT) (Ki of 19 and 64 nM for VGlut andVMAT, respectively）

TC-T 6000 (hENT4-IN-1) is a selective and potent inhibitor of human equilibrium nucleoside transporter protein 4 (ENT4) (IC50: 74.4 nM) with vasodilator activity, inhibits hENT1 and hENT2, and can be used for the study of cancer and cardiovascular injury.

(+)-Kavain ((R)-KAWAIN) is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.

Decynium 22 is a plasma membrane monoamine transporter (PMAT) inhibitor

Reserpine hydrochloride is the salt form of Reserpine and acts as an inhibitor of vesicular monoamine transporter 2 (VMAT2). It blocks the uptake of norepinephrine into storage vesicles, leading to the depletion of catecholamines and serotonin at central and peripheral nerve terminals. It has antihypertensive and antipsychotic properties and is commonly used to induce models of gastric ulcer and depression.

Nisoxetine hydrochloride is a noradrenaline transporter (NET) inhibitor

(+)-Tetrabenazine ((3R,11bR)-Tetrabenazine) is a reversible vesicular monoamine transporter 2 (VMAT-2) inhibitor, inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.

(2R,3S,11bS)-9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido[2,1-a]isoquinolin-2-ol is an impurity of Tetrabenazine, which is a VMAT inhibitor used in the treatment of hyperkinetic movement disorder.

Tetrabenazine Racemate (Rubigen) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2). Tetrabenazine Racemate blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high-affinity label for the vesicle transport system.

Fluorescent false neurotransmitter (FFN)

FFN 511 hydrochloride is a fluorescent pseudo-neurotransmitters (FFNs) targeting neuronal vesicular monoamine transporter 2 (VMA T2).FFN 511 hydrochloride inhibits the binding of 5-hydroxytryptamine to VMA T2-containing membranes and can be used for labelling of dopaminergic nerve endings in acute slices of in vivo cortex-striatum. The excitation and emission maxima are 406 and 501 nm, respectively.

Cavα2δ1&NET-IN-1 inhibits Ca(v)α2δ-1 with a K(i) of 112 nM and inhibits NET with a K(i) of 383 nM and IC(50) of 67 nM. Cavα2δ1&NET-IN-1 can be used for research on pain.

FFN246, a fluorescent probe, concurrently targets the serotonin transporter (SERT) and vesicular monoamine transporter 2 (VMAT2), exhibiting excitation and emission spectra at 392/427 nm, respectively. It serves to label serotonergic neurons within mouse brain tissue via SERT-dependent accumulation [1].

NMDAR antagonist 5 (Compound A17) is a multi-target antagonist that acts on NMDAR and monoamine transporters (SERT, DAT, and NET). It demonstrates strong NMDAR antagonistic efficacy (IC50= 0.3 μM) and effective activity on monoamine transporters (SERT IC50= 1.1 μM, DAT IC50= 0.7 μM, NET IC50= 2.7 μM). NMDAR antagonist 5 exhibits high safety with low toxicity (hepatic and renal toxicity IC50> 100 μM; cardiac toxicity IC50= 24.5 μM). It has antidepressant properties and is useful for depression research.