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.

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)

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

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.

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.

Reserpine (Serpalan) is an alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.

Nisoxetine hydrochloride is a noradrenaline transporter (NET) inhibitor

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

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

(+)-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.

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.

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.

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 tosylate, the tosylate salt of valbenazine, is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki value of 150 nM while displaying no significant binding to VAMT1(Ki<10 μM).

VMAT2-IN-2 tosylate is a potent inhibitor of VMAT2, applicable in tardive dyskinesia research [1].