monoaminetransporter

Fostamatinib (R788) is a small-molecule inhibitor and an oral prodrug of R406, a Syk/FLT3-targeted inhibitor (IC50 = 41 nM) that also inhibits Lyn (IC50 = 63 nM) and Lck (IC50 = 37 nM), featuring oral activity and cell permeability, used for the treatment of immune thrombocytopenia.

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.

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).

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.

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.

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)

(+)-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.

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.

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).

Nisoxetine hydrochloride is a noradrenaline transporter (NET) inhibitor

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.

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

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

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.

Trans (2,3)-Dihydrotetrabenazine is a Tetrabenazine metabolite, shows inhibition activity on vesicular monoamine transporter (VMAT2).

Tetrabenazine-D6 is a deuterated derivative of tetrabenazine that can be used in research related to Huntington’s disease and other hyperkinetic disorders.

Vanillylpyruvic acid is a phenylpyruvic acid derivative applicable in biochemical experiments and drug synthesis research.

3,4-Dihydroxypyrovalerone HCl is an analog of Pyrovalerone. Pyrovalerone inhibits the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET).

4-Methylamphetamine hydrochloride is a 5-HT1A receptor agonist that induces a decrease in body temperature in rats by binding to the 5-HT1A receptor. Additionally, it increases the extracellular levels of neurotransmitters norepinephrine (NE), dopamine (DA), and serotonin (5-HT) by affecting their transporters. 4-Methylamphetamine hydrochloride is applicable in the study of neurological disorders.

N-Methyl-2-phenylpropan-1-amine hydrochloride is an analogue of β-methylphenethylamine (BMPEA) and demonstrates neurotransmitter-releasing properties in experiments involving NET and DAT.

3-Bromoamphetamine hydrochloride is a para-substituted amphetamine that functions as a monoamine releaser.

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.

(2S,3S,11bR)-Dihydrotetrabenazine ((2S,3S,11bR)-DHTBZ) is a highly selective inhibitor of vesicular monoamine transporter 2 (VMAT2) with a Ki value of 593 nM. It suppresses the vesicular transport of monoamine neurotransmitters, such as dopamine and serotonin, leading to reduced release into the synaptic cleft. This compound holds potential for research in Huntington's disease and other hyperkinetic movement disorders.