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.

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).

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.

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

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.

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.

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

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

(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.

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

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

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 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.

(+)-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.

Cendifensine functions as a monoamine reuptake inhibitor, targeting the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT).

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.

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).

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

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.

J-147 is an experimental drug with reported effects against both Alzheimer's disease and ageing in mouse models of accelerated aging. It is a curcumin derivative and a potent neurogenic and neuroprotective drug candidate initially developed for the treatment of neurodegenerative conditions associated with aging that impacts many pathways implicated in the pathogenesis of diabetic neuropathy.

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

MAO-A SERT-IN-1 acts as an inhibitor for both MAO-A and the serotonin transporter (SERT). It decreases the SERT-mediated reuptake of 5-HT and demonstrates neuroprotective properties in cellular inhibition models. Additionally, this compound has shown to alleviate depressive behaviors in both zebrafish and mice.