Monoamine Transporter

Related Products

Monoamine transporters (MATs) belong to the solute carrier 6 (SLC6) family of human transporters, which, in turn, is a subfamily of the broader neurotransmitter:sodium symporters (NSSs) that comprise transporters from prokaryotic to human. MATs comprise three main members-the dopamine (DA) transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). MATs regulate neurotransmission via the reuptake of dopamine, serotonin and norepinephrine from extra-neuronal regions and thus maintain neurotransmitter homeostasis.

MATs are transmembrane proteins located in plasma membranes of monoaminergic neurons. These proteins use ion (Na⁺, Cl⁻) gradients as energy sources to move monoamines into or out of neurons. In the membrane of intracellular synaptic vesicles is the vesicular monoamine transporters 1 and 2 (VMAT1 and VMAT2), which use a proton gradient as the energy source to sequester cytosolic monoamines into the vesicles and then release the monoamines into synaptic cleft by exocytosis. Dysregulation of MATs has been linked to depression, anxiety disorder, attention-deficit-hyperactivity disorder, obsessive-compulsive disorder, substance-use disorders, epilepsy, Parkinson’s disease and autism-spectrum disorder. Thus, MATs serve as pharmacological targets for several neuropsychiatric and neurodegenerative disorders.

Monoamine Transporter Inhibitors (23)

Monoamine Transporter Related Products (27):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-148862

Cavα2δ1&NET-IN-1	Inhibitor
Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Ca_vα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Ca_vα2δ-1 with a K_i of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a K_i of 383 nM and IC₅₀ of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain.

HY-16771A

Valbenazine tosylate	Inhibitor
Valbenazine tosylate (NBI-98854 tosylate) is a vesicular monoamine transporter 2 (VMAT2) inhibitor with the K_i of 110-190 nM.

HY-103465

FFN511	Inhibitor
FFN511 is a potent fluorescent false neurotransmitters (FFNs) that targets neuronal vesicular monoamine transporter 2 (VMA T2). FFN511 inhibits serotonin binding to VMA T2-containing membranes with an IC₅₀ of 1 µM. FFN511 directly images the dynamics of release during exocytosis, can be used to label dopamine terminals in live cortical-striatalacute slices.

HY-G0025

Tetrabenazine Metabolite	Inhibitor
Tetrabenazine Metabolite is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a high affinity (K_i=13.4 nM). Tetrabenazine Metabolite is be developed for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders.

HY-153472

VMAT2-IN-2 tosylate	Inhibitor
VMAT2-IN-2 tosylate is a potent VMAT2 inhibitor. VMAT2-IN-2 tosylate can be used in research of tardive dyskinesia.

HY-15793A

Trans (2,3)-Dihydrotetrabenazine	Inhibitor
Trans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2).

HY-N7506

13-Hydroxyisobakuchiol	Inhibitor
Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC₅₀=0.58 μM) and norepinephrine transporter (NET) (IC₅₀=0.69 μM) than for the serotonin transporter (SERT) (IC₅₀=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease and depression.

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