Monoamine Transporter Inhibitor

Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

Netarsudil (AR-13324) is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil reduces intraocular pressure by inhibiting ROCK, causing relaxation of trabecular meshwork cells and dilation of episcleral veins, thereby increasing the ease of aqueous humor outflow, while inhibiting NET to reduce aqueous humor production. Netarsudil is mainly used in the study of ocular hypertension and primary open-angle glaucoma.

Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.

Pseudoisocyanine iodide (1,1'-Diethyl-2,2'-cyanine iodide) is an inhibitor of organic cation transporters (OCT1, OCT2, OCT3) and plasma membrane monoamine transporter (PMAT). Pseudoisocyanine iodide has antidepressant activity.

Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

DLX48 is a LeuBAT (Δ13 mutant) transporter inhibitor that binds to the transporter’s active site. DLX48 can crosses the blood-brain barrier, and has a lower risk of cytochrome P450-related drug-drug interactions. DLX48 can be used for the research of major depressive disorder.

Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a K_d of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

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

Tetrabenazine (Ro 1-9569) Racemate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine Racemate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine Racemate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine Racemate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.

Tetrabenazine-d₆ (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.

Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a K_d of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

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.

NBI-98782 is a high affinity and selectivity vesicular monoamine transporter 2 (VMAT2) inhibitor with a K_i of 3 nM. NBI-98782 has antipsychotic activity.

Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.

Reserpine (Standard) is the analytical standard of Reserpine. This product is intended for research and analytical applications. Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

Reserpine-d₉ is the deuterium labeled Reserpine. Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

(+)-Tetrabenazine ((+)-TBZ) is the enantiomer of Tetrabenazine (HY-B0590) and is also a Vesicular Monoamine Transporter 2 (VMAT2) inhibitor with a rat K_i of 4.61 nM. (+)-Tetrabenazine inhibits monoamine uptake into granular vesicles of presynaptic neurons. (+)-Tetrabenazine is 3 times more active than (-)-Tetrabenazine. (+)-Tetrabenazine can be used for the research of Huntington's disease and hyperkinetic movement disorders (including chorea).

Liafensine (BMS-820836) is an orally active, blood-brain barrier-permeable monoamine reuptake inhibitor, with an IC₅₀ of 5.67 nM against DAT, 1.08 nM against SERT, and 7.99 nM against NET. Liafensine binds to DAT to block dopamine reuptake. Liafensine binds to SERT to block serotonin reuptake. Liafensine binds to NET to block norepinephrine reuptake. Liafensine can be used in studies related to depression.

GZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an K_i of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction.

(R,S,S)-Dihydrotetrabenazine (R,S,S-DHTBZ) is a kind of discrete isomeric secondary alcohol metabolites of Tetrabenazine (TBZ, HY-B0590), is a poor VMAT2 inhibitor (K_i = 690 nM).