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).

Bevantolol hydrochloride (SOM3355) is a selective β1-adrenergic receptor antagonist, with an IC₅₀ of 35 nM for β₁-adrenergic receptor and an IC₅₀ of 60 nM for VMAT2. Bevantolol hydrochloride blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol hydrochloride reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol hydrochloride is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease.

Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine transporter (NET) inhibitor, with a pIC₅₀ of 9.6 and a pK_i of 9.2 in rats, and it can cross the blood-brain barrier. Esreboxetine increases urethral closure pressure and urethral resistance in rats. Esreboxetine is applicable to research related to inflammatory pain and stress urinary incontinence.

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.