Monoamine Transporter Inhibitor

Indatraline (Lu 19005 free base) is a long-acting monoamine reuptake inhibitor that can be used in the research of neurological diseases.

Cendifensine is the inhibitor for monoamine reuptake that inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT).

Bevantolol (SOM3355 (free base)) 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 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 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 is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease.

(2S,3S,11bR)-Dihydrotetrabenazine ((2S,3S,11bR)-DHTBZ) is a highly selective inhibitor of vesicular monoamine transporter 2 (VMAT2) with a K_i value of 593 nM. (2S,3S,11bR)-Dihydrotetrabenazine inhibits vesicular transport of monoamine neurotransmitters like dopamine and serotonin, reducing their synaptic release. (2S,3S,11bR)-Dihydrotetrabenazine is promising for research of Huntington's chorea and other hyperkinetic disorders.

VMAT2-IN-4 (compound 11) is a vesicular monoamine transporter-2 (VMAT2) inhibitor. VMAT2-IN-4 inhibits [³H]-DTBZ binding (Ki = 560 nM). VMAT2-IN-4 inhibits [³H]-DA (Ki = 45 nM) from entering vesicles and being taken up by cells. VMAT2-IN-4 can be used in methamphetamine addiction research.

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

Pseudoisocyanine iodide (Standard) is the analytical standard of Pseudoisocyanine (iodide) (HY-107740). This product is intended for research and analytical applications. 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.

FFN511 (Standard) is the analytical standard of FFN511 (HY-103465). This product is intended for research and analytical applications. 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.

Tetrabenazine (Standard) is the analytical standard of Tetrabenazine (HY-B0590). This product is intended for research and analytical applications. 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.

Bevantolol-d₇ hydrochloride (SOM3355-d₇) is the d₇-labeled Bevantolol hydrochloride (HY-121186). 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.

WY-46824 is a selective norepinephrine transporter (NET) inhibitor. WY-46824 does not alter the total expression level or cell surface expression level of hNET. WY-46824 can be used in related research on attention deficit hyperactivity disorder (ADHD).

GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder.

Nisoxetine (Standard) is the analytical standard of Nisoxetine. This product is intended for research and analytical applications. Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

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

Bevantolol hydrochloride (Standard) (SOM3355 (Standard)) is the analytical standard of Bevantolol hydrochloride (HY-121186). This product is intended for research and analytical applications. 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.

Valbenazine (Standard) is the analytical standard of Valbenazine. This product is intended for research and analytical applications. Valbenazine (NBI-98854) is a vesicular monoamine transporter 2 (VMAT2) inhibitor with the Ki of 110-190 nM.

EXP631 is a centrally acting non-opioid analgesic that targets serotonin and norepinephrine transporters. EXP631 exhibits activity against acute pain induced by chemical stimuli, stress, and electrical stimulation. EXP631 blocks the reuptake of serotonin and norepinephrine. EXP631 can be used in research related to moderate to moderately severe acute and chronic pain.

Esreboxetine succinate (PNU-165442G; (S,S)-Reboxetine succinate) 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 succinate increases urethral closure pressure and urethral resistance in rats. Esreboxetine succinate is applicable to research related to inflammatory pain and stress urinary incontinence.

13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) that can be isolated from Psoralea corylifolia (L.), is a potent selective 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 increases the activity of intact mice and improves the decreased activity of reserpinized mice in vivo. 13-Hydroxyisobakuchiol can be used for the research of disorders such as Parkinson's disease and depression.

TAS-303 is an orally effective selective norepinephrine transporter (NET) inhibitor. TAS-303 inhibits human NET ligand binding with a K_i of 50.9 nM, and suppresses NET-mediated norepinephrine uptake with an IC₅₀ of 38.9 nM. TAS-303 enhances norepinephrine-induced contraction in isolated rat urethral tissues, elevates plasma norepinephrine levels in rats, and increases urethral baseline pressure and leak point pressure. TAS-303 is applicable for research related to stress urinary incontinence, norepinephrine reuptake, and lower urinary tract function.