Monoamine Transporter Inhibitor

(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).

Dihydrotetrabenazine (DHTBZ) is the active metabolite of Tetrabenazine (HY-B0590). Dihydrotetrabenazine is the inhibitor for human vesicular monoamine transporter 2 (VMAT2), that reduces monoamine content in presynaptic neurons, and can be used in movement disorder research.

F3288-0031 is a brain-penetrant norepinephrine transporter (NET) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of NET, stabilizing the inward-open state and has a preferential NET/SERT inhibition with pIC₅₀ = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions.

(-)-Tetrabenazine ((-)-TBZ; compound 13) is an enantiomer of Tetrabenazine (HY-B0590). (+)-Tetrabenazine proves 3-fold more active than (-)-Tetrabenazine in inhibiting vesicular monoamine transporter 2 (VMAT2).

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

Radafaxine ((S,S)-Hydroxybupropion) is an antidepressant. Radafaxine blocks dopamine transporters (DAT). Radafaxine is an active metabolite of Bupropion.

Lafadofensine D-(-)-Mandelic acid is the monoamines reuptake inhibitor. Lafadofensine D-(-)-Mandelic acid has sufficient effects after short-term administration.

Cavα2δ1&NET-IN-2 (Compound 45CS) 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-2 inhibits Ca_vα2δ-1 with a K_i of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a K_i of 59 nM and IC₅₀ of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain.

Talopram hydrochloride is a selective inhibitor for norepinephrine transporter (NET), that inhibits 63% human NET at 100 nM.

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.

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

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.

VMAT2-IN-3 (compound 10) is a potent vesicular monoamine transporter-2 (VMAT2) inhibitor with a K_i of 0.71 nM. VMAT2-IN-3 has the potential for neurological or psychiatric disease research.

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

JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.

Lortalamine (LM 1404) is a selective norepinephrine transporter inhibitor with an IC₅₀ of <1 nM. Lortalamine is a non-tricyclic antidepressant. Lortalamine antagonises Reserpine (HY-N0480)-induced ptosis and hypothermia. Lortalamine inhibits norepinephrine uptake.

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

XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research.

Tetrabenazine-d₇ (TBZ-d₇-d₇) is deuterium labeled 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.