Dopamine Transporter Inhibitor

JJC8-091 is a potent dopamine transporter (DAT) inhibitor with K_i values of 230, 97800 nM for DAT, SERT, respectively. JJC8-091 has the potential for the research of psychostimulant use disorders (PSUD).

DAM-001 (Z236004662) is a potent, non-competitive allosteric inhibitor for human dopamine transporter (hDAT) with an IC₅₀ of 24.70 μM and 1.026 μM in the absence and presence of orthosteric inhibitor Nomifensine (HY-B1110).

Hordenine-d₆ hydrochloride (Ordenina-d₆ hydrochloride; Peyocactine-d₆ hydrochloride) is the deuterated-labeled Hordenine hydrochloride (HY-N0113B). Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride inhibits melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

(R)-Phenylpiracetam (MRZ 9547) is a dopamine transporter (DAT) inhibitor (K_i: 14.8 μM; IC₅₀: 65.5 μM). (R)-Phenylpiracetam can be used for the research of the neurological or neuropsychiatric disorders.

CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC₅₀s of 311 and 14.1 nM, respectively.

JJC8-089 is a dopamine transporter (DAT) inhibitor that may improve motivational dysfunction and increase effortful behavior in goal-directed activities. JJC8-089 significantly reversed the low-effort effects induced by the VMAT-2 inhibitor Tetrabenazine (HY-B0590) in rats and increased the choice of high-effort fixed-ratio 5-bar presses versus food intake. .

Tesofensine-¹³C,d₃ (NS-2330-¹³C,d₃) is the deuterium and ¹³C-labeled Tesofensine (HY-14472). Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC₅₀=6.5 nM), norepinephrine (NE;IC₅₀=1.7 nM), and serotonin (5-HT;IC₅₀=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.

CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease.

Hordenine (Standard) (Ordenina (Standard); Peyocactine (Standard)) is the analytical standard of Hordenine (HY-N0113). This product is intended for research and analytical applications. Hordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

RDS-04-010 is an atypical dopamine transporter (DAT) inhibitor. RDS-04-010 has the effect of inhibiting cocaine intake and seeking behavior. RDS-04-010 exerts its modulatory effect mainly by binding to the inward conformation of DAT, thereby reducing the reinforcing effect of cocaine. RDS-04-010 can be used in the study of cocaine use disorder (CUD).

SKF-83566 hydrochloride is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a K_i value of approximately 0.4-0.56 nM. SKF-83566 hydrochloride modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 hydrochloride acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 hydrochloride competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 hydrochloride is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect").

RDS03-94 is a dopamine transporter (DAT) inhibitor. RDS03-94 reduces hERG/DAT ratio.

JJC8-088, a Modafinil-derived ligand, is a dopamine transporter (DAT) inhibitor with a K_i of 2.53 nM. JJC8-088 dioxalate can be to study psychostimulant use disorders.

Hordenine hydrochloride (Standard) (Ordenina hydrochloride (Standard); Peyocactine hydrochloride (Standard)) is the analytical standard of Hordenine hydrochloride (HY-N0113B). This product is intended for research and analytical applications. Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride inhibits melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder.

iso-WAY-260022 (Compound 13R) is an orally active, brain-penetrant and selective norepinephrine transporter (hNET) inhibitor with an IC₅₀ value of 140 nM. iso-WAY-260022 also shows inhibitory effects on human serotonin (hSERT) and dopamine transporters (hDAT). iso-WAY-260022 inhibits norepinephrine reuptake and increases hypothalamic norepinephrine levels to regulate thermoregulatory center function. iso-WAY-260022 is promising for research of vasomotor symptoms, such as menopausal hot flushes, night sweats.

GBR-12879 methanesulfonate acts as a dopamine reuptake inhibitor.

Tesofensine-d₅ (NS-2330-d₅) is the deuterium labeled Tesofensine (HY-14472). Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC₅₀=6.5 nM), norepinephrine (NE;IC₅₀=1.7 nM), and serotonin (5-HT;IC₅₀=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.

DOV-216,303 is an antidepressant compound. DOV-216,303 inhibits the reuptake of norepinephrine (NE), serotonin (5‐HT), and dopamine (DA), with IC₅₀ values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. DOV-216,303 increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats.

Hordenine sulfate (Ordenina sulfate; Peyocactine sulfate) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine sulfate inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine sulfate promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine sulfate inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine sulfate activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine sulfate activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine sulfate inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine sulfate limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine sulfate can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.