Dopamine Transporter Inhibitor

Medifoxamine (Standard) is the analytical standard of Medifoxamine (HY-119468). This product is intended for research and analytical applications. Medifoxamine is an orally active monoamine reuptake inhibitor and antidepressant. Medifoxamine preferentially inhibits presynaptic dopamine reuptake. Medifoxamine acts as an intraocular pressure-lowering agent to reduce intraocular pressure, and also functions as a miotic agent to decrease pupil diameter. Medifoxamine exhibits characteristic properties of antidepressant compounds, including preventing hypothermia induced by Reserpine (HY-N0480) or Apomorphine (HY-12723), potentiating the toxic effects of Yohimbine (HY-N0127) in mice, and reducing immobility behavior in mice and rats in the "behavioral despair" model. Medifoxamine has no anticholinergic activity. Medifoxamine can be used in research related to depression.

NS2359 (GSK372475) is a serotonin-norepinephrine-dopamine triple reuptake inhibitor. NS2359 is used for research on depression.

AC-4-248 is an atypical non-competitive dopamine transporter (DAT) inhibitor and reduces the potency of cocaine to inhibit DAT. AC-4-248 is a non-selective inhibitor of SLC6 transporters with IC₅₀ values for hDAT, hSERT, and hNET of 45.5 μM, 96.2 μM, and 250 μM, respectively.

AHN 1-055 (hydrochloride) (Standard) is the analytical standard of AHN 1-055 (hydrochloride) (HY-101315). This product is intended for research and analytical applications. AHN 1-055 hydrochloride is a dopamine uptake inhibitor, with an IC50 of 71 nM. AHN 1-055 hydrochloride binds with high affinity to the dopamine transporter (DAT).

O-2172, a carbacyclic analog, is a DAT inhibitor, with IC₅₀ values of 47 nM and 7000 nM for DAT and SERT, respectively.

UWA-101 hydrochloride is a selective and non-cytotoxic DAT/SERT inhibitor, with EC₅₀ values of 3.6 µM and 2.3 µM for inhibiting DAT and SERT, respectively. UWA-101 hydrochloride can alleviate the side effects of dopaminergic agents (such as L-DOPA), such as motor disorders, and lacks psychotropic activity. UWA-101 hydrochloride can be used for research on neurodegenerative diseases such as Parkinson's disease.

GBR 13098 is a dopamine transporter inhibitor with a rat IC₅₀ of 43 nM, and exhibits dopaminergic activity in vivo.GBR 13098 selectively blocks dopamine uptake, increasing synaptic dopamine availability, with weaker activity against norepinephrine uptake.GBR 13098 induces ipsilateral circling in lesioned rats and increases locomotor activity in naive mice and habituated rats, with effects attenuated by dopamine receptor antagonism.GBR 13098 reduces DOPA formation in dopamine-rich brain regions and enhances inhibitory responses of substantia nigra zona compacta dopamine neurons to dopamine.GBR 13098 serves as a tool for studying dopaminergic systems.

Tesofensine (Standard) is the analytical standard of Tesofensine. This product is intended for research and analytical applications. 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.

Piroheptine is a muscarinic acetylcholine receptor (mAChR) antagonist and dopamine reuptake inhibitor. Piroheptine blocks the high-affinity dopamine transport system, prevents MPP⁺ uptake into dopaminergic neurons, and exerts anticholinergic activity. Piroheptine completely prevents MPTP (HY-W114750)-induced loss of striatal dopamine and DOPAC, and increases striatal dopamine levels. Piroheptine can be used in studies related to Parkinson's disease.

SPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior.

RTI-371 is a highly selective atypical dopamine transporter (DAT) inhibitor that crosses the blood-brain barrier. RTI-371 exhibits potent inhibitory activity in cell lines transfected with human DAT (IC₅₀ = 8.7 nM) and shows high binding affinity for rat DAT with a K_i value of 7.81 nM. RTI-371 also acts as a positive allosteric modulator of the human cannabinoid 1 receptor (hCB1 receptor), enhancing the activity of cannabinoid receptor agonists in a concentration-dependent manner. RTI-371 can be used for the research of Parkinson's disease.

Vanoxerine (dihydrochloride) (Standard) is the analytical standard of Vanoxerine (dihydrochloride). This product is intended for research and analytical applications. Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).

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.

GBR 12935 (dihydrochloride) (Standard) is the analytical standard of GBR 12935 (dihydrochloride). This product is intended for research and analytical applications. GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride also prevents the d-Fenfluramine-induced head-twitch response in mice.

KM822 is a dopamine transporter (DAT) inhibitor with an IC₅₀ of 2.2 μM against hDAT and an IC₅₀ of 10.4 μM against C. elegans DAT-1. KM822 binds to the allosteric A2 site in the extracellular vestibule of outward-facing DAT, reduces the affinity of psychostimulants and phenethylamine psychostimulants for DAT, and inhibits dopamine transport function. KM822 attenuates the behaviors induced by psychostimulants and phenethylamine psychostimulants in planarians and C. elegans, does not induce locomotor effects on its own, and exhibits specificity for DAT. KM822 can serve as a molecular probe for investigating the allosteric regulation of DAT function. KM822 is applicable to studies related to psychostimulant use disorders.