Dopamine Transporter Inhibitor

3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) is a potent dopamine uptake inhibitor. 3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) acts as a potent long-acting antihistaminic agent.

RTI 336 is a phenyltropane analog, as well as a potent and selective dopamine transporter (DAT) inhibitor. RTI 336 inhibits addictive agent induced locomotor activity and self-administration in Lewis rats. RTI 336 exhibits inhibitory effects depending on inherent NAc DAT levels.

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.

DOV-102,677 is an orally sctive triple monoamine neurotransmitter reuptake inhibitor that simultaneously inhibits the dopamine (DAT) (IC₅₀ = 129 nM; K_i = 222 nM), norepinephrine (NET) (IC₅₀ = 103 nM; K_i = 1030 nM), and serotonin (SERT) (IC₅₀ = 133 nM; K_i = 740 nM) transporters. DOV-102,677 demonstrated significant antidepressant-like activity and sensory-motor gating regulatory effects in mouse experiments. DOV-102,677 can be used for research on depression.

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

Bicifadine is an orally active serotonin/norepinephrine/dopamine triple reuptake inhibitor. Bicifadine is an effective antinociceptive in several models of acute, persistent, and chronic pain.

MRS7292 is a non-competitive inhibitor of human dopamine transporter (hDAT). MRS7292 inhibits dopamine transport.

JJC12-009 is a dopamine transporter (DAT) inhibitor, with a K_i of 5.45 nM.

Levophacetoperane (Phacetoperane free base) competitively inhibits the uptake of norepinephrin and dopamine.

SKF-83566 (Standard) is the analytical standard of SKF-83566 (HY-103430A). This product is intended for research and analytical applications. SKF-83566 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 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 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").

6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT₂ family receptors. For NET, 6-APDB has an IC₅₀ of 0.56 μM and a K_i of 18 μM; for SERT, it has an IC₅₀ of 2.3 μM and a K_i of 23 μM; for DAT, it has an IC₅₀ of 33 μM and a K_i of >30 μM, and affinity for rat and mouse TAAR1, with K_i values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse.

Levophacetoperane (hydrochloride) (Standard) is the analytical standard of Levophacetoperane (hydrochloride) (HY-101631). This product is intended for research and analytical applications. Levophacetoperane inhibits in vitro in a competitive manner, norepinephrin uptake and dopamine uptake.

Diclofensine (Ro 8-4650) hydrochloride (Standard) is the analytical standard of Diclofensine hydrochloride. This product is intended for research and analytical applications. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC₅₀ values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.

Amitifadine (DOV-21947; EB-1010) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC₅₀s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.

DAT-IN-2 is an atypical dopamine transporter (DAT) inhibitor with blood-brain barrier permeability. DAT-IN-2 binds to human DAT with a K_i of 63.0 nM and stabilizes the transporter in an inward-facing conformation. DAT-IN-2 produces only weak locomotor stimulant effects and does not induce conditioned place preference in mice, indicating no rewarding effects. DAT-IN-2 can be used in research related to psychostimulant use disorder.

Fourphit is a dopamine transporter (DAT) inhibitor and phencyclidine (PCP) receptor binding agent. Fourphit irreversibly acylates the DAT [³H]methylphenidate binding site, reversibly binds to the PCP receptor, and sensitizes neuronal L-type DHP calcium channels. Fourphit attenuates K⁺-stimulated ⁴⁵Ca²⁺ uptake at high concentrations, and after its pretreatment, Nifedipine (HY-B0284) effectively inhibits this uptake without affecting resting calcium uptake. Fourphit reduces cocaine-induced hyperactivity, decreases cocaine-induced rearing frequency, enhances cocaine-induced thigmotaxis, elicits an acute increase in locomotor activity, and suppresses dark-cycle activity. Fourphit is used in research related to cocaine abuse and addiction.

Bisacodyl (Standard) is the analytical standard of Bisacodyl. This product is intended for research and analytical applications. Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.

DAT-IN-1 (Coumpound 12b) is an atypical DAT inhibitor with a K_i of 8.37 nM. DAT-IN-1 can be used in the study of psychostimulant use disorder (PSUD).

GBR 12935 fumarate is a potent, and selective dopamine reuptake inhibitor, with the binding constant (K_d) of 1.08 nM in COS-7 cells. GBR 12935 fumarate stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 fumarate also prevents the d-Fenfluramine-induced head-twitch response in mice.

CTDP-32476 is a dopamine transporter (DAT) inhibitor with antidepressant activity, exhibiting a K_i value of 12 nM for human DAT and moderate affinity for the norepinephrine transporter (NET). CTDP-32476 blocks DAT to increase extracellular dopamine levels, and induces locomotor stimulation and brain-stimulation reward effects in rats. CTDP-32476 is used in research related to drug addiction.