Dopamine Transporter Inhibitor

Dopamine Transporter Inhibitors (64):

Cat. No.	Product Name	Effect	Purity

HY-B1272

Desipramine hydrochloride	Inhibitor	99.76%
Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with K_is of 4, 61 and 78,720 nM, respectively.

HY-13217

Vanoxerine dihydrochloride	Inhibitor	99.60%
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (K_i=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).

HY-B0527A

Amitriptyline hydrochloride	Inhibitor	99.94%
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-B0527

Amitriptyline	Inhibitor	99.94%
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K_i = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-B0557

Bisacodyl	Inhibitor	99.71%
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.

HY-173475

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

HY-174282

RDS-04-010	Inhibitor
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).

HY-10427A

iso-WAY-260022	Inhibitor
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.

HY-12850A

Dasotraline hydrochloride	Inhibitor	99.04%
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC₅₀ values of 4, 6, and 11 nM, respectively.

HY-16736A

Centanafadine hydrochloride	Inhibitor	99.93%
Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC₅₀s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.

HY-14472

Tesofensine	Inhibitor	99.35%
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.

HY-12242

GBR 12935 dihydrochloride	Inhibitor	99.80%
GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (K_d) 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.

HY-120170

BMS-466442	Inhibitor	98.99%
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC₅₀ of 11 nM. BMS-466442 inhibits [³H] D-serine uptake into rat brain synaptosomes, with an IC₅₀ of 400 nM. BMS-466442 can be used for schizophrenia research.

HY-101315

AHN 1-055 hydrochloride	Inhibitor	99.96%
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).

HY-13779

(E/Z)-J147	Inhibitor	99.80%
(E/Z)-J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. (E/Z)-J147 can readily pass the blood brain barrier (BBB). (E/Z)-J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC₅₀ values of 1.88 μM and 0.649 μM, respectively. (E/Z)-J147 has potential for the treatment of Alzheimer’s disease (AD).

HY-155036

Z1078601926	Inhibitor	98.94%
Z1078601926 is an allosterical inhibitor of human dopamine transporter (hDAT). Z1078601926 has synergistic effect with Nomifensine (HY-B1110).

HY-12766S

Bupropion morpholinol-d₆	Inhibitor	99.28%
Bupropion morpholinol-d6 is the deuterated form of Bupropion morpholinol. Bupropion morpholinol is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities.

HY-18610

Diclofensine hydrochloride	Inhibitor	99.79%
Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.

HY-B0527AR

Amitriptyline hydrochloride (Standard)	Inhibitor
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-18332A

Amitifadine hydrochloride	Inhibitor	99.64%
Amitifadine hydrochloride 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.

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