dopamine uptake

Fezolamine is a novel orally available non-tricyclic compound with antidepressant activity. It is three to two times more selective in blocking synaptosomal uptake of [3H]norepinephrine than uptake of [4H]3-hydroxytryptamine or [3H]dopamine in vitro. It blocked the inhibitory effects of rifampicin and tetraphenyl in classical behavioral tests using monoamine-depleted animals.

Roxindole (EMD 49980) is a selective dopamine autoreceptor and 5-HT1A dual agonist and inhibitor of 5-hydroxytryptamine (5-HT) uptake with antipsychotic and antidepressant activity.Roxindole can be used to study Parkinson's and neurodivergence.

Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a potent inhibitor of dopamine uptake (IC50: 1-51 nM).

Oxolinic acid (Nidantin) is a synthetic antimicrobial related to NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Benztropine mesylate (Benztropine methanesulfonate) is a centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.

AHN 1-055 hydrochloride (3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride) is an inhibitor of dopamine transporter (DAT) and dopamine uptake(IC50 = 71 nM).

Amoxapine (CL-67772) exerts its antidepressant effect by inhibiting the re-uptake of norepinephrine and, to a lesser degree, of serotonin, at adrenergic nerve endings and blocks the response of dopamine receptors to dopamine. Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class. This drug is used to treat symptoms of depression and may cause tardive dyskinesia. Amoxapine also binds to alpha-adrenergic, histaminergic, and cholinergic receptors which accounts for many of the side effects seen with this agent.

3-CPMT (FC-1) is a dopamine uptake inhibitor and a potent long-acting antihistaminic agent.

Rimcazole dihydrochloride is the hydrochloride salt of Rimcazole, a σ receptor antagonist. Rimcazole dihydrochloride also binds to dopamine transporter proteins and inhibits dopamine uptake.

GBR 12783 dihydrochloride (GBR12783 2HCl) is a specific, potent and selective dopamine uptake inhibitor. GBR 12783 dihydrochloride inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively.GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID:11454468 |Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID:12963052

GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats. GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively.

GBR-13098 dimethanesulfonate is an inhibitor of dopamine uptake.

GBR-13119 is a dopamine uptake inhibitor.

JHW 007 hydrochloride is a Dopamine uptake inhibitor.

Amfonelic Acid is a dopamine uptake blocker.

JNJ-7925476 HCl is a triple monoamine uptake inhibitor. JNJ-7925476 Salt blocks the dopamine transporter (DAT), norepinephrine transporter (NET) and serotonin transporter (SERT) in the central nervous system. The ED(50) values for JNJ-7925476 occupancy of

Mazaticol is an anticholinergic agent, which blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol potently inhibits 3H-QNB and 3H-PZ binding. Mazaticol can bind to the M2 receptors with high affinity. Mazaticol shows inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol has research in parkinsonian syndrome.

(S)-CE-123 is an innovative and highly selective atypical dopamine transporter (DAT) inhibitor, exhibiting an EC 50 of 2.76 μM in uptake inhibition assays performed in HEK293 cells with stable expression of human DAT isoforms. As a Modafinil analogue, (S)-CE-123 can cross the blood–brain barrier and enhances cognitive and motivational functions in experimental animals [1] [2].

Benzatropine is a centrally active muscarinic antagonist. It also inhibits the uptake of dopamine. It has been used in the symptomatic treatment of Parkinson's Disease.

Rimcazole is a sigma receptor antagonist. It also binds to the dopamine transporter and inhibiting dopamine uptake.

MCN-5908 is a dopamine uptake inhibitor.

Piroheptine HCl is an agent of anticholinergic that acts by inhibiting dopamine uptake and completely preventing loss of striatal dopamine in MPTP-treated mice.

SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM

GBR 13069 dihydrochloride is a dopamine uptake inhibitor.

DPT (hydrochloride), a psychedelic tryptamine class compound, acts by inhibiting dopamine, serotonin, and norepinephrine re-uptake (IC50s = 23, 2.9, and 9.1 μM, respectively). It is designated for research and forensic applications.

PD 89211 is a selective dopamine D4 receptor antagonist with high selectivity for the DA D4.2 receptor (> 800-fold) as compared to other hDA receptor subtypes, rat brain serotonin, and adrenergic receptors. In vitro, PD 89211 reverses quinpirole-induced [

Nomifensine maleate (Nomifensine (maleate)) is a selective inhibitor of dopamine uptake. Nomifensine maleate is used in adult attention deficit disorder.

FFN-102 (trifluoroacetate salt) is a synthetic biogenic neurotransmitter analog with pH-dependent fluorescence and electroactivity.