Monoamine-Transporter-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Monoamine Transporter.html Monoamine HYPERLINK https:/www.MedChemE/Targets/Monoamine Transporter.html HYPERLINK https:/www.MedChemE/Targets/Monoamine Transporter.html TransporterMonoamine transporters (MATs) belong to the solute carrier 6 (SLC6) family of human

2、 transporters, which, in turn, is a subfamily ofthe broader neurotransmitter:sodium symporters (NSSs) that comprise transporters from prokaryotic to human. MATs comprisethree main members-the dopamine (DA) transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET).MATs regu

3、late neurotransmission via the reuptake of dopamine, serotonin and norepinephrine from extra-neuronal regions andthus maintain neurotransmitter homeostasis.MATs are transmembrane proteins located in plasma membranes of monoaminergic neurons. These proteins use ion (Na+, Cl)gradients as energy source

4、s to move monoamines into or out of neurons. In the membrane of intracellular synaptic vesicles is thevesicular monoamine transporters 1 and 2 (VMAT1 and VMAT2), which use a proton gradient as the energy source to sequestercytosolic monoamines into the vesicles and then release the monoamines into s

5、ynaptic cleft by exocytosis. Dysregulation of MATshas been linked to depression, anxiety disorder, attention-deficit-hyperactivity disorder, obsessive-compulsive disorder,substance-use disorders, epilepsy, Parkinsons disease and autism-spectrum disorder. Thus, MATs serve as pharmacological targetsfo

6、r several neuropsychiatric and neurodegenerative disorders.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Monoamine Transporter.html Monoamine HYPERLINK https:/www.MedChemE/Targets/Monoamine Transporter.html HYPERLINK https:/www.MedChemE/Targets/Monoamine Transporter.html Transporter HYPERLINK

7、 https:/www.MedChemE/Targets/Monoamine Transporter.html HYPERLINK https:/www.MedChemE/Targets/Monoamine Transporter.html Inhibitors HYPERLINK https:/www.MedChemE/Tetrabenazine-_addition_-.html (+)-Tetrabenazine(+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) Cat. No.: HY-B0590B HYPERLINK https:/www.

8、MedChemE/_addition_-Tetrabenazine_D6.html (+)-Tetrabenazine HYPERLINK https:/www.MedChemE/_addition_-Tetrabenazine_D6.html HYPERLINK https:/www.MedChemE/_addition_-Tetrabenazine_D6.html D6Cat. No.: HY-B0590S1(+)-Tetrabenazine (+)-TBZ; (3R,11bR)-TBZ;(3R,11bR)-Tetrabenazine) is a reversible inhibitoro

9、f vesicular monoamine transporter 2 (VMAT-2),inhibits transport by VMAT2 with 10-fold greaterpotency than transport by VMAT1.(+)-Tetrabenazine D6 is the deuterium labeled(+)-Tetrabenazine. (+)-Tetrabenazine is areversible inhibitor of vesicular monoaminetransporter 2 (VMAT-2).Purity: 99.95%Clinical

10、Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/13-hydroxyisobakuchiol.html 13-Hydroxyisobakuchiol(Delta3,2-Hydroxylbakuchiol) Cat. No.: HY-N7506 HYPERLINK https:/www.MedChemE/ffn

11、200-dihydrochloride.html FFN200 HYPERLINK https:/www.MedChemE/ffn200-dihydrochloride.html HYPERLINK https:/www.MedChemE/ffn200-dihydrochloride.html dihydrochlorideCat. No.: HY-131006Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol),an analog of Bakuchiol (HY-N0235) isolated fromPsoralea corylifolia (

12、L.), is a potent monoaminetransporter inhibitor.FFN200 dihydrochloride, a fluorescent substrate ofVMAT2, selectively trace monoamine exocytosisin both neuronal cell culture and brain tissue.The fluorescence excitation and emission maxima ofFFN200 are determined to be 352 and 451 nm,respectively.Puri

13、ty: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/hent4-in-1.html hENT4-IN-1Cat. No.: HY-110165 HYPERLINK https:/www.MedChemE/nbi-98782.html NBI-98782(+)-DTBZ; (+)-Dihydrotetrabenazine; (+)-D

14、HTBZ) Cat. No.: HY-15793hENT4-IN-1 is a potent and selective human ENT4(equilibrative nucleoside transporter 4) inhibitorwith an IC of 74.4 nM.50NBI-98782(alpha-dihydrotetrabenazine) is avesicular monoamine transporter (VMAT2) inhibtiorwith an Ki value of 0.97 nM.Purity: 98%Clinical Data: No Develop

15、ment ReportedSize: 1 mg, 5 mgPurity: 98.73%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/nisoxetine-hydrochloride.html Nisoxetine HYPERLINK https:/www.MedChemE/nisoxetine-hydrochloride.html HYPERLINK https:/www.MedChemE/nisoxetine-hydrochloride.html

16、 hydrochloride HYPERLINK https:/www.MedChemE/nisoxetine-hydrochloride.html HYPERLINK https:/www.MedChemE/pseudoisocyanine-iodide.html Pseudoisocyanine HYPERLINK https:/www.MedChemE/pseudoisocyanine-iodide.html HYPERLINK https:/www.MedChemE/pseudoisocyanine-iodide.html iodide HYPERLINK https:/www.Med

17、ChemE/pseudoisocyanine-iodide.html (1,1-Diethyl-2,2-cyanine iodide;Cat. No.: HY-B1704ADecynium 22; Diethylcyanine iodide; Eastman 7851) Cat. No.: HY-107740Nisoxetine hydrochloride is a potent and selectiveinhibitor of noradrenaline transporter (NET), witha K of 0.76 nM. Nisoxetine hydrochloride is a

18、ndantidepressant and local anesthetic, it can blockvoltage-gated sodium channels.Pseudoisocyanine (iodide) is a pan inhibitor ofmonoamine transporters and organic cationtransporters with antidepressant-like activity.Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Dat

19、a: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Radafaxine-hydrochloride.html Radafaxine HYPERLINK https:/www.MedChemE/Radafaxine-hydrochloride.html HYPERLINK https:/www.MedChemE/Radafaxine-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Radafaxine-hydrochlori

20、de.html HYPERLINK https:/www.MedChemE/Reserpine.html Reserpine(GW-353162A; BW-306U) Cat. No.: HY-17590Cat. No.: HY-N0480Radafaxine hydrochloride (GW-353162A) is a DAT(dopamine transporter) and NET(norepinephrinetransporter) transporters inhibitor, and nAChRfamily modulator.Reserpine is an inhibitor

21、of the vesicularmonoamine transporter 2 (VMAT2).Purity: 99.88%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.83%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/reserpine-hydrochloride.html Reserpin

22、e HYPERLINK https:/www.MedChemE/reserpine-hydrochloride.html HYPERLINK https:/www.MedChemE/reserpine-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/reserpine-hydrochloride.html HYPERLINK https:/www.MedChemE/reserpine-d9.html Reserpine-d9Cat. No.: HY-N0480A Cat. No.: HY-N0480SReserpin

23、e hydrochloride is an inhibitor of thevesicular monoamine transporter 2 (VMAT2).Reserpine-d9 is the deuterium labeled Reserpine.Reserpine is an inhibitor of the vesicularmonoamine transporter 2 (VMAT2).Purity: 99.90%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Developm

24、ent ReportedSize: 2.5 mg, 25 mg HYPERLINK https:/www.MedChemE/Tetrabenazine.html Tetrabenazine(Ro 1-9569) Cat. No.: HY-B0590 HYPERLINK https:/www.MedChemE/tetrabenazine-metabolite.html Tetrabenazine HYPERLINK https:/www.MedChemE/tetrabenazine-metabolite.html HYPERLINK https:/www.MedChemE/tetrabenazi

25、ne-metabolite.html Metabolite(-)-Dihydrotetrabenazine; (-)-HTBZ) Cat. No.: HY-G0025Tetrabenazine is a VMAT-inhibitor used fortreatment of hyperkinetic movement disorder.Target: Others tetrabenazine (TBZ), amonoamine-depleting and adopamine-receptor-blocking drug.Tetrabenazine Metabolite is an active

26、 metaboliteof Tetrabenazine. Tetrabenazine Metabolite is avesicular monoamine transporter 2 (VMAT2)inhibitor with a high affinity (K=13.4 nM).iPurity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https

27、:/www.MedChemE/Tetrabenazine-Racemate.html Tetrabenazine HYPERLINK https:/www.MedChemE/Tetrabenazine-Racemate.html HYPERLINK https:/www.MedChemE/Tetrabenazine-Racemate.html Racemate(Ro 1-9569 Racemate) Cat. No.: HY-B0590A HYPERLINK https:/www.MedChemE/Tetrabenazine-D6.html Tetrabenazine-d6(Ro 1-9569

28、-d6) Cat. No.: HY-B0590STetrabenazine Racemate (Ro 1-9569 Racemate) is aselective and reversible inhibitor of vesicularmonoamine transporter-2 (VMAT-2).Tetrabenazine D6 is the deuterium labeledTetrabenazine, which is a VMAT-inhibitor used fortreatment of hyperkinetic movement disorder.Purity: 98.0%C

29、linical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.30%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 g, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/nbi-98854.html Trans HYPERLINK https:/www.MedChemE/nbi-98854.html HYPERLINK https:/www.MedChem

30、E/nbi-98854.html (2,3)-Dihydrotetrabenazine HYPERLINK https:/www.MedChemE/nbi-98854.html HYPERLINK https:/www.MedChemE/Valbenazine.html Valbenazine(2R,3R,11bR)-rel-Dihydrotetrabenazine; ) Cat. No.: HY-15793A (NBI-98854) Cat. No.: HY-16771Trans (2,3)-Dihydrotetrabenazine(2R,3R,11bR)-rel-Dihydrotetrabenazine), ametabolite of Tetrabenazine, shows remarkableinhibition activity on vesicular monoaminetransporter (VMAT2).Valbenazine (NBI-98854) is a vesicular monoaminetransporter 2 (VMAT2) inhibitor with th