Dopamine-Receptor-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html Dopamine HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html ReceptorDopamine Receptors are a class of G protein-coupled receptors that are prominent in the vertebrate

2、central nervous system (CNS).The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors. Dopamine receptors are implicated inmany neurological processes, including motivation, pleasure, cognition, memory, learning, and fine motor control, as well asmodulation of neuroendoc

3、rine signaling. Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated inseveral neuropsychiatric disorders. Thus, dopamine receptors are common neurologic drug targets; antipsychotics are oftendopamine receptor antagonists while psychostimulants are typically indirect ag

4、onists of dopamine receptors. There are at least fivesubtypes of dopamine receptors, D1, D2, D3, D4, and D5. The D1 and D5 receptors are members of the D1-like family of dopaminereceptors, whereas the D2, D3 and D4receptors are members of the D2-like family.www.MedChemE 1 HYPERLINK https:/www.MedChe

5、mE/Targets/Dopamine Receptor.html Dopamine HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html Inhi

6、bitors, HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html Antagonists, HYPERLINK https:/www.MedC

7、hemE/Targets/Dopamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html Activators, HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html Modulators HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.ht

8、ml HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Dopamine Receptor.html Chemicals HYPERLINK https:/www.MedChemE/_addition_-Dihydrexidine_hydrochloride.html (+)-Dihydrexidine HYPERLINK

9、https:/www.MedChemE/_addition_-Dihydrexidine_hydrochloride.html HYPERLINK https:/www.MedChemE/_addition_-Dihydrexidine_hydrochloride.html hydrochloride(+)-DAR-0100 hydrochloride) Cat. No.: HY-101299 HYPERLINK https:/www.MedChemE/_addition_-PD_128907_hydrochloride.html (+)-PD HYPERLINK https:/www.Med

10、ChemE/_addition_-PD_128907_hydrochloride.html HYPERLINK https:/www.MedChemE/_addition_-PD_128907_hydrochloride.html 128907 HYPERLINK https:/www.MedChemE/_addition_-PD_128907_hydrochloride.html HYPERLINK https:/www.MedChemE/_addition_-PD_128907_hydrochloride.html hydrochlorideCat. No.: HY-110000(+)-D

11、ihydrexidine hydrochloride (+)-DAR-0100hydrochloride) is a dopamine D1 receptoragonist with an EC of 72 21 nM.50(+)-PD 128907 hydrochloride is a selectivedopamine D2/D3 receptor agonist, with Kis of1.7, 0.84 nM for human and rat D receptors, 179,3770 n M for human and rat D receptors,3respectively.P

12、urity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/1s-5r-gsk598809.html (-)-GSK598809(1S,5R-GSK598809) Cat. No.: HY-19654B HYPERLINK https:/www.MedChemE/_-_-Isoc

13、orypalmine.html (-)-Isocorypalmine(Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) Cat. No.: HY-N0927(-)-GSK598809 is an isomer of GSK598809. GSK598809is a potent and selective dopamine D3 Receptor(DRD3) antagonist.(-)-Isocorypalmine (Tetrahydrocolumbamine),isolated from the crude base fraction of

14、 Corydalischaerophylla, is a dopamine receptor ligand.Recombinant CYP719A21 displays strict substratespecificity and high affinity (K =4.63 0.71mM) for (-)-Isocorypalmine.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.64%Clinical Data: No Development ReportedSize: 1 mg,

15、5 mg HYPERLINK https:/www.MedChemE/r-preclamol.html (R)-Preclamol(+)-3-PPP) Cat. No.: HY-145454 HYPERLINK https:/www.MedChemE/rac-methotrimeprazine-d3-hydrochloride.html (Rac)-Levomepromazine-d3 HYPERLINK https:/www.MedChemE/rac-methotrimeprazine-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/r

16、ac-methotrimeprazine-d3-hydrochloride.html hydrochloride(Rac)-Methotrimeprazine-d3 hydrochloride) Cat. No.: HY-19489S1(R)-Preclamol is a dopamine (DA) agonist withautoreceptor as well as postsynaptic receptorstimulatory properties. (R)-Preclamol inhibits thelocomotor activity of mice and rats in low

17、 doses.(Rac)-Levomepromazine-d3(Rac)-Methotrimeprazine-d3) hydrochloride is alabelled racemic Methotrimeprazine, which is aphenothiazine which has antagonist actions atmultiple neurotransmitter receptor sites,including dopaminergic, cholinergic, serotoninPurity: 99.88%Clinical Data: No Development R

18、eportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/rac-pf-06256142.html (Rac)-PF-06256142 HYPERLINK https:/www.MedChemE/rac-pf-06256142.html HYPERLINK https:/www.MedChemE/rac-Rotigotine-Hydrochloride.html (Rac)-Rotigotine HYPERLIN

19、K https:/www.MedChemE/rac-Rotigotine-Hydrochloride.html HYPERLINK https:/www.MedChemE/rac-Rotigotine-Hydrochloride.html hydrochlorideCat. No.: HY-119943A Cat. No.: HY-15394(Rac)-PF-06256142 is the less effective enantiomerof PF-06256142 (HY-119943). (Rac)-PF-06256142 isan agonist of D1 receptor, wit

20、h an EC of 10750nM. (Rac)-PF-06256142 can be used for the researchof schizophrenia and Parkinsons disease.(Rac)-Rotigotine hydrochloride is a racemate ofRotigotine.Purity: 99.31%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.66%Clinical Data: No D

21、evelopment ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/rac-rotigotine-d7-hydrochloride.html (Rac)-Rotigotine-d7 HYPERLINK https:/www.MedChemE/rac-rotigotine-d7-hydrochloride.html HYPERLINK https:/www.MedChemE/rac-rotigotine-d7-hydrochloride.html hydrochloride HYPERLI

22、NK https:/www.MedChemE/rac-rotigotine-d7-hydrochloride.html HYPERLINK https:/www.MedChemE/rac-tavapadon.html (Rac)-TavapadonCat. No.: HY-15394S(Rac)-PF-06649751; (Rac)-CVL-751) Cat. No.: HY-119486A(Rac)-Rotigotine-d7 (hydrochloride) is deuteriumlabeled (Rac)-Rotigotine (hydrochloride).(Rac)-Rotigoti

23、ne hydrochloride is a racemate ofRotigotine.(Rac)-Tavapadon (Rac)-PF-06649751) is a potentand selective noncatechol dopamine D1 receptoragonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.63%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 1

24、00 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/s-amisulpride.html (S)-Amisulpride(Esamisulpride; SEP-4199) Cat. No.: HY-126068 HYPERLINK https:/www.MedChemE/z-chlorprothixene-d6-hydrochloride.html (Z)-Chlorprothixene-d6 HYPERLINK https:/www.MedChemE/z-c

25、hlorprothixene-d6-hydrochloride.html HYPERLINK https:/www.MedChemE/z-chlorprothixene-d6-hydrochloride.html hydrochlorideCat. No.: HY-B0274S(S)-Amisulpride (Esamisulpride) is a potentdopamine D /D receptor antagonist.2 3(S)-Amisulpride is an antagonist at the 5-HT7receptor with a K of 900 nM. (S)-Ami

26、sulpride hasIantipsychotic and antidepressant effects.(Z)-Chlorprothixene-d6 hydrochloride is thedeuterium labeled Chlorprothixene. Chlorprothixeneis a dopamine and histamine receptorsantagonist with Ks of 18 nM, 2.96 nM, 4.56 nM, 9inM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1receptors, respectivel

27、y. Antipsychotic activity.Purity: 99.75%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/_plusmn_-Methotrimeprazine-D6.html ()-Levomepromazine-d6()-Methotrimeprazine-d6; dl-Met

28、hotrimeprazine-d6) Cat. No.: HY-19489S HYPERLINK https:/www.MedChemE/2-o-methylisoliquiritigenin.html 2-O-MethylisoliquiritigeninCat. No.: HY-N1745()-Levomepromazine D6 ()-Methotrimeprazine D6)is the deuterium labeled Methotrimeprazine, whichis a D3 dopamine and Histamine H1 receptorantagonist.2-O-M

29、ethylisoliquiritigenin, isolated from theArachis species, up-regulates 5-HT, NE, DA andGABA pathways, but does not put a verysignificant effect on ne NE pathway.Purity: 98.0%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK ht

30、tps:/www.MedChemE/3-o-methyldopa.html 3-O-Methyldopa(3-Methoxy-L-tyrosine; 3-O-Methyl-L-DOPA) Cat. No.: HY-113468A HYPERLINK https:/www.MedChemE/3-o-methyldopa-d3.html 3-O-Methyldopa-d3(3-Methoxy-L-tyrosine-d3; 3-O-Methyl-L-DOPA-d3) Cat. No.: HY-113468AS3-O-Methyldopa (3-Methoxy-L-tyrosine) is ameta

31、bolite of L-DOPA which is formed bycatechol-O-methyltransferase (COMT).3-O-Methyldopa competitively inhibits thepharmacodynamics of l-DOPA and dopamine.3-O-Methyldopa D3 (3-Methoxy-L-tyrosine D3) isdeuterium labeled 3-O-Methyldopa. 3-O-Methyldopais a metabolite of L-DOPA which is formed bycatechol-O

32、-methyltransferase (COMT).3-O-Methyldopa competitively inhibits thepharmacodynamics of l-DOPA and dopamine.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mgPurity: 99.34%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/3-o-methyldopa-

33、d3-hydrate.html 3-O-Methyldopa-d3 HYPERLINK https:/www.MedChemE/3-o-methyldopa-d3-hydrate.html HYPERLINK https:/www.MedChemE/3-o-methyldopa-d3-hydrate.html hydrate HYPERLINK https:/www.MedChemE/3-o-methyldopa-d3-hydrate.html (3-Methoxy-L-tyrosine-d3 hydrate; HYPERLINK https:/www.MedChemE/1H-Isoindol

34、e-1,3_2H_-dione,_2-2-4-_6-fluoro-1,2-benzisoxazol-3-yl_-1-piperidinylethyl-.html 5-HT6/7 HYPERLINK https:/www.MedChemE/1H-Isoindole-1,3_2H_-dione,_2-2-4-_6-fluoro-1,2-benzisoxazol-3-yl_-1-piperidinylethyl-.html HYPERLINK https:/www.MedChemE/1H-Isoindole-1,3_2H_-dione,_2-2-4-_6-fluoro-1,2-benzisoxazo

35、l-3-yl_-1-piperidinylethyl-.html antagonist HYPERLINK https:/www.MedChemE/1H-Isoindole-1,3_2H_-dione,_2-2-4-_6-fluoro-1,2-benzisoxazol-3-yl_-1-piperidinylethyl-.html HYPERLINK https:/www.MedChemE/1H-Isoindole-1,3_2H_-dione,_2-2-4-_6-fluoro-1,2-benzisoxazol-3-yl_-1-piperidinylethyl-.html 13-O-Methyl-

36、L-DOPA-d3 hydrate) Cat. No.: HY-113468AS1Cat. No.: HY-1016223-O-Methyldopa D3 (3-Methoxy-L-tyrosine D3)hydrate is the deuterium labeled 3-O-Methyldopa.3-O-Methyldopa (3-Methoxy-L-tyrosine) is ametabolite of L-DOPA which is formed bycatechol-O-methyltransferase (COMT).5-HT6/7 antagonist 1 is a multif

37、unctional ligandthat antagonizes 5-HT6/7/2A and D2 receptors,without interacting with M1 receptors and hERGchannels.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/A-381393.html A-381393

38、HYPERLINK https:/www.MedChemE/A-381393.html HYPERLINK https:/www.MedChemE/A37203.html A-437203Cat. No.: HY-116941(Lu201640; A37203) Cat. No.: HY-U00185A-381393 is a potent, selective, brain penetratedopamine D receptor antagonist, with s of4 Ki1.5, 1.9 and 1.6 nM for human dopamine D ,4.4D , and D r

39、eceptor, respectively,4.2 4.72700-fold selectivity over D , D , D and1 2 3D dopamine receptors.5Purity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgA-437203 is a selective D receptor antagonist3with K of 71, 1.6, and 6220 nM for D , D , andi 2 3D re

40、ceptors, respectively.4Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/a-77636-hydrochloride.html A-77636 HYPERLINK https:/www.MedChemE/a-77636-hydrochloride.html HYPERLINK https:/www.MedChemE/a-77636-hydrochloride.html hydrochloride HYPE

41、RLINK https:/www.MedChemE/a-77636-hydrochloride.html HYPERLINK https:/www.MedChemE/a68930.html A68930Cat. No.: HY-103416 Cat. No.: HY-120687A-77636 hydrochloride is a potent, orally active,selective and long acting dopamine D1 receptoragonist (pKi=7.40; Ki=39.8 nM) withantiparkinsonian activity. A-7

42、7636 hydrochlorideis functionally inactive at dopamine D2 receptor.A68930, as a dopamine D1 receptor agonist, canbe used for the research of bronchiectasis.Purity: 98.00%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:

43、/www.MedChemE/a68930-hydrochloride.html A68930 HYPERLINK https:/www.MedChemE/a68930-hydrochloride.html HYPERLINK https:/www.MedChemE/a68930-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/a68930-hydrochloride.html HYPERLINK https:/www.MedChemE/Abaperidone.html AbaperidoneCat. No.: HY-

44、103431 Cat. No.: HY-101619A68930 hydrochloride, as a dopamine D1receptor agonist, can be used for the research ofbronchiectasis.Abaperidone is a potent antagonist of5-HT receptor2A and dopamine D2 receptorwith IC s of 6.2 and 17 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgP

45、urity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ABT-670.html ABT-670 HYPERLINK https:/www.MedChemE/ABT-670.html HYPERLINK https:/www.MedChemE/abt-724.html ABT-724Cat. No.: HY-19483 Cat. No.: HY-14330ABT-670 is a selective, oral bioavailable agonistof do

46、pamine D4 receptor, with EC50 of 89nM, 160 nM, and 93 nM for humanD , ferretD ,4 4and ratD , respectively.4Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgABT-724 is a potent and highly selectivedopamine D receptor4 agonist with an EC50of 12.4 nM for human dopamine D receptor.4ABT-7

47、24 is a potent partial agonist at the ratD4 (EC50 of 14.3 nM) and the ferret D4receptor (EC of 23.2 nM).50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/abt-724-trihydrochloride.html ABT-724 HYPERLINK https:/www.MedChemE/abt-724-trihydrochloride.html

48、HYPERLINK https:/www.MedChemE/abt-724-trihydrochloride.html trihydrochloride HYPERLINK https:/www.MedChemE/abt-724-trihydrochloride.html HYPERLINK https:/www.MedChemE/Adoprazine.html AdoprazineCat. No.: HY-103409(SLV313) Cat. No.: HY-14782ABT-724 trihydrochloride is a potent and highlyselective dopa

49、mine D receptor agonist with4an EC50 of 12.4 nM for human dopamine D4receptor.Adoprazine (SLV313) is a full 5-HT receptor1Aagonist with a pEC of 9 at cloned h5-HT50 1Areceptors. Adoprazine (SLV313) is a full D and2D3 receptor pA2santagonist with of 9.3 and8.9 at hD and hD receptors, respectively.2 3

50、Purity: 99.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.10%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Alizapride_hydrochloride.html Alizapride HYPERLINK https:/www.MedChemE/Alizapride_hydrochlorid

51、e.html HYPERLINK https:/www.MedChemE/Alizapride_hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Alizapride_hydrochloride.html HYPERLINK https:/www.MedChemE/alizapride-13c-d3-hydrochloride.html Alizapride-13C,d3 HYPERLINK https:/www.MedChemE/alizapride-13c-d3-hydrochloride.html HYPERLI

52、NK https:/www.MedChemE/alizapride-13c-d3-hydrochloride.html hydrochlorideCat. No.: HY-A0125A Cat. No.: HY-A0125ASAlizapride hydrochloride is a dopaminereceptor antagonist with prokinetic andantiemetic effects which can also be used in thetreatment of nausea and vomiting, includingpostoperative nause

53、a and vomiting.Alizapride-13C,d3 (hydrochloride) is deuteriumlabeled Alizapride (hydrochloride).Purity: 98.72%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mgPurity: 98%Clinical Data:Size: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Amisul

54、pride.html Amisulpride(DAN 2163) Cat. No.: HY-14545 HYPERLINK https:/www.MedChemE/amisulpride-hydrochloride.html Amisulpride HYPERLINK https:/www.MedChemE/amisulpride-hydrochloride.html HYPERLINK https:/www.MedChemE/amisulpride-hydrochloride.html hydrochloride(DAN 2163 hydrochloride) Cat. No.: HY-14

55、545AAmisulpride is a dopamine D /D receptor2 3antagonist with Ks of 2.8 and 3.2 nM for humanidopamine D2 D3and , respectively.Amisulpride hydrochloride is a dopamine D /D2 3receptor antagonist with Ks of 2.8 and 3.2 nMifor human dopamine D2 and D3, respectively.Purity: 99.96%Clinical Data: LaunchedS

56、ize: 10 mM 1 mL, 100 mg, 200 mg, 500 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/amisulpride-d5.html Amisulpride-d5 HYPERLINK https:/www.MedChemE/amisulpride-d5.html HYPERLINK https:/www.MedChemE/amisulpride-d5-n-oxide.html Amisulpride-d5 HYPERLINK https:/www.M

57、edChemE/amisulpride-d5-n-oxide.html HYPERLINK https:/www.MedChemE/amisulpride-d5-n-oxide.html N-OxideCat. No.: HY-14545S Cat. No.: HY-14545S1Amisulpride-d5 is the deuterium labeledAmisulpride. Amisulpride is a dopamine D /D2 3receptor antagonist with Ks of 2.8 and 3.2 nMifor human dopamine D2 and D3

58、, respectively.Amisulpride-d5 N-Oxide is the deuterium labeledAmisulpride. Amisulpride is a dopamine D /D2 3receptor antagonist with Ks of 2.8 and 3.2 nMifor human dopamine D and , respectively.2 D3Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical Data: No Develop

59、ment ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/Ansofaxine_hydrochloride.html Ansofaxine HYPERLINK https:/www.MedChemE/Ansofaxine_hydrochloride.html HYPERLINK https:/www.MedChemE/Ansofaxine_hydrochloride.html hydrochloride(LY03005; LPM570065) Cat. No.: HY-U00096 HYPERLINK https:/www.Med

60、ChemE/aramisulpride.html Aramisulpride(R-(+)-Amisulpride) Cat. No.: HY-109167Ansofaxine hydrochloride (LY03005; LPM570065) is atriple reuptake inhibitor; inhibits serotonin,dopamine and norepinephrine reuptake with IC50values of 723, 491 and 763 nM, respectively.Aramisulpride is a dopamine D2 recept