Histamine-Receptor-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html Histamine HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html ReceptorHistamine Receptors are a class of G protein-coupled receptors with histamine as their endogeno

2、us ligand. There are four knownhistamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to thefamily of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, isexpressed through

3、out the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the centralnervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, whichleads to activation of Protein Kinase A. Histamine H3 rec

4、eptors are expressed in the central nervous system and to a lesser extentthe peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamineturnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has bee

5、n shown to be involved inmediating eosinophil shape change and mast cell chemotaxis.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html Histamine HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html Recep

6、tor HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html Inhibitors, HYPERLINK https:/www.Me

7、dChemE/Targets/Histamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html Modulators HYPERLINK https:/www.MedChemE/Targets/Histamine Recept

8、or.html HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html HYPERLINK https:/www.MedChemE/Targets/Histamine Receptor.html Activators HYPERLINK https:/www.MedChemE/r-minus-methylhistamine-dihydrobromide.html (R)-(-)-Methylhista

9、mine HYPERLINK https:/www.MedChemE/r-minus-methylhistamine-dihydrobromide.html HYPERLINK https:/www.MedChemE/r-minus-methylhistamine-dihydrobromide.html dihydrobromide HYPERLINK https:/www.MedChemE/r-minus-methylhistamine-dihydrobromide.html HYPERLINK https:/www.MedChemE/r-minus-methylhistamine-dihy

10、drochloride.html (R)-(-)-Methylhistamine HYPERLINK https:/www.MedChemE/r-minus-methylhistamine-dihydrochloride.html HYPERLINK https:/www.MedChemE/r-minus-methylhistamine-dihydrochloride.html dihydrochlorideCat. No.: HY-100999 Cat. No.: HY-W014941(R)-(-)-Methylhistamine dihydrobromide is apotent, sel

11、ective and brain-penetrant agonist ofH3 histamine receptor, with a K of 50.3 nM.d(R)-(-)-Methylhistamine dihydrobromide canenhance memory retention, attenuates memoryimpairment in rats.(R)-(-)-Methylhistamine dihydrochloride is apotent, selective and brain-penetrant agonist ofH3 histamine receptor,

12、with a K of 50.3 nM.d(R)-(-)-Methylhistamine dihydrochloride canenhance memory retention, attenuates memoryimpairment in rats.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/rac-methotri

13、meprazine-d3-hydrochloride.html (Rac)-Levomepromazine-d3 HYPERLINK https:/www.MedChemE/rac-methotrimeprazine-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/rac-methotrimeprazine-d3-hydrochloride.html hydrochloride(Rac)-Methotrimeprazine-d3 hydrochloride) Cat. No.: HY-19489S1 HYPERLINK https:/ww

14、w.MedChemE/z-chlorprothixene-d6-hydrochloride.html (Z)-Chlorprothixene-d6 HYPERLINK https:/www.MedChemE/z-chlorprothixene-d6-hydrochloride.html HYPERLINK https:/www.MedChemE/z-chlorprothixene-d6-hydrochloride.html hydrochlorideCat. No.: HY-B0274S(Rac)-Levomepromazine-d3(Rac)-Methotrimeprazine-d3) hy

15、drochloride is alabelled racemic Methotrimeprazine, which is aphenothiazine which has antagonist actions atmultiple neurotransmitter receptor sites,including dopaminergic, cholinergic, serotonin(Z)-Chlorprothixene-d6 hydrochloride is thedeuterium labeled Chlorprothixene. Chlorprothixeneis a dopamine

16、 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, respectively. Antipsychotic activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HY

17、PERLINK https:/www.MedChemE/z-lafutidine.html (Z)-Lafutidine(Z)-FRG-8813) Cat. No.: HY-121406 HYPERLINK https:/www.MedChemE/z-olopatadine-d3-hydrochloride.html (Z)-Olopatadine-d3 HYPERLINK https:/www.MedChemE/z-olopatadine-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/z-olopatadine-d3-hydrochl

18、oride.html hydrochlorideCat. No.: HY-B0426AS1(Z)-Lafutidine (Z)-FRG-8813) is a potenthistamine H2 receptor antagonist.(Z)-Lafutidine shows anti-secretory andgastroprotective activities.(Z)-Olopatadine-d3 (hydrochloride) is deuteriumlabeled Olopatadine (hydrochloride).Purity: 98%Clinical Data: No Dev

19、elopment ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/_plusmn_-Methotrimeprazine-D6.html ()-Levomepromazine-d6 HYPERLINK https:/www.MedChemE/_plusmn_-Methotrimeprazine-D6.html HYPERLINK https:/www.MedChemE/(plusmn)-Tazifyllin

20、e.html ()-Tazifylline()-Methotrimeprazine-d6; dl-Methotrimeprazine-d6) Cat. No.: HY-19489SCat. No.: HY-U00018()-Levomepromazine D6 ()-Methotrimeprazine D6)is the deuterium labeled Methotrimeprazine, whichis a D3 dopamine and Histamine H1 receptorantagonist.()-Tazifylline is a potent, selective andlo

21、ng-acting histamine H1 receptor antagonist.Purity: 98.0%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/4-methylhistamine-dihydrochloride.html 4-Methylhistamine HYPERLINK https:/www.MedChemE/4-methylhista

22、mine-dihydrochloride.html HYPERLINK https:/www.MedChemE/4-methylhistamine-dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChemE/4-methylhistamine-dihydrochloride.html HYPERLINK https:/www.MedChemE/a-987306.html A-987306Cat. No.: HY-107560 Cat. No.: HY-143644-Methylhistamine (dihydrochlo

23、ride) is the potentagonist of histamine 4 receptor (H4R).4-Methylhistamine (dihydrochloride) has thepotential for the research of immune-relateddiseases such as cancer and autoimmune disorders.A-987306 is a potent and oral bioavailablehistamine H antagonist, with s of 3.4 nM and4 Ki5.8 nM for rat H

24、, and human H . A-987306 shows4 4anti-inflammatory activity in mice peritonitismodel.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedCh

25、emE/ABT-239.html ABT-239Cat. No.: HY-12195 HYPERLINK https:/www.MedChemE/Acrivastine.html Acrivastine(BW825C) Cat. No.: HY-B1510ABT-239 is a novel, highly efficacious,non-imidazole class of H3R antagonist and atransient receptor potential vanilloid type 1(TRPV1) antagonist. .Acrivastine (BW825C) is

26、a short actinghistamine 1 receptor antagonist for thetreatment of allergic rhinitis.Purity: 98.49%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.37%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/acrivas

27、tine-d7.html Acrivastine HYPERLINK https:/www.MedChemE/acrivastine-d7.html HYPERLINK https:/www.MedChemE/acrivastine-d7.html D7(BW825C D7) Cat. No.: HY-B1510S HYPERLINK https:/www.MedChemE/acrivastine-d8.html Acrivastine-d8(BW825C-d8) Cat. No.: HY-B1510S1Acrivastine D7 (BW825C D7) is a deuterium lab

28、eledAcrivastine. Acrivastine is a short actinghistamine 1 receptor antagonist.Acrivastine-d8 (BW825C-d8) is the deuteriumlabeled Acrivastine. Acrivastine (BW825C) is ashort acting histamine 1 receptor antagonistfor the treatment of allergic rhinitis.Purity: 98%Clinical Data: No Development ReportedS

29、ize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/PF-3893787_hydrochloride.html Adriforant HYPERLINK https:/www.MedChemE/PF-3893787_hydrochloride.html HYPERLINK https:/www.MedChemE/PF-3893787_hydrochloride.html hydrochloride(PF-3893787 hyd

30、rochloride) Cat. No.: HY-19705B HYPERLINK https:/www.MedChemE/Alcaftadine.html Alcaftadine(R89674) Cat. No.: HY-17039Adriforant hydrochloride (PF-3893787hydrochloride) is a novel histamine H4receptor antagonist binding affinity (K=2.4 nM)iand is also a functional (K=1.56 nM) antagonist.iAlcaftadine

31、(R89674) is a histamine H1receptor antagonist, which is used to prevent eyeirritation brought on by allergic conjunctivitis.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.42%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPER

32、LINK https:/www.MedChemE/alcaftadine-d3.html Alcaftadine-D3 HYPERLINK https:/www.MedChemE/alcaftadine-d3.html HYPERLINK https:/www.MedChemE/alginic-acid.html Alginic HYPERLINK https:/www.MedChemE/alginic-acid.html HYPERLINK https:/www.MedChemE/alginic-acid.html acid(R89674-D3) Cat. No.: HY-17039SCat

33、. No.: HY-W127758Alcaftadine-D3 (R89674-D3) is a deuterium labeledAlcaftadine. Alcaftadine (HY-17039) is a H1histamine receptor antagonist.Alginic acid is a natural polysaccharide, whichhas been widely concerned and applied due to itsexcellent water solubility, film formation,biodegradability and bi

34、ocompatibility.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/alimemazine.html Alimemazine HYPERLINK https:/www.MedChemE/alimemazine.html HYPERLINK https:/www.MedChemE/Alimemazine-D6.htm

35、l Alimemazine HYPERLINK https:/www.MedChemE/Alimemazine-D6.html HYPERLINK https:/www.MedChemE/Alimemazine-D6.html D6(Trimeprazine) Cat. No.: HY-12752 (Trimeprazine D6) Cat. No.: HY-12752SAlimemazine is a phenothiazine derivative that isgenerally used as an antipruritic agent and also ahemagglutinin

36、(HA)-receptorantagonist.Alimemazine (Trimeprazine) is also actsas a partial agonist against the histamine H1receptor (H1R) and other GPCRs.Alimemazine D6 is deuterium labeled Alimemazine,which is an antihistamine.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 99.43%Clinical Data: No Devel

37、opment ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Alimemazine_hemitartrate.html Alimemazine HYPERLINK https:/www.MedChemE/Alimemazine_hemitartrate.html HYPERLINK https:/www.MedChemE/Alimemazine_hemitartrate.html hemitartrate(Trimeprazine hemitartrate) Cat. No.: HY-12752A HY

38、PERLINK https:/www.MedChemE/alimemazine-hemitartrate-d6-l-tartrate.html Alimemazine HYPERLINK https:/www.MedChemE/alimemazine-hemitartrate-d6-l-tartrate.html HYPERLINK https:/www.MedChemE/alimemazine-hemitartrate-d6-l-tartrate.html hemitartrate-d6 HYPERLINK https:/www.MedChemE/alimemazine-hemitartra

39、te-d6-l-tartrate.html HYPERLINK https:/www.MedChemE/alimemazine-hemitartrate-d6-l-tartrate.html L-TartrateCat. No.: HY-12752ASAlimemazine hemitartrate is a phenothiazinederivative that is generally used as anantipruritic agent and also a hemagglutinin(HA)-receptor antagonist.Alimemazine hemitartrate

40、-d6 (L-Tartrate) is thedeuterium labeled Alimemazine hemitartrate.Alimemazine hemitartrate is a phenothiazinederivative that is generally used as anantipruritic agent and also a hemagglutinin(HA)-receptor antagonist.Purity: 98.46%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 9

41、8%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html Amitriptyline HYPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html HYPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html hydrochloride HYPERLINK https:/www.MedCh

42、emE/amitriptyline-hydrochloride.html HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.html Amitriptyline-d3 HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.html hydrochlorideCat. No.: HY-B0527A Cat. No.: HY-13

43、5096Amitriptyline hydrochloride is an inhibitor ofserotonin reuptake transporter (SERT) andnoradrenaline reuptake transporter (NET), with Ksiof 3.45 nM and 13.3 nM for human SERT and NET,respectively.Amitriptyline-d3 hydrochloride is the deuteriumlabeled Amitriptyline (hydrochloride).Purity: 99.56%C

44、linical Data: LaunchedSize: 10 mM 1 mL, 500 mg, 1 g, 5 gPurity: 98%Clinical Data: No Development ReportedSize: 2.5 mg, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/amitriptyline-d6-hydrochloride.html Amitriptyline-d6 HYPERLINK https:/www.MedChemE/amitriptyline-d6-hydrochloride.html HYPERLINK http

45、s:/www.MedChemE/amitriptyline-d6-hydrochloride.html hydrochlorideCat. No.: HY-B0527AS HYPERLINK https:/www.MedChemE/Antazoline-hydrochloride.html Antazoline HYPERLINK https:/www.MedChemE/Antazoline-hydrochloride.html HYPERLINK https:/www.MedChemE/Antazoline-hydrochloride.html hydrochloride(Phenazoli

46、ne hydrochloride) Cat. No.: HY-B1067Amitriptyline-d6 hydrochloride is the deuteriumlabeled Amitriptyline hydrochloride.Antazoline hydrochloride is a 1st generationantihistamine with also anticholinergic propertiesused to relieve nasal congestion and in eye drops.Purity: 98%Clinical Data: No Developm

47、ent ReportedSize: 2.5 mg, 1 mg, 5 mg, 25 mgPurity: 99.43%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/Antihistamine-1.html Antihistamine-1 HYPERLINK https:/www.MedChemE/Antihistamine-1.html HYPERLINK https:/www.MedChemE/Asenapine.html AsenapineCat. No.: HY-100238(Org

48、 5222) Cat. No.: HY-10121Antihistamine-1 is a H1-antihistamine (K=6.9inM) with acceptable blood-brain barrierpenetration and also an inhibitor of CYP2D6 andhERG channel with IC s of 5.4 and 0.8 M,50respectively.Asenapine (Org 5222), an atypical antipsychotic,is an antagonist of serotonin receptors (

49、pK:i8.4-10.5), adrenoceptors (pK: 8.9-9.5),idopamine receptors (pK: 8.9-9.4) andihistamine receptors (pK: 8.2-9.0).iPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.81%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/asenapine-d3.

50、html Asenapine-d3 HYPERLINK https:/www.MedChemE/asenapine-d3.html HYPERLINK https:/www.MedChemE/asenapine-d7.html Asenapine-d7(Org 5222-d3) Cat. No.: HY-10121S (Org 5222-d7) Cat. No.: HY-10121S1Asenapine-d3 (Org 5222-d3) is the deuteriumlabeled Asenapine.Asenapine-d7 (Org 5222-d7) is the deuteriumla

51、beled Asenapine.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/astemizole.html Astemizole(R 43512) Cat. No.: HY-12532 HYPERLINK

52、https:/www.MedChemE/astemizole-d3.html Astemizole-d3Cat. No.: HY-12532SAstemizole (R 43512), a second-generationantihistamine drug to diminish allergic symptomswith a long duration of action, is a histamineH1-receptor antagonist, with an IC of 4 nM.50Astemizole-d3 is the deuterium labeled Astemizole

53、.Astemizole (R 43512), a second-generationantihistamine drug to diminish allergic symptomswith a long duration of action, is a histamineH1-receptor antagonist, with an IC of 4 nM.50Purity: 99.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No De

54、velopment ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/Azacyclonol.html Azacyclonol(-pipradol) Cat. No.: HY-B0530 HYPERLINK https:/www.MedChemE/azatadine.html AzatadineCat. No.: HY-B0170Azacyclonol (-pipradol), a metabolite ofTerfenadine, is a central depressant agent.Azacyclonol is a gan

55、glion-blocking agent.Azacyclonol can be used to diminishpsychoses-induced hallucinations.Azatadine is an histamine and cholinergicinhibitor with IC50 of 6.5 nM and 10 nM,respectively. Target: Histamine ReceptorAzatadine, a new antihistamine, was evaluated forits efficacy in 20 patients with chronic

56、allergicrhinitis.Purity: 99.99%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 500 mg, 1 g, 5 gPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Azatadine-dimaleate.html Azatadine HYPERLINK https:/www.MedChemE/Azatadine-dimaleate.html HYPERLINK https:/www.MedCh

57、emE/Azatadine-dimaleate.html dimaleate(Azatadine maleate) Cat. No.: HY-B0170A HYPERLINK https:/www.MedChemE/azelastine.html AzelastineCat. No.: HY-B0462AAzatadine dimaleate is an histamine andcholinergic inhibitor with IC50 of 6.5 nM and 10nM, respectively. Target: Histamine ReceptorAzatadine, a new

58、 antihistamine, was evaluated forits efficacy in 20 patients with chronic allergicrhinitis.Azelastine, an antihistamine, is a potent andselective histamine 1 (H ) antagonist.1Azelastine can be used for the research ofallergic rhinitis, asthma, diabetic hyperlipidemicand SARS-CoV-2.Purity: 99.76%Clin

59、ical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Azelastine-hydrochloride.html Azelastine HYPERLINK https:/www.MedChemE/Azelastine-hydrochloride.html HYPERLINK https:/www.MedChemE/Azelastine-hydrochloride.html h

60、ydrochloride HYPERLINK https:/www.MedChemE/Azelastine-hydrochloride.html HYPERLINK https:/www.MedChemE/azelastine-13c-d3.html Azelastine-13C,d3Cat. No.: HY-B0462 Cat. No.: HY-B0462ASAzelastine hydrochloridem, an antihistamine, is apotent and selective histamine 1 (H )1antagonist. Azelastine hydrochl