Histamine Receptor

Histamine Receptors are a class of G protein-coupled receptors with histamine as their endogenous 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 throughout 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 receptors 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 been shown to be involved inmediating eosinophil shape change and mast cell chemotaxis

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Histamine Receptor Antagonists Inhibitors Agonists Modulators amp Activators

(plusmn)-Methotrimeprazine D6 (dl-Methotrimeprazine D6) Cat No HY-19489S

(plusmn)-Methotrimeprazine (D6) is the deuteriumlabeled Methotrimeprazine which is a D3 dopamineand Histamine H1 receptor antagonist

Purity gt98Clinical Data No Development ReportedSize 1 mg

(plusmn)-TazifyllineCat No HY-U00018

(plusmn)-Tazifylline is a potent selective andlong-acting antagonisthistamine H1 receptor

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

ABT-239Cat No HY-12195

ABT-239 is a novel highly efficaciousnon-imidazole class of antagonist and aH3Rtransient receptor potential vanilloid type 1( ) antagonist TRPV1

Purity 9906Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg

Acrivastine (BW825C) Cat No HY-B1510

Acrivastine (BW825C) is a short acting receptor antagonist for thehistamine 1

treatment of allergic rhinitis

Purity 9800Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

Adriforant hydrochloride (PF-3893787 (hydrochloride)) Cat No HY-19705B

Adriforant hydrochloride (PF-3893787hydrochloride) is a novel histamine H4

antagonist binding affinity ( =24 nM)receptor Ki

and is also a functional ( =156 nM) antagonistKi

Purity gt980Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Alcaftadine (R89674) Cat No HY-17039

Alcaftadine(R89674) is a H1 histamine receptorantagonist which is used to prevent eyeirritation brought on by allergic conjunctivitis

Purity 9717Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

Alimemazine D6 (Trimeprazine D6) Cat No HY-12752S

Alimemazine D6 is deuterium labeled Alimemazinewhich is an antihistamine

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Antazoline hydrochloride (Phenazoline hydrochloride) Cat No HY-B1067

Antazoline hydrochloride is a 1st generationantihistamine with also anticholinergic propertiesused to relieve nasal congestion and in eye drops

Purity 9936Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Antihistamine-1Cat No HY-100238

Antihistamine-1 is a ( =69H1-antihistamine Ki

nM) with acceptable blood-brain barrierpenetration and also an inhibitor of andCYP2D6

with s of 54 and 08 μMhERG channel IC50

respectively

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Astemizole (R 43512) Cat No HY-12532

Astemizole (R 43512) a second-generationantihistamine drug to diminish allergic symptomswith a long duration of action is a histamine

antagonist with an of 4 nMH1-receptor IC50

Purity gt980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg

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AzatadineCat No HY-B0170

Azatadine is an histamine and cholinergicinhibitor with IC50 of 65 nM and 10 nMrespectively Target Histamine ReceptorAzatadine a new antihistamine was evaluated forits efficacy in 20 patients with chronic allergicrhinitis

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Azatadine dimaleate (Azatadine maleate) Cat No HY-B0170A

Azatadine dimaleate is an histamine andcholinergic inhibitor with IC50 of 65 nM and 10nM respectively Target Histamine ReceptorAzatadine a new antihistamine was evaluated forits efficacy in 20 patients with chronic allergicrhinitis

Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

AzelastineCat No HY-B0462A

Azelastine is a potent second-generationselective histamine antagonist

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg

Azelastine hydrochlorideCat No HY-B0462

Azelastine hydrochloride is a potentsecond-generation selective histamineantagonist

Purity 9995Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg

Bamirastine (TAK-427) Cat No HY-101601

Bamirastine inhibits ligand binding to recombinanthuman histamine H receptors ( ) with an1 rhH R1

value of 173 nMIC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Bavisant (JNJ-31001074) Cat No HY-14880

Bavisant (JNJ-31001074) is a highly selectiveorally active antagonist of the human H3 receptorwith a novel mechanism of action involvingwakefulness and cognition with potential as atreatment for ADHD

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Bavisant dihydrochlorideCat No HY-14880A

Bavisant Hcl (JNJ-31001074) is a highly selectiveorally active antagonist of the human H3 receptorwith a novel mechanism of action involvingwakefulness and cognition with potential as atreatment for ADHD

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Bavisant dihydrochloride hydrate (JNJ31001074AAC) Cat No HY-14880B

Bavisant dihydrochloride hydrate (JNJ31001074AAC)is a highly selective orally active antagonist ofthe human H3 receptor with a novel mechanism ofaction involving wakefulness and cognition withpotential as a treatment for ADHD

Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

Bepotastine BeslilateCat No HY-A0015

Bepotastine Beslilate (Bepreve) is a histamine H1receptor anatagonist

Purity 9936Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

Betahistine dihydrochlorideCat No HY-B0524A

Betahistine dihydrochloride is a histamine H3receptors inhibitor used as an antivertigo drug

Purity 9988Clinical Data LaunchedSize 10 mM times 1 mL 1 g 5 g 10 g

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BilastineCat No HY-14447

Bilastine is a selective histamine H1 receptorantagonist used for treatment of allergicrhinoconjunctivitis and urticaria

Purity 9995Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

BMY-25271Cat No HY-100191

BMY-25271 is a histamine H2 receptorantagonist

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Brompheniramine maleateCat No HY-B0480

Brompheniramine maleate is a histamine H1receptors antagonist

Purity 9995Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg

Carbinoxamine maleate saltCat No HY-B1589A

Carbinoxamine maleate salt is a histamine H1 antagonistreceptor

Purity 9978Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg

CarebastineCat No HY-121356

Carebastine is the active metabolite of EbastineCarebastine is a histamine H1 receptorantagonist Carebastine inhibits VEGF-inducedHUVEC and HPAEC proliferation migration andangiogenesis in a dose-dependent manner

Purity gt98Clinical DataSize 1 mg

CetirizineCat No HY-17042

Cetirizine a second-generation antihistamine isa major metabolite of hydroxyzine and a racemicselective H1 receptor inverse agonist used in thetreatment of allergies hay fever angioedema andurticaria

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Cetirizine D4 dihydrochlorideCat No HY-17042AS

Cetirizine D4 2Hcl is deuterium labeledCetirizine which is a major metabolite ofhydroxyzine and a racemic selective H1 receptorinverse agonist

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Cetirizine D8 dihydrochlorideCat No HY-17042AS1

Cetirizine D8 2Hcl is deuterium labeledCetirizine which is a major metabolite ofhydroxyzine and a racemic selective H1 receptorinverse agonist

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Cetirizine dihydrochloride (P071) Cat No HY-17042A

Cetirizine dihydrochloride a second-generationantihistamine is a major metabolite ofhydroxyzine and a racemic selective H1 receptorinverse agonist used in the treatment ofallergies hay fever angioedema and urticaria

Purity 9917Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg

Chlorcyclizine hydrochlorideCat No HY-112067A

Chlorcyclizine hydrochloride is a histamine H1antagonist

Purity 9990Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg

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Chloropyramine hydrochlorideCat No HY-B1305

Chloropyramine hydrochloride is a histamine antagonist which can also inhibit thereceptor H1

biochemical function of and VEGFR-3 FAK

Purity 9930Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg

Chlorpheniramine maleate (Chlorphenamine maleate) Cat No HY-B0286A

Chlorpheniramine maleate is an histamine H1receptor antagonist with IC50 of 12 nM

Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 1 g 5 g

ChlorphenoxamineCat No HY-B1607

Chlorphenoxamine is an antihistamine andanticholinergic used as an antipruritic andantiparkinsonian agent

Purity 9509Clinical Data LaunchedSize 10 mM times 1 mL 50 mg

CI-949Cat No HY-U00364

CI-949 is an allergic mediator release inhibitorwhich inhibits histamine leukotriene C D4 4

and ( )LTC4 LTD4 thromboxane B ( )2 TXB2

release with s of 114 μM 05 μM and 01 μMIC50

respectively

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Cimetidine (SKF-92334) Cat No HY-14289

Cimetidine is a histamine-2 (H2) receptorantagonist

Purity gt980Clinical Data LaunchedSize 1 g 5 g 10 g

CinnarizineCat No HY-B1090

Cinnarizine is an antihistamine and a calciumchannel blocker promote cerebral blood flow usedto treat cerebral apoplexy post-trauma cerebralsymptoms and cerebral arteriosclerosis

Purity 9967Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Cipralisant (GT-2331) Cat No HY-106993

Cipralisant is a potent and selective histamine antagonist in vivo and an agonist inH3 receptor

vitro with a of 99 for histamine H3 receptorpKi

and a of 047 nM for rat histamine H3 receptorKi

Cipralisant has entered in clinical trials for thetreatment of attention-deficithellip

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Ciproxifan (FUB-359) Cat No HY-14567

Ciproxifan(FUB-359) is a highly potent andselective histamin H3-receptor antagonist withIC50 of 92 nM with low apparent affinity atother receptor subtypes

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Ciproxifan maleate (FUB 359 maleate) Cat No HY-15289

Ciproxifan maleate(FUB-359 maleate) is a highlypotent and selective histamin H3-receptorantagonist with IC50 of 92 nM with low apparentaffinity at other receptor subtypes

Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg

Clemastine fumarate (HS-592 (fumarate) Meclastine (fumarate)) Cat No HY-B0298A

Clemastine (fumarate) (HS-592 (fumarate)) is aselective histamine H1 receptor antagonist withIC of 3 nM50

Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg

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ClemizoleCat No HY-30234

Clemizole is an H1 histamine receptorantagonist is found to substantially inhibit HCVreplication The of Clemizole for RNA bindingIC50

by is 24plusmn1 nM whereas its for viralNS4B EC50

replication is 8 microM

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Clemizole hydrochlorideCat No HY-30234A

Clemizole hydrochloride is an H1 histamine antagonist is found to substantiallyreceptor

inhibit replication The of ClemizoleHCV IC50

for RNA binding by is 24plusmn1 nM whereas itsNS4B for viral replication is 8 microMEC50

Purity 9932Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

CP-66948Cat No HY-19048

CP-66948 is a antagonisthistamine H2-receptorwith gastric antisecretory activity and mucosalprotective properties

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Cyproheptadine hydrochloride sesquihydrateCat No HY-B1165

Cyproheptadine hydrochloride sesquihydrate is anantihistamine and is an antagonist of serotoninand histamine2

Purity 9920Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Decloxizine (UCB-1402 NSC289116) Cat No HY-17582

Decloxizine(UCB-1402 NSC289116) is a histamine 1receptor antagonist

Purity gt98Clinical Data LaunchedSize 50 mg 100 mg 500 mg

Decloxizine dihydrochloride (UCB 1402 dihydrochloride) Cat No HY-A0075

Decloxizine dihydrochloride(UCB-1402 NSC289116)is a histamine 1 receptor antagonist

Purity gt980Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg

Desloratadine (Sch34117) Cat No HY-B0539

Desloratadine(Sch34117) is a potent antagonist forhuman histamine H1 receptor used to treatallergies

Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg

Dexchlorpheniramine maleate (S-(+)-Chlorpheniramine maleate salt) Cat No HY-B1062

Dexchlorpheniramine maleate is an antihistaminewith anticholinergic properties used to treatallergic conditions

Purity gt980Clinical Data LaunchedSize 10 mM times 1 mL 200 mg

DimenhydrinateCat No HY-B1215

Dimenhydrinate is an anti-emetic andanti-histamine commonly available over-the-counteras a motion sickness remedy

Purity 9989Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Diphenhydramine hydrochlorideCat No HY-B0303A

Diphenhydramine hydrochloride a histamine H1antagonist used as an antiemetic antitussive fordermatoses and pruritus for hypersensitivityreactions as a hypnotic an antiparkinson and asan ingredient in common cold preparations

Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 250 mg 500 mg 5 g

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Diphenylpyraline hydrochloride (4-Diphenylmethoxy-1-methylpiperidine hydrochloride) Cat No HY-B0970

Diphenylpyraline hydrochloride(4-Diphenylmethoxy-1-methylpiperidinehydrochloride) is a first-generation antihistaminewith anticholinergic effects acts as a dopaminereuptake inhibitor shows to be useful in thetreatment of Parkinsonism

Purity 9902Clinical Data LaunchedSize 10 mM times 1 mL 1 g

Doxylamine D5 succinateCat No HY-A0069S

Doxylamine D5 succinate is deuterium labeledDoxylamine which is a first generationantihistamine

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Doxylamine succinateCat No HY-A0069

Doxylamine (succinate) is a first generationantihistamine can be used by itself as ashort-term sedative and in combination with otherdrugs to provide night-time allergy and coldrelief

Purity 9977Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Ebastine (LAS-W 090 RP64305) Cat No HY-B0674

Ebastine(LAS-W 090RP64305) is a long-acting andselective H1-histamine receptor antagonistTarget Histamine H1 Receptor Ebastine is a H1antihistamine with low potential for causingdrowsiness

Purity 9996Clinical Data Phase 4Size 10 mM times 1 mL 500 mg 1 g 5 g

Ebrotidine (FI3542) Cat No HY-15538

Ebrotidine(FI 3542) is a competitive H2-receptorantagonist (Ki= 1275 nM) with a potentantisecretory activity and evidencedgastroprotection

Purity 9778Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg

Epinastine (WAL801) Cat No HY-B0640

Epinastine(WAL801) is an antihistamine and mastcell stabilizer that is used in eye drops to treatallergic conjunctivitis

Purity gt980Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg

Famotidine (MK-208) Cat No HY-B0377

Famotidine (MK-208) is a competitive histamineH2-receptor antagonist Its main pharmacodynamiceffect is the inhibition of gastric secretion

Purity 9817Clinical Data LaunchedSize 10 mM times 1 mL 1 g 5 g

Fenspiride HydrochlorideCat No HY-A0027

Fenspiride Hcl is an α adrenergic and H1 histaminereceptor antagonist

Purity 9903Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Fexofenadine D6 (MDL-16455 D6) Cat No HY-B0801S

Fexofenadine D6 is deuterium labeled isFexofenadine which is an antihistaminepharmaceutical drug

Purity gt980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Fexofenadine hydrochloride (MDL-16455 hydrochloride

Terfenidine carboxylate hydrochloride) Cat No HY-B0801A

Fexofenadine hydrochloride (MDL-16455hydrochloride) a antagonist is anH1Ranti-allergic agent used in seasonal allergicrhinitis and chronic idiopathic urticarial (personaged ge16 years)

Purity 9961Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg

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FRG8701Cat No HY-U00238

FRG-8701 is a new Histamine H -receptor2

antagonist with an of ranging from 025 toIC50

043 μM

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

GSK189254A (GSK189254) Cat No HY-14111

GSK189254A (GSK189254) is a novel potent andselective histamine receptor antagonist withH3

values of 959-990 and 851-917 for humanpKi

and rat H3 respectively

Purity 9858Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg

H3 receptor antagonist 1Cat No HY-U00269

H3 receptor antagonist 1 is an antagonist of used in the research ofhistamine H3 receptor

neurological disease

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

H3 receptor-MO-1Cat No HY-U00339

H3 receptor-MO-1 is a modulator of histamine H3receptor

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

H3R-IN-1 HydrochlorideCat No HY-112219A

H3R-IN-1 Hydrochloride is a histamine receptor ( ) inverse agonist extracted from patent3 H3R

WO2013107336A1 compound example 2

Purity 9552Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

H4 Receptor antagonist 1Cat No HY-114025

H4 Receptor antagonist 1 is a potent and selective inverse agonist with anhistamine H4 receptor

of 19 nMIC50

Purity 9970Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

H4R antagonist 1Cat No HY-111501

H4R antagonist 1 is a potent and highly selective ( ) antagonist withhistamine H4 receptor H4R

an IC of 27 nM H4R antagonist 1 does not show50

any noticeable binding affinity to other subtypesof histamine receptors H1R H2R and H3R

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Histamine (Ergamine) Cat No HY-B1204

Histamine is an organic nitrogenous compoundinvolved in local immune responses as well asregulating physiological function in the gut andacting as a neurotransmitter

Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Histamine phosphate (Histamine diphosphate) Cat No HY-A0129

Histamine (phosphate) diphosphate is a potentagonist of histamine receptors and vasodilator Itcan activate nitric oxide synthetase

Purity 9979Clinical Data LaunchedSize 10 mM times 1 mL 1 g

HydroxyzineCat No HY-B0548

Hydroxyzine is a histamine H1-receptor antagonist

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

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Hydroxyzine D4 dihydrochlorideCat No HY-B0548AS

Hydroxyzine D4 2Hcl is deuterium labeledHydroxyzine which is a histamine H1-receptorantagonist

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Hydroxyzine dihydrochlorideCat No HY-B0548A

Hydroxyzine dihydrochloride is a histamineH1-receptor antagonist Target HistamineH1-Receptor Hydroxyzine dihydrochloride inhibitscarbachol (10 μM)-induced serotonin release by 34at 10 μM by 25 1 μM and by 17 01 μM inpretreated bladder slices for 60 min

Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg

Hydroxyzine pamoateCat No HY-B0895

Hydroxyzine pamoate is a histamine H1-receptorantagonist Target Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-inducedserotonin release by 34 at 10 μM by 25 1 μM andby 17 01 μM in pretreated bladder slices for 60min

Purity gt98Clinical Data LaunchedSize 100 mg

JNJ-39758979Cat No HY-101189

JNJ-39758979 is a selective high-affinity antagonist with a ofhistamine H receptor4 Ki

125 nM

Purity 9801Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg

JNJ-5207852Cat No HY-12190

JNJ-5207852 is a selective and potent histamine receptor (H R) antagonist with of 89H3 3 pK si

924 for rat and human H R respectively3

Purity gt980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

JNJ-7777120Cat No HY-13508

JNJ-7777120 is a selective H4R antagonist with Kiof 4 plusmn1 nM exhibits gt1000-fold selectivityover the other histamin receptors

Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

Ketotifen fumarate (HC 20511 fumarate) Cat No HY-B0157A

Ketotifen (fumarate) is a second-generationnoncompetitive H1-antihistamine and mast cellstabilizer which is used to prevent asthmaattacks

Purity 9992Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 1 g

KP136 (AL136) Cat No HY-U00168

KP136 is an orally effective antiallergic agentThe is 761 μgmL for andIC50 histamine release63 ugmL for degranulation

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Lafutidine (FRG-8813) Cat No HY-B0160

Lafutidine a newly developed histamineH(2)-receptor antagonist inhibits gastric acidsecretion

Purity 9786Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg

Latrepirdine dihydrochloride (Dimebolin dihydrochloride) Cat No HY-14537

Latrepirdine dihydrochloride is a neuroactivecompound with antagonist activity athistaminergic α-adrenergic and serotonergicreceptors Latrepirdine stimulates amyloidprecursor protein (APP) catabolism and

( ) secretionamyloid-β Aβ

Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

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Levodropropizine (DF-526 (S)-(-)-Dropropizine) Cat No HY-B1895

Levodropropizine (DF-526) is a histamine receptorinhibitor Levodropropizine is an effective andvery well tolerated peripheral antitussive drug

Purity 9992Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg

LodoxamideCat No HY-14270

Lodoxamide is an antiallergic compound acting as amast-cell stabilizer for the treatment of asthmaand allergic conjunctivitis

Purity gt980Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg

Lodoxamide tromethamine (U 42585 E) Cat No HY-16289

Lodoxamide tromethamine (U 42585 E) is amedication for the treatment of prophylaxis ofmast cell-mediated allergic disease

Purity 9937Clinical Data LaunchedSize 10 mM times 1 mL 1 mg 5 mg

Loratadine (SCH 29851 Loratidine) Cat No HY-17043

Loratadine(SCH-29851) is a selective inverseperipheral histamine H1-receptor agonist with anIC50 of gt32 μM

Purity 9995Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

MebhydrolinCat No HY-B1303A

Mebhydrolin is a specific histamine H1

antagonistreceptor

Purity 9946Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Mebhydrolin napadisylate (Mebhydroline 15-naphthalenedisulfonate salt) Cat No HY-B1303

Mebhydrolin napadisylate is a specific antagonisthistamine H receptor1

Purity 9953Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Meclizine dihydrochloride (Meclozine dihydrochloride NSC28728) Cat No HY-B0349

Meclizine dihydrochloride is a histamine H1receptor antagonist used to treat nausea andmotion sickness Target Histamine H1 ReceptorMeclizine dihydrochloride is a histamine H1receptor antagonist used to treat nausea andmotion sickness possesseshellip

Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 5 g

Mepyramine maleate (Pyrilamine maleate) Cat No HY-B1281

Mepyramine maleate a first generationantihistamine is an antagonist of histamine H1

with s of 08 nM 5200 nM andreceptor Kd

gt3000 nM for H1 H2 and H3 receptorrespectively and a of 94 for H1 receptorpKd

Purity gt990Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg

Mequitazine (LM-209) Cat No HY-B2168

Mequitazine is a potent nonsedative andlong-acting histamine antagonistH1

Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

Metiamide (SKampF 92058) Cat No HY-15540

Metiamide (SKampF 92058) is a histamineH2-receptor antagonist developed from another H2antagonist burimamide

Purity 9731Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg

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Mianserin (Mianserine) Cat No HY-B0188

Mianserin is a H1 receptor inverse agonist and isa psychoactive agent of the tetracyclicantidepressant

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Mianserin hydrochloride (Org GB 94) Cat No HY-B0188A

Mianserin hydrochloride is a H1 receptor inverseagonist and is a psychoactive agent of thetetracyclic antidepressant Target H1 receptorMianserin is a psychoactive drug of thetetracyclic antidepressant (TeCA) therapeuticfamily

Purity 9979Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg

MizolastineCat No HY-B0164

Mizolastine is a histamine H1-receptor antagonistwith IC50 of 47 nM used in the treatment of hayfever (seasonal allergic rhinitis) hives andother allergic reactions

Purity 9933Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Mizolastine dihydrochlorideCat No HY-B0164A

Mizolastine dihydrochloride is a histamineH1-receptor antagonist with IC50 of 47 nM used inthe treatment of hay fever (seasonal allergicrhinitis) hives and other allergic reactions

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

MK-0249Cat No HY-U00076

MK-0249 is a potent histamine H3 receptorantagonist with of 17 nM for human H3Ki

Purity gt98Clinical Data Phase 2Size 1 mg 5 mg 10 mg 20 mg

N-Acetylhistamine (N-Omega-acetylhistamine) Cat No HY-112175

N-Acetylhistamine is a histamine metaboliteN-acetylhistamine can be used as a potentialbiomarker of histidine metabolism foranaphylactoid reactions

Purity 9899Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg

Nedocromil (FPL 59002) Cat No HY-13448

Nedocromil suppresses the action or formation ofmultiple mediators including histamine

( ) and leukotriene C4 LTC4 prostaglandin D2

( )PGD2

Purity 9566Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg

Nedocromil sodium (FPL 59002KP Nedocromil disodium salt) Cat No HY-16344

Nedocromil sodium suppresses the action orformation of multiple mediators including

( ) andhistamine leukotriene C4 LTC4

( )prostaglandin D2 PGD2

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

NiperotidineCat No HY-15539

Niperotidine is a histamine H2-receptorantagonist

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

NizatidineCat No HY-B0310

Nizatidine is a histamine H2 receptor antagonistwith low toxicity that inhibits gastric acidsecretion

Purity 9949Clinical Data LaunchedSize 10 mM times 1 mL 1 g 5 g

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Olopatadine hydrochloride (ALO4943A KW4679) Cat No HY-B0426A

Olopatadine hydrochloride (ALO4943A) is ahistamine blocker used to treat allergicconjunctivitis

Purity 9955Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg

Osthole (NSC 31868 Osthol Ostol) Cat No HY-N0054

Osthole is a natural antihistamine alternativeOsthole may be a potential inhibitor of

activityhistamine H receptor1

Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 250 mg 1 g 5 g

Pemirolast potassium (TWT-8152 BMY 26517) Cat No HY-B0538A

Pemirolast potassium (TWT-8152) is a histamine H1antagonist and mast cell stabilizer that acts asan antiallergic agent

Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

Peptide 401Cat No HY-12537

Peptide 401 a potent mast cell degranulatingfactor from bee venom suppresses the increasedvascular permeability due to intradermal injectionof various smooth muscle spasmogens ( histamineand )5-HT

Purity 9829Clinical Data No Development ReportedSize 500 μg 1 mg 5 mg

PerphenazineCat No HY-A0077

Perphenazine is a typical antipsychotic druginhibits 5-HT receptor Alpha-1A adrenergic2A

receptor Dopamine receptor D2D3 D2L receptorand with values ofHistamine H1 receptor Ki

56 10 0765013 34 and 8 nM respectively

Purity 9990Clinical Data LaunchedSize 10 mM times 1 mL 1 g 5 g

Perphenazine D8 DihydrochlorideCat No HY-A0077AS

Perphenazine D8 Dihydrochloride is the deuteriumlabeled Perphenazine which is a typicalantipsychotic drug(5-HT Dopamine receptorligand)

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

PF-03654746Cat No HY-11045

PF-03654746 is a potent and selective histamine antagonist with high brainH3 receptor

penetration PF-03654746 reduces allergen-inducednasal symptoms might be a novel therapeuticstrategy to further explore allergic rhinitis

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

PF-03654746 TosylateCat No HY-11044

PF-03654746 Tosylate is a potent and selective antagonist with highhistamine H3 receptor

brain penetration PF-03654746 Tosylate reducesallergen-induced nasal symptoms

Purity gt98Clinical Data No Development ReportedSize 1 mg

Pheniramine MaleateCat No HY-B0971

Pheniramine Maleate ia an antihistamine andvasoconstrictor

Purity 9988Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg

Pimethixene (Pimetixene) Cat No HY-B1101

Pimethixene is antihistamine and antiserotonergiccompound acts as an antimigraine agent

Purity gt98Clinical Data LaunchedSize 10 mg

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Pimethixene maleate (Pimetixene maleate) Cat No HY-B1101A

Pimethixene maleate is antihistamine andantiserotonergic compound acts as an antimigraineagent

Purity gt98Clinical Data No Development ReportedSize 10 mg

Pirolate (CP-32387) Cat No HY-100280

Pirolate is a receptorhistamine H1

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Pitolisant (Tiprolisant) Cat No HY-12199

Pitolisant is a potent and selective nonimidazoleinverse agonist at the recombinant human

( =016 nM)histamine H3 receptor Ki

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Pitolisant hydrochloride (Ciproxidine BF 2649) Cat No HY-12199B

Pitolisant hydrochloride is a potent and selectivenonimidazole inverse agonist at the recombinanthuman ( =016 nM)histamine H3 receptor Ki

Purity 9922Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg

Pitolisant oxalate (Tiprolisant oxalate) Cat No HY-12199A

Pitolisant oxalate is a potent and selectivenonimidazole inverse agonist at the recombinanthuman ( =016 nM)histamine H3 receptor Ki

Purity gt98Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg

Promethazine hydrochlorideCat No HY-B0781

Promethazine hydrochloride is the first-generationantihistamine strong antagonist of the H1receptor and moderate mACh receptor antagonistmoderate affinity for 5-HT2A 5-HT2C D2 andα1-adrenergic receptors

Purity 9982Clinical Data LaunchedSize 1 g 5 g

Quinotolast sodium (FR71021) Cat No HY-U00027

Quinotolast sodium in the concentration range of1-100 μgmL inhibits andhistamine LTC4

release in a concentration-dependentPGD2

manner

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Ranitidine hydrochlorideCat No HY-B0281A

Ranitidine hydrochloride is a histamineH2-receptor antagonist that inhibits stomach acidproduction Target Histamine H2-ReceptorRanitidine hydrochloride is a histamineH2-receptor antagonist with IC50 of 33 plusmn 14 uMIt inhibits stomach acid production

Purity 9948Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg

ReN-1869 hydrochloride (NNC-05-1869 hydrochloride) Cat No HY-101724

ReN 1869 hydrochloride is a novel selective antagonist whichhistamine H receptor1

demonstrates affinity to the histamine H1

receptor (guinea pig brain) with K of 019plusmn004 μMi

and the non-selective σ site (guinea pig brain)with K of 045 μMi

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Rocastine (AHR-11325) Cat No HY-101745

Rocastine is a selective nonsedating H1antagonist acting as an antihistamine

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

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Roxatidine Acetate Hydrochloride (HOE 760) Cat No HY-B0305A

Roxatidine Acetate Hydrochloride is a specific andcompetitive histamin H2 receptor antagonist

Purity 9887Clinical Data LaunchedSize 10 mM times 1 mL 1 g 5 g

S 38093Cat No HY-104003

S 38093 is a brain-penetrant antagonist of H3 with of 88 144 and 12 microM forreceptor Ki

rat mouse and human H3 receptors respectively

Purity 9902Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg

SUN 1334HCat No HY-U00084

SUN 1334H is a potent orally active highlyselective antagonist with of 97H1 receptor Ki

nM

Purity gt950Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Terfenadine ((plusmn)-Terfenadine MDL-991) Cat No HY-B1193

Terfenadine ((plusmn)-Terfenadine) is a potentopen-channel blocker of with an of 204hERG IC50

nM Terfenadine an H1 histamine receptorantagonist acts as a potent apoptosis inducer inmelanoma cells through modulation of Ca2+

homeostasis

Purity 9826Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg

Toreforant (JNJ-38518168) Cat No HY-16756

Toreforant is a potent and selective histamine H4

receptor ( ) antagonist with a at the humanH4R Ki

receptor of 84 nM

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Tripelennamine hydrochlorideCat No HY-17428

Tripelennamine hydrochloride a H1-receptorantagonist is a psychoactive drug and member ofthe pyridine andethylenediamine classes that isused as an antipruritic and first-generationantihistamine

Purity 9987Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g

VUF10460Cat No HY-101420

VUF10460 is a non-imidazole histamine receptorH4agonist binds to rat H4 receptor with a ofpKi

746

Purity 9837Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

Wy 49051Cat No HY-101830

Wy 49051 is a potent orally active H1 receptorantagonist with of 44 nMIC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Zaltidine (CP-57361) Cat No HY-15541

Zaltidine(CP-57361) is a H2-receptor antagonistwhich has the antisecretory action

Purity gt990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg

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