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Results for "

H3 antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amyloid-β (1) Apoptosis (2) Calcium Channel (1) Cholinesterase (ChE) (3) Estrogen Receptor/ERR (3) Ferroptosis (1) Histamine Receptor (79) Histone Methyltransferase (3) iGluR (1) Isotope-Labeled Compounds (1) Ligands for E3 Ligase (1) Monoamine Oxidase (1) Parasite (2) Reactive Oxygen Species (1) Serotonin Transporter (2) Sigma Receptor (4) Tau Protein (1) TRP Channel (1)
By Research Areas:	Cancer (8) Cardiovascular Disease (1) Endocrinology (23) Infection (2) Inflammation/Immunology (21) Metabolic Disease (3) Neurological Disease (61)

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-U00076

MK-0249	Histamine Receptor	Neurological Disease Endocrinology
MK-0249 (Compound 1) is a potent, selective and orally active histamine H₃ receptor antagonist, with an IC₅₀ of 1.7 nM for human H3 .

HY-160668

*Histamine H3 antagonist-1*	Histamine Receptor Serotonin Transporter	Neurological Disease
Histamine H3 antagonist-1 (Compound 10o) is a histamine H3 antagonist and a serotonin reuptake inhibitor, which can be used in depression research .

HY-107557

Proxyfan	Histamine Receptor	Neurological Disease
Proxyfan is a potent histamine H3 receptor antagonist with K_i values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan is over 1000-fold more potent at H3 receptors than other histamine receptors .

HY-107557A

Proxyfan Oxalate	Histamine Receptor	Neurological Disease
Proxyfan Oxalate is a potent histamine H3 receptor antagonist with K_i values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan Oxalate is over 1000-fold more potent at H3 receptors than other histamine receptors .

HY-116386

GSK334429	Histamine Receptor	Neurological Disease
GSK334429 is a selective and orally active non-imidazole histamine H₃ receptor antagonist with a pK_i of 9.49 against human H₃ receptor. GSK334429 can be utilized in neurological research .

HY-146383

*H3R antagonist* 2**	Histamine Receptor Cholinesterase (ChE) Monoamine Oxidase	Neurological Disease
H3R antagonist 2 (Compound 23) is a multitarget histamine H₃ receptor (H₃R) antagonist with a K_i of 170 nM for hH₃R . H3R antagonist 2 shows inhibitory effects with IC₅₀ values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB .

HY-107556

VUF 5681 dihydrobromide	Histamine Receptor	Neurological Disease
VUF 5681 dihydrobromide is a neutral antagonist of histamine H₃ receptor. VUF 5681 dihydrobromide also has partial agonist function of H₃ receptor. VUF 5681 dihydrobromide blocks the effects of Thioperamide (HY-12206). VUF 5681 dihydrobromide is used in central nervous system disease research .

HY-122171

A-317920	Histamine Receptor	Neurological Disease
A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pK_i value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .

HY-107563

ROS 234	Histamine Receptor	Inflammation/Immunology
ROS 234 is a potent H3 antagonist, with a pK_B of 9.46 for Guinea-pig ileum H₃-receptor, a pK_i of 8.90 for Rat cerebral cortex H₃-receptor, and a ED₅₀ of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access .

HY-107563A

ROS 234 dioxalate	Histamine Receptor	Inflammation/Immunology
ROS 234 dioxalate is a potent H3 antagonist, with a pK_B of 9.46 for Guinea-pig ileum H₃-receptor, a pK_i of 8.90 for Rat cerebral cortex H₃-receptor, and a ED₅₀ of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access .

HY-104003

S 38093	Histamine Receptor	Neurological Disease Endocrinology
S 38093 is a brain-penetrant, orally active antagonist of H3 receptor, with K_is of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.

HY-104003A

S 38093 hydrochloride	Histamine Receptor	Neurological Disease
S 38093 hydrochloride is a brain-penetrant, orally active antagonist of H3 receptor, with K_is of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.

HY-12191A

A 331440 hydrochloride	Histamine Receptor	Metabolic Disease
A 331440 hydrochloride is a histamine H3 receptor antagonist. A 331440 hydrochloride binds potently and selectively to human and rat histamine H3 receptors (K_i≤25 nM). A 331440 hydrochloride can be used for antiobesity research .

HY-12200

GSK189254A hydrochloride GSK189254	Histamine Receptor	Neurological Disease
GSK189254A hydrochloride is a novel, potent and selective histamine H3 receptor antagonist with pK_i values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively .

HY-117981

OUP-186	Histamine Receptor	Inflammation/Immunology
OUP-186 is a histamine H3 receptor antagonist .

HY-117500

Aplysamine-1	Histamine Receptor	Inflammation/Immunology
Aplysamine-1 acts as an antagonist for the histamine H3 receptor.

HY-12193

A-349821	Histamine Receptor	Others
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .

HY-123812

PF-03654764	Histamine Receptor	Neurological Disease Inflammation/Immunology
PF-03654764 is an orally active, selective histamine H₃ receptor antagonist with K_i values of 1.2 nM and 7.9 nM for human H₃ and rat H₃ in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research .

HY-14111

GSK189254A 1 Publications Verification GSK189254 free base	Histamine Receptor	Neurological Disease Endocrinology
GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pK_i values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

HY-17610

Enerisant TS-091	Histamine Receptor	Neurological Disease
Enerisant is a potent, highly selective, competitive and orally active histamine H₃ receptor antagonist/inverse agonist with IC₅₀s of 2.89 nM and 14.5 nM against human and rat histamine H₃ receptors, respectively .

HY-107564

Impentamine dihydrobromide VUF 4702 dihydrobromide	Others	Inflammation/Immunology
Impentamine dihydrobromide (VUF 4702 dihydrobromide) is a histamine H3 receptor antagonist with potential antihistamine activity. Impentamine dihydrobromide shows the strongest selective H3 antagonism among a series of 4(5)-(ω-aminoalkyl)-1H-imidazole compounds. The pA2 value of impentamine dihydrobromide is 8.4, showing its high efficacy in guinea pig jejunum. Impentamine dihydrobromide has a specific antagonistic binding site with the H3 receptor .

HY-107566

Conessine	Histamine Receptor Parasite	Infection
Conessine, a steroidal alkaloid, is a potent and selective histamine H₃ receptor antagonist with K_is of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H₃ receptor, respectively. Anti-malarial activity .

HY-17610A

Enerisant hydrochloride TS-091 hydrochloride	Histamine Receptor	Neurological Disease
Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H₃ receptor antagonist/inverse agonist with IC₅₀s of 2.89 nM and 14.5 nM against human and rat histamine H₃ receptors, respectively .

HY-12190

JNJ-5207852	Histamine Receptor	Neurological Disease Endocrinology
JNJ-5207852 is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is of 8.9, 9.24 for rat and human H₃R, respectively.

HY-12190A

JNJ-5207852 dihydrochloride	Histamine Receptor	Neurological Disease
JNJ-5207852 dihydrochloride is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is of 8.9, 9.24 for rat and human H₃R, respectively.

HY-155616

KSK94	Sigma Receptor Histamine Receptor	Neurological Disease
KSK94 is a high-affinity histamine H3 receptor antagonist, with K_is of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain .

HY-107566A

Conessine dihydrobromide	Histamine Receptor Parasite	Infection
Conessine dihydrobromide is a steroidal alkaloid and an effective, selective histamine H3 receptor antagonist with K_i values of 5.4, 6.0, 5.7, and 25 nM for human, dog, guinea pig, and rat H3 receptors, respectively. Conessine dihydrobromide exhibits antimalarial activity and can be used in infection-related research .

HY-125087

A-304121	Histamine Receptor	Neurological Disease
A-304121 is a selective and brain penetrating H3 receptor antagonist. A-304121 is a cognition-enhancing agent .

HY-106993

Cipralisant GT-2331	Histamine Receptor	Neurological Disease Endocrinology
Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pK_i of 9.9 for histamine H3 receptor and a K_i of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research . Cipralisant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-106993A

Cipralisant maleate GT-2331 maleate	Histamine Receptor	Neurological Disease
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pK_i of 9.9 for histamine H3 receptor and a K_i of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research . Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-107567B

Carcinine dihydrochloride β-Alanylhistamine dihydrochloride	Histamine Receptor	Neurological Disease
Carcinine (β-Alanylhistamine) dihydrochloride is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice .

HY-155615

KSK67	Sigma Receptor Histamine Receptor	Neurological Disease
KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with K_is of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain .

HY-107567

Carcinine β-Alanylhistamine	Histamine Receptor	Neurological Disease
Alistin (Carcinine; β-Alanylhistamine) is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice .

HY-B0524A

Betahistine dihydrochloride	Histamine Receptor	Neurological Disease Inflammation/Immunology Endocrinology
Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .

HY-B0524

Betahistine	Histamine Receptor	Inflammation/Immunology Cancer
Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine is used for the study of rheumatoid arthritis (RA) .

HY-D0237

Betahistine mesylate	Histamine Receptor	Inflammation/Immunology
Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine mesylate is used for the study of rheumatoid arthritis (RA) .

HY-106000

GSK239512	Histamine Receptor	Neurological Disease
GSK239512 is a potent and brain penetrated H₃ receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD) .

HY-101633

GSK-1004723	Others	Others
GSK-1004723 is a novel H1/H3 receptor antagonist with limited activity for the suppression of seasonal allergic rhinitis. GSK-1004723 is available as a suspension or solution for intranasal administration.

HY-107568

Iodophenpropit dihydrobromide	Histamine Receptor	Inflammation/Immunology
Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [ ¹²⁵I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (K_D 0.32 nM) .

HY-155614

KSK68	Sigma Receptor Histamine Receptor	Neurological Disease
KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with K_is of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain .

HY-B0524AS

Betahistine-d3 dihydrochloride	Histamine Receptor	Neurological Disease Inflammation/Immunology Endocrinology
Betahistine-d₃ (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].

HY-129250

AZD5213	Histamine Receptor	Neurological Disease
AZD5213 is a selective and competitive human H3 receptor antagonist with a pK_i value of 9.3 for hH3R. AZD5213 can be used for the research of sleep and cognitive regulation .

HY-115447

Clobenpropit	Histamine Receptor	Neurological Disease
Clobenpropit is a potent histamine H3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock .

HY-19881

ABT-288	Histamine Receptor	Neurological Disease
ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. ABT-288 has K_i values of 1.9 and 8.2 nM for human and rat H3Rs, respectively. ABT-288 can be used in cognitive impairment research. .

HY-14880B

Bavisant dihydrochloride hydrate JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate	Histamine Receptor	Neurological Disease Endocrinology
Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H₃ receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research .

HY-B1281

Mepyramine maleate 2 Publications Verification Pyrilamine maleate	Histamine Receptor	Neurological Disease Endocrinology
Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with K_ds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pK_d of 9.4 for H1 receptor.

HY-14880A

Bavisant dihydrochloride JNJ-31001074 dihydrochloride	Histamine Receptor	Neurological Disease Endocrinology
Bavisant (JNJ-31001074) dihydrochloride is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H₃ receptor. Bavisant dihydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research .

HY-14880

Bavisant JNJ-31001074	Histamine Receptor	Neurological Disease Endocrinology
Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H₃ receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research .

HY-19899

APD-916	Histamine Receptor	Neurological Disease
APD-916 is an H3 receptor antagonist. APD-916 shows good pharmacokinetic properties, and oral administration of APD-916 has been shown to enhance wakefulness in various animal models .

HY-14567

Ciproxifan FUB-359	Histamine Receptor	Neurological Disease Endocrinology
Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H₃-receptor, with an IC₅₀ of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease .

Cat. No.	Product Name	Target	Research Area

HY-100832

UNC3866 2 Publications Verification	Histone Methyltransferase	Cancer
UNC3866 is a potent antagonist of the *CBX7*-H3 interaction as determined by AlphaScreen (IC₅₀=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.

HY-100832A

UNC3866 TFA	Histone Methyltransferase	Cancer
UNC3866 TFA is a potent antagonist of the *CBX7*-H3 interaction as determined by AlphaScreen (IC₅₀=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-107566

Conessine	Infection Structural Classification other families Classification of Application Fields Source classification Plants Disease Research Fields Steroids	Histamine Receptor Parasite
Conessine, a steroidal alkaloid, is a potent and selective histamine H₃ receptor antagonist with K_is of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H₃ receptor, respectively. Anti-malarial activity .

HY-117500

Aplysamine-1	Structural Classification Alkaloids Animals Other Alkaloids Marine natural products Source classification Sponge	Histamine Receptor
Aplysamine-1 acts as an antagonist for the histamine H3 receptor.

Cat. No.	Product Name	Chemical Structure

HY-B0524AS

Betahistine-d3 dihydrochloride
Betahistine-d₃ (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].

HY-B0524AS1

Betahistine-13C,d3 dihydrochloride
Betahistine- ¹³C,d₃ (dihydrochloride) is the ¹³C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].

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H3 antagonist

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