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histamine receptor ligand

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By Targets:	Histamine Receptor (13) 5-HT Receptor (1) Adrenergic Receptor (1) Apoptosis (5) Calcium Channel (1) CCR (1) Cholinesterase (ChE) (2) Fluorescent Dye (1) Isotope-Labeled Compounds (1) Reference Standards (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Endocrinology (3) Inflammation/Immunology (5) Neurological Disease (7)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: Histamine Receptor Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0349

Meclizine dihydrochloride 4 Publications Verification Meclozine dihydrochloride	Histamine Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse *constitutive androstane receptor* (CAR)** and an inverse agonist for Human CAR .

HY-B0349A

Meclizine Meclozine	Histamine Receptor Apoptosis	Neurological Disease Inflammation/Immunology
Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse *constitutive androstane receptor* (CAR)** and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .

HY-101601

Bamirastine TAK-427	Histamine Receptor	Inflammation/Immunology Endocrinology
Bamirastine inhibits ligand binding to recombinant human histamine H₁ receptors (rhH₁R) with an IC₅₀ value of 17.3 nM.

HY-170789

H1R ligand-1	Histamine Receptor	Neurological Disease
H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). H1R ligand-1 can be used as a scaffold to design and synthesize a set of derivatives to explore H1R binding kinetics .

HY-B0349S

Meclizine-d8 Meclozine-d₈	Isotope-Labeled Compounds Histamine Receptor Apoptosis	Inflammation/Immunology
Meclizine-d₈ is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

HY-B0349B

Meclizine dihydrochloride monohydrate Meclozine dihydrochloride monohydrate	Histamine Receptor Apoptosis	Neurological Disease Inflammation/Immunology
Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse *constitutive androstane receptor* (CAR)** and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .

HY-146035

AChE-IN-14	Cholinesterase (ChE) Histamine Receptor	Neurological Disease
AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC₅₀s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H₃ receptor (H₃R; K_i= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease .

HY-B0349R

Meclizine dihydrochloride (Standard) Meclozine dihydrochloride (Standard)	Reference Standards Histamine Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Meclizine (dihydrochloride) (Standard) is the analytical standard of Meclizine (dihydrochloride). This product is intended for research and analytical applications. Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

HY-176060

Platelet aggregation-IN-3	Histamine Receptor Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease Cancer
Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis .

HY-121364

Bodilisant	Histamine Receptor Fluorescent Dye	Others
Bodilisant is a histamine H3 receptor (hH3R) ligand and imaging/labeling agent, with a K_i value of 6.51 nM for hH3R. Bodilisant binds to hH3R to produce strong green fluorescence, localizes to the extracellular membrane without internalization, and generates clear, displaceable fluorescent labeling of hH3R in native human brain tissues. Bodilisant serves as a pharmacological tool to visualize the distribution of hH3R via fluorescence confocal laser scanning microscopy .

HY-181597

LINS05414	Cholinesterase (ChE) Histamine Receptor	Neurological Disease
LINS05414 is a histamine H3 receptor ligand with antiCholinesterase and metal chelating activities. LINS05414 exhibits inhibitory activity against acetylcholinesterase (pIC₅₀ = 4.03) and butyrylcholinesterase (pIC₅₀ = 3.83), with a pK_i of 6.37 for human histamine H3 receptors. LINS05414 chelates copper ions, ferrous ions and ferric ions. LINS05414 regulates the release of neurotransmitters. LINS05414 can be used in the research of neurodegenerative diseases .

HY-124912

VUF-6884	Histamine Receptor	Others
VUF-6884 (Compound 7j) is a histamine receptor (Histamine *Receptor) ligand* with activity toward human H4R and H1R. Its pEC₅₀ and pK_i values against human H4R are 7.70 and 7.55, respectively, while those against human H1R are 8.17 and 8.11, respectively. VUF-6884 competitively binds to the orthosteric binding site of human H4R to displace histamine, and exhibits inverse agonist activity at human H1R .

HY-182736

YM-344484	CCR Histamine Receptor Calcium Channel	Inflammation/Immunology
YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine **histamine H1 receptor*. YM-344484 inhibits ligand-induced Ca ²⁺* influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca ²⁺ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis .

Cat. No.	Product Name	Chemical Structure

HY-B0349S

Meclizine-d8
Meclizine-d₈ is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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