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Immunology and Inflammatory Disease Models Digestive System Disease Models Histamine Receptor Reactive Oxygen Species (ROS) Akt Endogenous Metabolite p38 MAPK Apoptosis
Gastrointestinal Inflammation and Ulcer Models Gastrointestinal Disease Models
Gastric Ulcer Models Duodenal Ulcer Models
Histamine

Cat. No.: HY-B1204

Histamine

(Synonyms: Ergamine)

21 Cited Publications

Avis client

Based on 21 publication(s) in Google Scholar

Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

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Pureté: 99.99%
CAS No.: 51-45-6
Formule: C₅H₉N₃
Masse moléculaire:111.15

Stockage:

-20°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Histamine Chemical Structure

CAS No.: 51-45-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Induced Disease Models
- Essai clinique
Chemical Information
Publications (21)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Human Endogenous Metabolite

Voir tous les produits spécifiques à Isoform Histamine Receptor :

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform Endogenous Metabolite :

Voir tous les produits spécifiques à Isoform p38 MAPK :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	640 nM Compound: Histamine	Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting	[PMID: 20384344]
HEK293	EC₅₀	13 nM Compound: Histamine	Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay	[PMID: 27007611]
HEK293	EC₅₀	94 nM Compound: Histamine	Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay	[PMID: 27007611]
Sf9	EC₅₀	11 nM Compound: Histamine	Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay	[PMID: 27007611]
Sf9	EC₅₀	11.6 nM Compound: 1	Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay	[PMID: 18950149]
Sf9	EC₅₀	1200 nM Compound: 1	Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	[PMID: 18950149]
Sf9	EC₅₀	1200 nM Compound: 1	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	[PMID: 18950149]
Sf9	EC₅₀	13 nM Compound: Histamine	Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay	[PMID: 27007611]
Sf9	EC₅₀	190 nM Compound: 1	Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	[PMID: 18950149]
Sf9	EC₅₀	190 nM Compound: Histamine	Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP	[PMID: 27007611]
Sf9	EC₅₀	25.1 nM Compound: 1	Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay	[PMID: 18950149]

In Vitro

Histamine (0.01-10 μM, 72 h) exhibits a bidirectional regulatory effect on the proliferation of MDA-MB-231, arrests the cell cycle at G2/M phase, induces the formation of lipid droplet, induces differentiation and apoptosis in MDA-MB-231^[4].
Histamine (10 μM, 24 h) increases the generation of ROS, especially H₂O₂, reduces the activity of antioxidant enzymes (such as catalase), thereby promoting radiosensitivity in MDA-MB-231^[4].
Histamine (1-100 μM, 12 h) inhibits the migration of microglia and the release of inflammatory mediator IL-1β in LPS (HY-D1056)-stimulated N9 mouse microglial, exhibits anti-inflammatory activity^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[4]

Cell Line:

MDA-MB-231
Concentration:

0.01-10 µM
Incubation Time:

72 h
Result:

Promoted cell proliferation at 10 µM, inhibited cell proliferation at 0.01 µM.

Apoptosis Analysis^[4]

Cell Line:

MDA-MB-231
Concentration:

10 µM
Incubation Time:

48 h
Result:

Induced apoptosis.

In Vivo

Animal Model:

Mouse model^[3]
Dosage:

0.05-100 μg/mouse
Administration:

icv, single dose
Result:

Prolonged the licking latency at the dose of 50 and 100 μg/mouse.
Shortened the licking latency at the dose of 0.1-1 μg/mouse.

Animal Model:

Ovariectomized female mice of the SW strain^[6]
Dosage:

62.5-2000 μg
Administration:

Intravaginal injection
Result:

Stimulated a vaginal response similar to that caused by estrogen, resulting in a decrease in intravaginal tetrazolium, increased epithelial growth, and keratinization.

Induced Disease Models

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Histamine (0.05-100 μg/mouse, icv, single dose) exhibits analgesic effect at high doses of histamine (50-100 μg/mouse), causes hyperalgesia at low doses (0.1-1 μg/mouse) in mouse model^[3].
Histamine dihydrochloride (62.5-2000 μg; Intravaginal injection) can exert a similar effect to estrogen in ovariectomized mice, causing a decrease in intravaginal tetrazolium, an increase in epithelial growth, and keratinization^[6].
Histamine can be used in animal modeling to create gastrointestinal ulcer models^[1].

Induction of Gastrointestinal Ulcer^[1]

Background

Histamine can cause increased gastric acid secretion, decreased mucus production, reflux of pancreatic juice, poor gastric blood flow, and thus gastric ulcers. Stress can cause increased gastrointestinal motility, making the gastric folds more susceptible to damage when exposed to acid.

Specific Modeling Methods

Guinea Pig: male • albino • Administration: 5 mg/kg • i.p. • single dose

Note

(1) No eating or drinking is allowed 24 hours before the experiment.
(2) The animals are sacrificed 2 hours after histamine injection, and treated with 1% formalin to check for gastric ulcers.

Modeling Indicators

The ulcers were punctate or elongated. After the model was dissected, the ulcer index (the sum of the lengths of the lesions) was measured under a microscope to be 3.4 mm.

Correlated Product(s): Serotonin (HY-B1473A); Reserpine (HY-N0480)

Opposite Product(s): Cimetidine (HY-14289)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 51-45-6
Appearance Solid
Masse moléculaire 111.15
Formule C₅H₉N₃
Color White to yellow
SMILES

NCCC1=CN=CN1
Synonyms

Ergamine
Structure Classification
- Others
Initial Source
- Endogenous metabolite
- Human Gut Microbiota Metabolites
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-20°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Publications (21)

All In Vivo Efficacy StudyRT-PCRIFWB

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Journal Impact Factor

Cancer Cell

Cancer cell autophagy, reprogrammed macrophages, and remodeled vasculature in glioblastoma triggers tumor immunity. [Abstract]

2022 Oct 10;40(10):1111-1127.e9. PMID: 36113478
Immunity

Spatiotemporal dynamics of CXCL10 encode contextual immune information revealed by the genetically encoded fluorescent sensor. [Abstract]

2025 Sep 9;58(9):2320-2335.e9. PMID: 40818452
Adv Sci (Weinh)

MCU Upregulation Overactivates Mitophagy by Promoting VDAC1 Dimerization and Ubiquitination in the Hepatotoxicity of Cadmium. [Abstract]

2023 Mar;10(7):e2203869. PMID: 36642847

Histamine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2203869. [Abstract]

Confocal microscopy of mitochondrial Ca²⁺ levels in HepG2 transfected with GCaMP6m. Histamine (100 μM) was applied to stimulate mitochondrial Ca²⁺ accumulation, and the 475/410 fluorescence ratio was analyzed.
Gut Microbes

Aging-caused the changes of the gut microbiota drive intestinal barrier dysfunction and increase sepsis susceptibility. [Abstract]

2026 Dec 31;18(1):2630475. PMID: 41723572
ACS Sens

A Sensitive Green-Red FRET Sensor for Calpain-1 Utilizing Heterodimeric Fluorescent Proteins from Distinct Evolutionary Origins. [Abstract]

2026 Mar 27;11(3):1891-1907. PMID: 41837894
Br J Pharmacol

A plant-derived TRPV3 inhibitor suppresses pain and itch. [Abstract]

2021 Apr;178(7):1669-1683. PMID: 33501656
J Agric Food Chem

Bifidobacterium animalis Subsp. Lactis Bla36 Postbiotics Ameliorate Allergic Rhinitis in Juvenile Mice by Repairing the Mucosal Barrier and Modulating Inflammatory Pathways. [Abstract]

2025 Nov 19;73(46):29604-29618. PMID: 41199139
Front Pharmacol

Intradermal Injection of Oxytocin Aggravates Chloroquine-Induced Itch Responses via Activating the Vasopressin-1a Receptor/Nitric Oxide Pathway in Mice. [Abstract]

2019 Nov 15;10:1380. PMID: 31824317

Histamine purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2019 Nov 15;10:1380. [Abstract]

Effects of histamine (0.1%, 20 µL/site, intradermal injection) on scratching behavior in mice.
mBio

Mycobacterium tuberculosis Utilizes Host Histamine Receptor H1 to Modulate Reactive Oxygen Species Production and Phagosome Maturation via the p38MAPK-NOX2 Axis. [Abstract]

2022 Oct 26;13(5):e0200422. PMID: 36000734
Pharm Res

Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]

2025 Aug;42(8):1315-1329. PMID: 40760405
FASEB J

MRGPRX2 Mediates Mast Cell-Induced Endometriosis Pain Through the Sensitization of Sensory Neurons via Histamine/HRH1/TRPV1 Signaling Pathway. [Abstract]

2025 Jul 15;39(13):e70778. PMID: 40600649

Histamine purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 Jul 15;39(13):e70778. [Abstract]

Changes in HRH1 gene expression in F11 cells after treatment with 10⁻⁷ mM histamine for 24 h, as measured by RT–qPCR.

Histamine purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 Jul 15;39(13):e70778. [Abstract]

Changes in HRH1 protein expression in F11 cells after treatment with 10⁻⁷ mM histamine for 24 h, as detected by western blotting.

Histamine purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 Jul 15;39(13):e70778. [Abstract]

Increase in the Ca²⁺ peak (DF/F0) in F11 cells from the control, histamine (10⁻⁷ mM for 24 h), and histamine+DLT groups (n = 3 in each group).
Toxics

Co-Exposure of Microplastics and Avermectin at Environmental-Related Concentrations Caused Severe Heart Damage Through ROS-Mediated MAPK Signaling in Larval and Adult Zebrafish. [Abstract]

2025 Dec 25;14(1):24. PMID: 41600573
J Cell Commun Signal

Critical role of mitogen-inducible gene 6 in restraining endothelial cell permeability to maintain vascular homeostasis. [Abstract]

2023 Mar;17(1):151-165. PMID: 36284029
Microbiol Spectr

Disruption of the Intestinal Mucosal Barrier Induced by High Fructose and Restraint Stress Is Regulated by the Intestinal Microbiota and Microbiota Metabolites. [Abstract]

2023 Jan 31;11(2):e0469822. PMID: 36719201
Insect Sci

UV2 and LW opsin genes mediate phototactic responses in the Asian lady beetle, Harmonia axyridis. [Abstract]

2025 Sep 11. PMID: 40931758
Fishes

2025 Aug 14.
Biochem Biophys Res Commun

TRPC1 downregulation enhances catecholamine secretion in adrenal chromaffin cells under metabolic syndrome conditions. [Abstract]

2025 Apr 1:755:151566. PMID: 40043610
Biol Pharm Bull

Inhibition of TRPC4/5 Channel Is Effective in Protecting against Histamine-Induced Hyperpermeability by Blocking Ca2+ Influx in Lung Microvascular Endothelial Cells. [Abstract]

2023;46(6):864-868. PMID: 37258152
bioRxiv

2026 Mar 30.
JID Innov

The PAR2 Antagonist Larazotide Can Mitigate Acute Histamine-Stimulated Epithelial Barrier Disruption in Keratinocytes: A Potential Adjunct Treatment for Atopic Dermatitis. [Abstract]

2025 Apr 3;5(4):100369. PMID: 40330848
bioRxiv

2024 June 12.

Solvant et solubilité

In Vitro:

H₂O : 100 mg/mL (899.69 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

8.9969 mL

44.9843 mL

89.9685 mL

5 mM

1.7994 mL

8.9969 mL

17.9937 mL

10 mM

0.8997 mL

4.4984 mL

8.9969 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (899.69 mM); Clear solution; Need ultrasonic

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
SDS (647 KB)
- English - EN (647 KB)
- Français - FR (647 KB)
- Deutsch - DE (647 KB)
- Norwegian - NO (647 KB)
- Español - ES (647 KB)
- Swedish - SV (647 KB)
- Italian - IT (647 KB)
- Korean - KR (647 KB)
- Portuguese - PT (647 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Okabe S, et al. Effects of cimetidine, a histamine H2-receptor antagonist, on various experimental gastric and duodenal ulcers. Am J Dig Dis. 1977 Aug;22(8):677-84. [Content Brief]

[2]. Rietveld S et al. The influence of respiratory sounds on breathlessness in children with asthma: a symptom-perceptionapproach. Health Psychol. 1997 Nov;16(6):547-53. [Content Brief]

[3]. Malmberg-Aiello P, et al., Role of histamine in rodent antinociception. Br J Pharmacol. 1994 Apr;111(4):1269-79. [Content Brief]

[4]. Medina V, et al., Histamine-mediated signaling processes in human malignant mammary cells. Cancer Biol Ther. 2006 Nov;5(11):1462-71. [Content Brief]

[5]. Ferreira R, et al., Histamine modulates microglia function. J Neuroinflammation. 2012 May 8;9:90. [Content Brief]

[6]. MARTIN L. The effects of histamine on the vaginal epithelium of the mouse. J Endocrinol. 1962 Jan;23:329-40. [Content Brief]

[7]. Yang LP, et al. Spotlight on histamine dihydrochloride in acute myeloid leukaemia. Drugs Aging. 2011 Apr 1;28(4):325-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	8.9969 mL	44.9843 mL	89.9685 mL	224.9213 mL
	5 mM	1.7994 mL	8.9969 mL	17.9937 mL	44.9843 mL
	10 mM	0.8997 mL	4.4984 mL	8.9969 mL	22.4921 mL
	15 mM	0.5998 mL	2.9990 mL	5.9979 mL	14.9948 mL
	20 mM	0.4498 mL	2.2492 mL	4.4984 mL	11.2461 mL
	25 mM	0.3599 mL	1.7994 mL	3.5987 mL	8.9969 mL
	30 mM	0.2999 mL	1.4995 mL	2.9990 mL	7.4974 mL
	40 mM	0.2249 mL	1.1246 mL	2.2492 mL	5.6230 mL
	50 mM	0.1799 mL	0.8997 mL	1.7994 mL	4.4984 mL
	60 mM	0.1499 mL	0.7497 mL	1.4995 mL	3.7487 mL
	80 mM	0.1125 mL	0.5623 mL	1.1246 mL	2.8115 mL
	100 mM	0.0900 mL	0.4498 mL	0.8997 mL	2.2492 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Histamine

21 Cited Publications

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