Histamine

Alias: LS82-556; LS 82-556; LS-82-556
Cat No.:V30332 Purity: ≥98%
Histamine is an organic nitrogen compound and endogenous hormone involved in local immune responses, as well as regulating physiological functions in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus.
Histamine Chemical Structure CAS No.: 51-45-6
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Histamine is an organic nitrogen compound and endogenous hormone involved in local immune responses, as well as regulating physiological functions in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. Histamine has been regarded as a local hormone since its discovery in 1910 because it is not secreted by the traditional endocrine glands; nevertheless, in more recent times, it has been identified as a central neurotransmitter. Histamine is involved in the inflammatory response and has a central role as a mediator of itching. As part of an immune response to foreign pathogens, histamine is produced by basophils and by mast cells found in nearby connective tissues. In order to enable white blood cells and certain proteins to interact with pathogens within infected tissues, histamine increases the permeability of capillaries to these entities. The structure is comprised of an imidazole ring joined to an ethylamine chain, with the side-chain'saminogroup being protonated in a physiological environment.

Biological Activity I Assay Protocols (From Reference)
Targets
Human Endogenous Metabolite
ln Vitro
Human articular chondrocytes in culture proliferate more when histamine is present. Numerous cell types, including chondrocytes, fibroblasts, macrophages, endothelial cells, epithelial cells, and T cells, have been shown to exhibit altered behavior in vitro when exposed to histamine. Additionally, histamine affects the expression of many cytokines' receptors as well as how many of them are produced. Histamine receptor expression allows histamine to control various cellular functions. Histamine stimulates the production of matrix metalloproteinases (MMPs)-13 and -3 (collagenase 3 and stromelysin-1, respectively) by histidine decarboxylase (HAC) in vitro[1].
ln Vivo
Histamine is a known contributor to allergic and inflammatory responses and a key regulator of many physiological functions, such as angiogenesis, vasopermeability, and cell proliferation[1]. Histamine causes venula hyperpermeability while dilating the vasculature and boosting blood flow. Changes in the location of vascular endothelial cadherin (VE-cadherin) at the endothelial cell junction are indicative of its disruption of the endothelial barrier formation of venula[3].
Cell Assay
In 80 cm2 culture flasks, cells are grown to confluence using 10% fetal calf serum (FCS) and Dulbecco's modified Eagle's medium (DMEM). At first or second passage, cells are seeded into 96 well culture plates, at densities of approximately 2×103 cells/well. After a day, the cells are treated with either DMEM + 2% FCS on its own (control) or DMEM + 2% FCS plus histamine at a concentration of 1-100 μmol/l (each treatment requiring a minimum of eight wells). Every 48 hours, the medium—containing or not—is replaced, and after six days, the rate of cell growth is calculated.
Animal Protocol
New Zealand adult healthy albino rabbits 50, 100, 200 μg/kg s.c.
References

[1]. Ann Rheum Dis . 2003 Oct;62(10):991-4.

[2]. Asian Pacific Journal of Tropical Medicine. 2010, 3(2): 112-116.

[3]. PLoS One . 2015 Jul 9;10(7):e0132367.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C5H9N3
Molecular Weight
111.1451
Exact Mass
310.17
Elemental Analysis
C, 73.52; H, 7.14; N, 9.03; O, 10.31
CAS #
51-45-6
Appearance
Solid powder
SMILES
C1=C(NC=N1)CCN
InChi Key
NTYJJOPFIAHURM-UHFFFAOYSA-N
InChi Code
InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8)
Chemical Name
2-(1H-imidazol-5-yl)ethanamine
Synonyms
LS82-556; LS 82-556; LS-82-556
HS Tariff Code
2934.99.03.00
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~22 mg/mL (~197.9 mM)
Water: ~22 mg/mL
Ethanol: ~22 mg/mL
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00362999 Active
Recruiting
N/A Allergic Rhinitis Children's Mercy Hospital
Kansas City
August 2006 N/A
NCT05131555 Active
Recruiting
Drug: Placebo: Placebo
+ exercise training.
Drug: H1 blockade: H1
receptor antagonist
+ exercise training
Exercise
Histamine
University Ghent August 16, 2021 Not Applicable
NCT06152497 Recruiting Drug: Placebo
Behavioral: Resistance training
Histamine University Ghent September 1, 2023 Not Applicable
NCT06154824 Recruiting Other: Histamine
Other: Cowhage
Histamine
Cowhage
Aalborg University December 15, 2023 Not Applicable
NCT06081998 Recruiting Other: Histamine
Other: Cowhage
Histamine
Cowhage
Sleep Deprivation
Aalborg University November 1, 2023 Not Applicable
Biological Data
  • Effect of histamine on the proliferative rate of HAC in vitro. Ann Rheum Dis . 2003 Oct;62(10):991-4.
  • Histamine increased blood flow volume. PLoS One . 2015 Jul 9;10(7):e0132367.
  • L-NAME or phenylephrine pretreatment inhibited histamine-induced hyperpermeability and vascular relaxation. PLoS One . 2015 Jul 9;10(7):e0132367.
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