Home Neuronal Signaling Histamine Receptor agonist Histamine 2HCl

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Histamine 2HCl Histamine Receptor agonist

Cat.No.S4118

Histamine(Ceplene) is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.Histamine 2HCl can be used to induce animal models of Gastric and Intestinal Ulcers.
Histamine 2HCl Histamine Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 184.07

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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

Water : 37 mg/mL

DMSO : 3 mg/mL (16.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 184.07 Formula

C5H9N3.2HCl

 Storage (From the date of receipt)
CAS No. 56-92-8 Download SDF Storage of Stock Solutions

Synonyms Ceplene Smiles C1=C(NC=N1)CCN.Cl.Cl

Mechanism of Action

Targets/IC50/Ki
Histamine H1 receptor
Histamine H2 receptor
In vitro

Histamine suppresses the generation of ROS through the Histaminetype-2 receptor (H2 receptor). Histamine inhibits the generation and release of reactive oxygen species (ROS) by monocytes/macrophages (MO) during respiratory burst. Histamine and interleukin-2 (IL-2) act synergistically to activate NK cell cytotoxicity (NKCC). Histamine combined with IL-2 might improve response rates and disease-free survival by protecting the cells of the immune system from oxidative stress and inducing natural endogenous immune cytotoxicity.

In vivo

Histamine treatment (0.5 mg/kg or 5.0 mg/kg, twice daily) protects against liver injury as evident by normal serum transaminase levels and significantly reduced liver pathology scores in a rat model with early alcohol-induced liver injury. The protective effect of histamine is blocked by Ranitidine (10 mg/kg), an H2 receptor antagonist, indicating that the histamine effect is predominantly mediated through the H2 receptor. Histamine (30 pg/rat, icv) increases both 3,4-dihydroxyphenylalanine accumulation and 3,4-dihydroxyphenylalanine acid concentrations in the nucleus accumbens in male rats, and this effect is not affect by H2 antagonist zolantidine, indicating that histamine stimulates mesolimbic DA neurons through an action at the H1 receptor. Histamine (0.5 mg/kg s.c.) reduces the liver tumour weight by 46% and subcutaneous tumour weight by 41% versus rats receiving subcutaneous saline injections. The anti-tumour effect observed by subcutaneous histamine injections is inhibited by Ranitidine (50 mg/kg s.c.) in rats sarcoma. Histamine (1000 mg/kg s.c.) displays acute tissue damage after 24 hours and indications of pathological inflammation at the injection sites at 5 days and 28 days in Sprague-Dawley rats. Histamine (1000 mg/kg s.c.) results in Cmax of 167 mM, tmax of 0.5 hour, t1/2 of 0.95 and AUC of 186 mmol-h/L in male Sprague-Dawley rats.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12174868/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12643039/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06281366 Recruiting
Pregnancy Complications
Hospital Universitari Vall d''Hebron Research Institute|DR Healthcare
 February 16 2024 --
NCT05216133 Enrolling by invitation
Airway Disease|Barrett Esophagus|Gastroesophageal Reflux Disease
NYU Langone Health|National Institute for Occupational Safety and Health (NIOSH/CDC)
 March 22 2023 --
NCT05701826 Completed
Skeletal Muscle Relaxation
Fujian Shengdi Pharmaceutical Co. Ltd.
 February 15 2023 Phase 1
NCT05676346 Completed
Lower Urinary Tract Symptoms|Histamine Intolerance
Complexo Hospitalario Universitario de A Coruña
 October 11 2022 --

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