N-Methylhistamine dihydrochloride
Based on 1 Customer Validation
N-Methylhistamine dihydrochloride (Nα-Methylhistamine dihydrochloride) is a non-selective Histamine receptor agonist. N-Methylhistamine dihydrochloride activates histamine H1, H2 and H3 receptors; it stimulates central H1 receptors by activating sympathetic α and β adrenergic receptors to inhibit intestinal transit, exerts dose-dependent inhibition on intestinal transit, reduces histamine turnover in mouse brains, and increases gastric acid secretion without altering plasma gastrin concentrations. N-Methylhistamine dihydrochloride produces a pH-dependent, voltage-independent potentiating effect on acid-sensing ion channel 1a, and shows no significant activity toward homologous ASIC2a channels. N-Methylhistamine dihydrochloride can be used in studies related to Helicobacter pylori infection.
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 16503-22-3
- Formula: C6H13Cl2N3
- Molecular Weight:198.09
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
H2 Receptor |
H3 receptor |
N-Methylhistamine dihydrochloride (500 μM-1 mM) potently potentiates recombinant rat homologous ASIC1a channels expressed in CHO cells, with an EC50 of 350 μM and a maximum potentiation effect reaching 340% relative to the control group[1].
N-Methylhistamine dihydrochloride (1 μM; 30 min) effectively discriminates the non-specific binding of [3H]Nα-methylhistamine on guinea pig brain cell membranes and reverses the binding of pre-bound radioligands[3].
N-Methylhistamine dihydrochloride potently competes with [3H]Nα-methylhistamine for binding to guinea pig brain cell membranes, with a Ki value of 0.4 nM[3].
N-Methylhistamine dihydrochloride (1 μM; 30 min) enables quantitative analysis of specific [3H]Nα-methylhistamine binding. Results show that the binding level is the highest in guinea pig neural tissues, lower in the large intestine and ileum, and negligible in most peripheral tissues[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddY mice (male, 27-32 g)[2]
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Dosage:1 mg/kg; 2 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg (i.p.); 10 mg/kg (s.c.)
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Administration:i.p.; single dose; s.c.; single dose
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Result:Dose-dependently inhibited intestinal transit, with significant effects at 10 mg/kg and 20 mg/kg versus saline control (control transit ~60%).
Fully attenuated the inhibitory effect of 20 mg/kg Nα-Methylhistamine when pretreated with mepyramine (2 or 5 mg/kg s.c.) or triprolidine (5 mg/kg s.c.).
Did not significantly alter the inhibitory effect of 20 mg/kg Nα-Methylhistamine when pretreated with cimetidine (10 mg/kg s.c.), zolantidine (5 mg/kg s.c.), or thioperamide (5 mg/kg s.c.).
Prevented the inhibitory effect of 20 mg/kg Nα-Methylhistamine when pretreated with combined phentolamine (5 mg/kg s.c.) and propranolol (15 mg/kg s.c.).
Reduced the inhibitory effect of 20 mg/kg Nα-Methylhistamine to non-significant levels when pretreated with 6-hydroxydopamine (20 mg/kg i.p., 2 days prior).
Increased mouse brain histamine levels by 43% and decreased tele-methylhistamine levels by 51% 90 minutes post-treatment at 10 mg/kg s.c.
Completely blocked pargyline-induced tele-methylhistamine accumulation in the brain at 10 mg/kg s.c., indicating reduced histamine turnover.
Chemical Information
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CAS No. 16503-22-3
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Appearance Solid
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Molecular Weight 198.09
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Formula C6H13Cl2N3
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Color White to off-white
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SMILES
CNCCC1=CN=CN1.Cl.Cl
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Synonyms
Nα-Methylhistamine dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 100 mg/mL (504.82 mM; Need ultrasonic)
DMSO : 4.17 mg/mL (21.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, 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.
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 (sealed storage, 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (616 KB)
- English - EN (616 KB)
- Français - FR (616 KB)
- Deutsch - DE (616 KB)
- Norwegian - NO (616 KB)
- Español - ES (616 KB)
- Swedish - SV (616 KB)
- Italian - IT (616 KB)
- Korean - KR (616 KB)
- Portuguese - PT (616 KB)
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Handling Instructions (2659 KB)
References
[1]. Shteinikov VY, et al. Ligands of histamine receptors modulate acid-sensing ion channels. Biochemical and biophysical research communications. 2017 Sep 02;490(4):1314-1318. [Content Brief]
[2]. Oishi R, et al. N alpha-methylhistamine inhibits intestinal transit in mice by central histamine H1 receptor activation. European journal of pharmacology. 1993 Jun 24;237(2-3):155-9. [Content Brief]
[3]. Korte A, et al. Characterization and tissue distribution of H3 histamine receptors in guinea pigs by N alpha-methylhistamine. Biochemical and biophysical research communications. 1990 May 16;168(3):979-86. [Content Brief]
[4]. Murray S, et al. N alpha-methylhistamine: association with Helicobacter pylori infection in humans and effects on gastric acid secretion. Clin Chim Acta. 2000 Nov;301(1-2):181-92. [Content Brief]
Complete Stock Solution Preparation Table
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 (sealed storage, 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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 5.0482 mL | 25.2411 mL | 50.4821 mL | 126.2053 mL |
| 5 mM | 1.0096 mL | 5.0482 mL | 10.0964 mL | 25.2411 mL | |
| 10 mM | 0.5048 mL | 2.5241 mL | 5.0482 mL | 12.6205 mL | |
| 15 mM | 0.3365 mL | 1.6827 mL | 3.3655 mL | 8.4137 mL | |
| 20 mM | 0.2524 mL | 1.2621 mL | 2.5241 mL | 6.3103 mL | |
| H2O | 25 mM | 0.2019 mL | 1.0096 mL | 2.0193 mL | 5.0482 mL |
| 30 mM | 0.1683 mL | 0.8414 mL | 1.6827 mL | 4.2068 mL | |
| 40 mM | 0.1262 mL | 0.6310 mL | 1.2621 mL | 3.1551 mL | |
| 50 mM | 0.1010 mL | 0.5048 mL | 1.0096 mL | 2.5241 mL | |
| 60 mM | 0.0841 mL | 0.4207 mL | 0.8414 mL | 2.1034 mL | |
| 80 mM | 0.0631 mL | 0.3155 mL | 0.6310 mL | 1.5776 mL | |
| 100 mM | 0.0505 mL | 0.2524 mL | 0.5048 mL | 1.2621 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.
N-Methylhistamine dihydrochloride Related Classifications
HY-101005 Related Classifications
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- N-Methylhistamine
- 16503-22-3
- Nα-Methylhistamine
- Histamine Receptor
- Sodium Channel
- acid-sensing ion channel 1a
- CHO cells
- guinea pig central nervous system
- male ddY mice
- histamine H2 receptors
- ASIC2a channels
- histamine H3 receptors
- Helicobacter pylori
- histamine receptor
- histamine H1 receptors
- Inhibitor
- inhibitor
- inhibit