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Nα-Methylhistamine dihydrochloride

Non-selective H3 agonist CAS# 16503-22-3

Nα-Methylhistamine dihydrochloride

2D Structure

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Nα-Methylhistamine dihydrochloride

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Chemical Properties of Nα-Methylhistamine dihydrochloride

Cas No. 16503-22-3 SDF Download SDF
PubChem ID 16078977 Appearance Powder
Formula C6H13Cl2N3 M.Wt 198.09
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water
Chemical Name 2-(1H-imidazol-5-yl)-N-methylethanamine;dihydrochloride
SMILES CNCCC1=CN=CN1.Cl.Cl
Standard InChIKey AYUQICXJAMPXPF-UHFFFAOYSA-N
Standard InChI InChI=1S/C6H11N3.2ClH/c1-7-3-2-6-4-8-5-9-6;;/h4-5,7H,2-3H2,1H3,(H,8,9);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Nα-Methylhistamine dihydrochloride

DescriptionPotent histamine agonist, particularly at H3 receptors (potency relative to histamine is 81, 185, and 270% at H1, H2 and H3 respectively). Also displays agonist properties at H4 receptors to which it binds with moderate affinity (Ki = 23 nM).

Nα-Methylhistamine dihydrochloride Dilution Calculator

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Preparing Stock Solutions of Nα-Methylhistamine dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 5.0482 mL 25.2411 mL 50.4821 mL 100.9642 mL 126.2053 mL
5 mM 1.0096 mL 5.0482 mL 10.0964 mL 20.1928 mL 25.2411 mL
10 mM 0.5048 mL 2.5241 mL 5.0482 mL 10.0964 mL 12.6205 mL
50 mM 0.101 mL 0.5048 mL 1.0096 mL 2.0193 mL 2.5241 mL
100 mM 0.0505 mL 0.2524 mL 0.5048 mL 1.0096 mL 1.2621 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Nα-Methylhistamine dihydrochloride

Characterization of a digitonin-solubilized bovine brain H3 histamine receptor coupled to a guanine nucleotide-binding protein.[Pubmed:1328529]

J Neurochem. 1992 Nov;59(5):1661-6.

The H3 receptor is a high-affinity histamine receptor that inhibits release of several neurotransmitters, including histamine. We have characterized H3 receptor binding in bovine brain and developed conditions for its solubilization. Particulate [3H]histamine binding showed an apparently single class of sites (KD = 4.6 nM; Bmax = 78 fmol/mg of protein). Of the detergents tested, digitonin at a detergent/protein ratio of 1:1 (wt/wt) yielded the greatest amount of solubilized receptors, typically 15-30% of particulate binding. Neither equilibrium binding of [3H]histamine to receptors (KD = 6.1 nM; Bmax = 92 fmol/mg of protein) nor the inhibitor profile was substantially altered by digitonin solubilization. However, solubilization did increase the rate of [3H]histamine association with and dissociation from the receptor. Size-exclusion chromatography indicated an apparent molecular weight of 220,000 for the solubilized receptor, and peak binding from this column retained its guanine nucleotide sensitivity. These last two observations are consistent with the solubilized receptor occurring in complex with a guanine nucleotide-binding protein.

Distribution, properties, and functional characteristics of three classes of histamine receptor.[Pubmed:2164693]

Pharmacol Rev. 1990 Mar;42(1):45-83.

It is clear from the preceding overview of histamine receptor pharmacology that research into the pharmacology of histamine receptors is at an exciting stage of development. The rapid advance of molecular biology should soon see the structural identification and cloning of all three of the major vertebrate histamine receptors. Further work will continue toward enhancing our understanding of the control by histamine of intracellular signaling via H1- and H2-receptors, and the rapid explosion of work on the H3-receptor should begin to unravel the mechanisms underlying its actions, perhaps via effects on ionic channels. The potential role of histamine as an intracellular second messenger raises exciting possibilities, as does the search for a histamine receptor analogous to the ligand-gated ion channel in the invertebrate nervous system.

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