| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
H3 histamine receptor (HRH3). The compound acts as a selective agonist at this receptor, with a binding affinity Kd of 50.3 nM. It shows very low affinity for H1 and H2 receptors (pKi < 3.5), indicating high selectivity.
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| ln Vitro |
(R)-(-)-α-Methylhistamine dihydrochloride is more than ten times more efficient as an H3 agonist than histamine (HA). It is more than 1,000 times more selective for H3 receptors than HA is. (R) -(-)-α-Methylhistamine dihydrochloride has a pKi of 4.8 and less than 3.5 for H1 and H2 receptors, respectively, indicating a very low affinity. The dihydrochloride of (R)-(-)-α-methylhistamine binds to the H4 receptor more than 200 times [1][2][3].
R(-)-alpha-Methylhistamine 2HCl demonstrates potent agonistic activity at the H3 receptor in cell-free binding assays with a Kd of 50.3 nM. Its selectivity for H3 over H1 and H2 receptors is >1000-fold. The compound effectively displaces specific H3 radioligands in competitive binding experiments and activates H3 receptor-mediated signaling pathways in heterologous expression systems. |
| ln Vivo |
Restoration with (R)-(-)-α-methylhistamine dihydrochloride (RAMH; 10 mg/kg; i.p.; 60 minutes before training) reversed propofol-induced (25 mg/kg; i.p. injection; 30 min before training) (R)-(-)-α-methylhistamine dihydrochloride (6.3 mg/kg; ip) significantly reduced t-MH levels in the mouse brain, and these compounds No significant changes in HA levels
In vivo, R(-)-alpha-Methylhistamine 2HCl crosses the blood-brain barrier and produces central nervous system effects characteristic of H3 receptor activation. It has been used in antagonist assays to validate H3-mediated responses in animal models. The compound modulates neurotransmitter release in the brain, consistent with the known role of H3 receptors as presynaptic autoreceptors and heteroreceptors regulating histamine and other neurotransmitter systems. |
| Enzyme Assay |
Typical cell-free binding assays for H3 receptor agonists involve incubation of membrane preparations from cells expressing recombinant human H3 receptor with varying concentrations of the test compound and a fixed concentration of a radiolabeled H3 antagonist (e.g., [³H]-N-alpha-methylhistamine). Nonspecific binding is determined in the presence of an excess of unlabeled ligand. After incubation at room temperature for 60-90 minutes, bound and free radioactivity are separated by rapid filtration through glass fiber filters, followed by scintillation counting. Kd and Ki values are calculated from competition curves using nonlinear regression analysis.
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| Cell Assay |
In vitro cellular assays typically utilize cell lines stably expressing the human H3 receptor (e.g., CHO or HEK-293 cells). Cells are seeded in 96-well plates and incubated with various concentrations of R(-)-alpha-Methylhistamine 2HCl for 30-60 minutes. Receptor activation is measured by monitoring downstream signaling, such as inhibition of forskolin-stimulated cAMP accumulation via a homogeneous time-resolved fluorescence (HTRF) or ELISA-based cAMP assay. EC50 values are determined from dose-response curves. Antagonist assays can be performed by pre-incubating cells with antagonists prior to agonist addition.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (10-12 weeks) [3]
Doses: 10 mg/kg Route of Administration: IP; [3]. Results 60 minutes before training: Reversal of propofol-induced memory retention. In vivo animal studies typically involve administration of R(-)-alpha-Methylhistamine 2HCl to rodents via intraperitoneal or oral routes. Doses range from 1-10 mg/kg depending on the study design. Behavioral assays such as the open field test, elevated plus maze, or passive avoidance are used to assess central H3 receptor-mediated effects. Brain penetration is confirmed by measuring compound concentrations in brain tissue homogenates via LC-MS/MS. Antagonist challenge studies are performed by co-administering selective H3 antagonists to verify target engagement and specificity of observed effects. |
| ADME/Pharmacokinetics |
As a small molecule agonist, R(-)-alpha-Methylhistamine 2HCl is expected to have favorable brain penetration due to its ability to cross the blood-brain barrier. The compound is typically administered in aqueous solution and shows rapid systemic absorption. Its metabolic stability and half-life are consistent with histamine receptor ligands, with elimination primarily via hepatic metabolism. Detailed pharmacokinetic parameters such as Cmax, Tmax, and bioavailability are compound-specific and should be determined experimentally for each route of administration.
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| Toxicity/Toxicokinetics |
The compound is classified as a research chemical and is not approved for human therapeutic use. Standard safety precautions should be observed when handling. Toxicology data are limited to in vitro and in vivo pharmacological studies at research-grade doses. At concentrations used for receptor binding and functional assays (nM to low μM range), the compound does not exhibit acute cytotoxicity. Higher concentrations may produce off-target effects due to reduced selectivity. Comprehensive toxicological profiling has not been publicly reported.
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| References |
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| Additional Infomation |
R(-)-alpha-Methylhistamine 2HCl is an extensively characterized pharmacological tool for H3 receptor research. It is not a therapeutic agent and has not entered clinical trials. The compound is available from multiple chemical suppliers for research purposes only. Its high selectivity and brain penetrance make it a standard reference agonist in the histamine receptor field. The compound is typically stored desiccated at -20°C for long-term stability. It is soluble in water and DMSO for experimental use.
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| Molecular Formula |
C6H11N3.2[HCL]
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| Molecular Weight |
198.09352
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| Exact Mass |
197.049
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| CAS # |
75614-89-0
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| PubChem CID |
11957567
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| Appearance |
White to off-white ointment
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| LogP |
2.776
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
11
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| Complexity |
84.4
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](CC1=CN=CN1)N.Cl.Cl
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| InChi Key |
IZHCNQFUWDFPCW-ZJIMSODOSA-N
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| InChi Code |
InChI=1S/C6H11N3.2ClH/c1-5(7)2-6-3-8-4-9-6;;/h3-5H,2,7H2,1H3,(H,8,9);2*1H/t5-;;/m1../s1
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| Chemical Name |
(2R)-1-(1H-imidazol-5-yl)propan-2-amine;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| 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, 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)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~1262.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (10.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (10.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.0482 mL | 25.2411 mL | 50.4821 mL | |
| 5 mM | 1.0096 mL | 5.0482 mL | 10.0964 mL | |
| 10 mM | 0.5048 mL | 2.5241 mL | 5.0482 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.
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.
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