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(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective, and brain-penetrant agonist of the H3 histamine receptor with high receptor affinity, capable of enhancing memory retention and attenuating cognitive impairment in rat models, making it a valuable pharmacological probe for elucidating central histaminergic signaling and H3 receptor-mediated modulation of learning and memory processes.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $40 | - | In Stock | |
| 5 mg | $92 | - | In Stock | |
| 10 mg | $147 | - | In Stock | |
| 25 mg | $297 | - | In Stock | |
| 50 mg | $442 | - | In Stock | |
| 100 mg | $638 | - | In Stock |
| Description | (R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective, and brain-penetrant agonist of the H3 histamine receptor with high receptor affinity, capable of enhancing memory retention and attenuating cognitive impairment in rat models, making it a valuable pharmacological probe for elucidating central histaminergic signaling and H3 receptor-mediated modulation of learning and memory processes. |
| Targets&IC50 | H3 receptor:50.3 nM (kd) |
| In vitro | (R)-(-)-α-Methylhistamine dihydrobromide is an H3-agonist with over 10 times the potency of histamine (HA). It exhibits weak affinities for H1 and H2 receptors, with pKi values of 4.8 and <3.5, respectively. The compound shows more than 1,000 times selectivity for H3-receptors compared to HA and over 200-fold selectivity over H4 receptors[1]. |
| In vivo | In mouse and rat models, intraperitoneal (i.p.) administration of (R)-(-)-α-Methylhistamine dihydrobromide (e.g., 6.3 mg/kg) decreases the steady-state levels of tele-methylhistamine (t-MH), a primary histamine metabolite, without changing total histamine levels. This indicates an inhibition of histamine turnover. In a rat model of anesthesia-induced amnesia, pretreatment with 10 mg/kg (i.p.) reverses memory retention deficits caused by Propofol [2][3][4]. |
| Molecular Weight | 287 |
| Formula | C6H13Br2N3 |
| Cas No. | 868698-49-1 |
| Smiles | C[C@@H](N)CC1=CN=CN1.Br.Br |
| Relative Density. | no data available |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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