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(R)-(-)-α-Methylhistamine dihydrochloride

Cat. No. M30579
(R)-(-)-α-Methylhistamine dihydrochloride Structure
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Biological Activity

(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.

Chemical Information
Molecular Weight 198.09
Formula C6H13Cl2N3
CAS Number 75614-89-0
Form Solid
Solubility (25°C) DMSO 250 mg/mL (ultrasonic)
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hsiangkuo Yuan, et al. Headache. Histamine and Migraine

[2] Wei-Wei Li, et al. CNS Neurosci Ther. (R)-alpha-methylhistamine suppresses inhibitory neurotransmission in hippocampal CA1 pyramidal neurons counteracting propofol-induced amnesia in rats

[3] Pengyuan Sun, et al. Biol Pharm Bull. R-(-)-alpha-methylhistamine, a histamine H3 receptor agonist, induces endothelium-dependent vasodilation in rat mesenteric resistance arteries

[4] M Krause, et al. Curr Med Chem. Azomethine prodrugs of (R)-alpha-methylhistamine, a highly potent and selective histamine H3-receptor agonist

[5] R L McLeod, et al. Gen Pharmacol. Hemodynamic profile of activation of histamine H3 receptors by R-alpha-methylhistamine in the guinea pig

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