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JNJ-5207852

Cat. No. M10717
JNJ-5207852  Structure
Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 155  USD155 In stock
50mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

JNJ-5207852 IS HISTAMINE H3 RECEPTORS ARE SELECTIVELY EFFECTIVE ANTAGONISTS, WHICH ARE H AGAINST RATS AND HUMANS3 receptors pKi the values are 8.9 and 9.24, respectively.

Chemical Information
Molecular Weight 316.48
Formula C20H32N2O
CAS Number 398473-34-2
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Hiroki Takei, et al. Front Neural Circuits. Histamine H 3 Heteroreceptors Suppress Glutamatergic and GABAergic Synaptic Transmission in the Rat Insular Cortex

[2] T Nakamura, et al. Br J Pharmacol. The expression and function of histamine H₃ receptors in pancreatic beta cells

[3] Detlef Neumann, et al. Naunyn Schmiedebergs Arch Pharmacol. The dual H3/4R antagonist thioperamide does not fully mimic the effects of the 'standard' H4R antagonist JNJ 7777120 in experimental murine asthma

[4] Rushdie M A Abuhamdah, et al. Front Syst Neurosci. Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze

[5] A J Barbier, et al. Br J Pharmacol. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist

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