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JNJ-10181457 

Cat. No. M30278
JNJ-10181457  Structure
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Biological Activity

JNJ-10181457 is a selective non-imidazole histamine H3 receptor antagonist that normalizes acetylcholine neurotransmission.

Chemical Information
Molecular Weight 312.45
Formula C20H28N2O
CAS Number 544707-19-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Junichi Kitanaka, et al. Brain Res. In vivo evaluation of effects of histamine H3 receptor antagonists on methamphetamine-induced hyperlocomotion in mice

[2] Attayeb Mohsen, et al. Neuropharmacology. Mechanism of the histamine H(3) receptor-mediated increase in exploratory locomotor activity and anxiety-like behaviours in mice

[3] J Vanhanen, et al. Br J Pharmacol. Histamine is required for H₃ receptor-mediated alcohol reward inhibition, but not for alcohol consumption or stimulation

[4] Saara Nuutinen, et al. Neuropharmacology. Effects of histamine H3 receptor ligands on the rewarding, stimulant and motor-impairing effects of ethanol in DBA/2J mice

[5] Ruggero Galici, et al. Neuropharmacology. JNJ-10181457, a selective non-imidazole histamine H(3) receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition

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Keywords: JNJ-10181457  supplier, Histamine Receptor, inhibitors, activators


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