JNJ 10181457 dihydrochloride

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Cat.No. 4019 - JNJ 10181457 dihydrochloride | C20H28N2O.2HCl | CAS No. 544707-20-2
Description: H3 antagonist
Chemical Name: 4-[3-[4-[Piperidinyl]but-1-ynyl]benzyl]morpholine dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

Histamine H3 receptor antagonist (pKi values are 8.15 and 8.93 for rat and human H3 receptors respectively). Increases extracellular norepinephrine and acetylcholine levels in rat frontal cortex but does not stimulate dopamine release. Brain penetrant.

Licensing Information

Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.

Technical Data

M. Wt 385.37
Formula C20H28N2O.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 544707-20-2
PubChem ID 10237424
InChI Key PAQHERKZFLOHCA-UHFFFAOYSA-N
Smiles C1(CN2CCOCC2)=CC=CC(C#CCCN3CCCCC3)=C1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 9.63 25
water 38.54 100

Preparing Stock Solutions

The following data is based on the product molecular weight 385.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.59 mL 12.97 mL 25.95 mL
5 mM 0.52 mL 2.59 mL 5.19 mL
10 mM 0.26 mL 1.3 mL 2.59 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Bonaventure et al (2007) Histamine H3 receptor antagonists: from target identification to drug leads. Biochem.Pharmacol. 73 1084 PMID: 17129577

Esbenshade et al (2008) The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. Br.J.Pharmacol. 154 1166 PMID: 18469850

Boggs et al (2009) JNJ-10181457, a selective non-imidazole histamine H3 receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition. Neuropharmacology 56 1131 PMID: 19345233


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1 Citation for JNJ 10181457 dihydrochloride

Citations are publications that use Tocris products. Selected citations for JNJ 10181457 dihydrochloride include:

Iida (2017) JNJ10181457, a histamine H3 receptor inverse agonist, regulates in vivo microglial functions and improves depression-like behaviours in mice. Biochem Biophys Res Commun 488 534 PMID: 28526411


Do you know of a great paper that uses JNJ 10181457 dihydrochloride from Tocris? If so please let us know.

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