JNJ 10181457 dihydrochloride

Discontinued Product

JNJ 10181457 dihydrochloride (Cat. No. 4019) has been withdrawn from sale for commercial reasons.
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)
Reviews
Literature (4)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References

References are publications that support the biological activity of the product.

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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Keywords: JNJ 10181457 dihydrochloride, JNJ 10181457 dihydrochloride supplier, JNJ10181457, dihydrochloride, histamine, h3, receptors, antagonists, brain, penetrant, Histamine, H3, Receptors, 4019, Tocris Bioscience

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


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