JNJ-10181457
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525296

CAS#: 544707-19-9

Description: JNJ-10181457 is a histamine H3 receptor antagonist (pKi values are 8.15 and 8.93 for rat and human H3 receptors respectively). It increases extracellular norepinephrine and acetylcholine levels in rat frontal cortex but does not stimulate dopamine release.


Price and Availability

Size
Price

10mg
USD 320
Size
Price

50mg
USD 1040
Size
Price

JNJ-10181457 purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 525296
Name: JNJ-10181457
CAS#: 544707-19-9
Chemical Formula: C20H28N2O
Exact Mass: 312.22016
Molecular Weight: 312.45
Elemental Analysis: C, 76.88; H, 9.03; N, 8.97; O, 5.12


Synonym: JNJ-10181457; JNJ10181457; JNJ 10181457.

IUPAC/Chemical Name: 4-(3-(4-(Piperidinyl)but-1-ynyl)benzyl)morpholine

InChi Key: HDRIBIYPLKZUDQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H28N2O/c1-3-10-21(11-4-1)12-5-2-7-19-8-6-9-20(17-19)18-22-13-15-23-16-14-22/h6,8-9,17H,1,3-5,10-16,18H2

SMILES Code: N1(CC2=CC=CC(C#CCCN3CCCCC3)=C2)CCOCC1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: García M, García-Pedraza JÁ, Villalón CM, Morán A. Pharmacological Evidence that Histamine H3 Receptors Mediate Histamine-Induced Inhibition of the Vagal Bradycardic Out-flow in Pithed Rats. Basic Clin Pharmacol Toxicol. 2016 Feb;118(2):113-21. doi: 10.1111/bcpt.12475. Epub 2015 Sep 14. PubMed PMID: 26301462.

2: Mohsen A, Yoshikawa T, Miura Y, Nakamura T, Naganuma F, Shibuya K, Iida T, Harada R, Okamura N, Watanabe T, Yanai K. Mechanism of the histamine H(3) receptor-mediated increase in exploratory locomotor activity and anxiety-like behaviours in mice. Neuropharmacology. 2014 Jun;81:188-94. doi: 10.1016/j.neuropharm.2014.02.003. Epub 2014 Feb 13. PubMed PMID: 24530460.

3: Vanhanen J, Nuutinen S, Lintunen M, Mäki T, Rämö J, Karlstedt K, Panula P. Histamine is required for H₃ receptor-mediated alcohol reward inhibition, but not for alcohol consumption or stimulation. Br J Pharmacol. 2013 Sep;170(1):177-87. doi: 10.1111/bph.12170. PubMed PMID: 23489295; PubMed Central PMCID: PMC3764859.

4: Nuutinen S, Vanhanen J, Pigni MC, Panula P. Effects of histamine H3 receptor ligands on the rewarding, stimulant and motor-impairing effects of ethanol in DBA/2J mice. Neuropharmacology. 2011 Jun;60(7-8):1193-9. doi: 10.1016/j.neuropharm.2010.10.027. Epub 2010 Oct 31. PubMed PMID: 21044640.

5: Galici R, Boggs JD, Aluisio L, Fraser IC, Bonaventure P, Lord B, Lovenberg TW. JNJ-10181457, a selective non-imidazole histamine H(3) receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition. Neuropharmacology. 2009 Jun;56(8):1131-7. doi: 10.1016/j.neuropharm.2009.03.011. Epub 2009 Apr 2. PubMed PMID: 19345233.

6: Bonaventure P, Letavic M, Dugovic C, Wilson S, Aluisio L, Pudiak C, Lord B, Mazur C, Kamme F, Nishino S, Carruthers N, Lovenberg T. Histamine H3 receptor antagonists: from target identification to drug leads. Biochem Pharmacol. 2007 Apr 15;73(8):1084-96. Epub 2006 Nov 3. PubMed PMID: 17129577.

7: Airaksinen AJ, Jablonowski JA, van der Mey M, Barbier AJ, Klok RP, Verbeek J, Schuit R, Herscheid JD, Leysen JE, Carruthers NI, Lammertsma AA, Windhorst AD. Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1-ynyl)-[11C]benzyl]-morpholine: evaluation of a potential PET ligand. Nucl Med Biol. 2006 Aug;33(6):801-10. PubMed PMID: 16934699.