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.
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
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).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 312.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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.
