JNJ-10181457 | CAS#544707-19-9 | H3 Receptor Antagonist

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.

Chemical Structure

JNJ-10181457

CAS# 544707-19-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525296
Name: JNJ-10181457
CAS#: 544707-19-9
Chemical Formula: C20H28N2O
Exact Mass: 312.22
Molecular Weight: 312.457
Elemental Analysis: C, 76.88; H, 9.03; N, 8.97; O, 5.12

Price and Availability

Size	Price	Availability
25mg	USD 350	2 Weeks
50mg	USD 550	2 Weeks
100mg	USD 950	2 Weeks
200mg	USD 1450	2 Weeks
500mg	USD 3250	2 Weeks
1g	USD 4850	2 Weeks
2g	USD 7650	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 544707-19-9

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

More Info:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	JNJ-10181457 is a histamine H3 receptor antagonist.
In vitro activity:	TBD
In vivo activity:	Figure 7 shows that, in contrast to the rats pre-treated with saline (1 ml/kg, i.v.; left panel), i.v. pre-treatment with the selective H3 receptor antagonist, JNJ 10181457 (1 mg/kg; right panel), (i) completely blocked the inhibition of the vagally induced bradycardic responses produced by histamine (50 μg/kg) or methimepip (50 μg/kg), and (ii) had no effect per se on the vagally induced bradycardic responses induced in the animals receiving saline. Reference: Basic Clin Pharmacol Toxicol. 2016 Feb;118(2):113-21. https://pubmed.ncbi.nlm.nih.gov/26301462/

Preparing Stock Solutions

The following data is based on the product molecular weight 312.46 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

Formulation protocol:	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. PMID: 26301462. 2. 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. PMID: 23489295; PMCID: PMC3764859.
In vitro protocol:	TBD
In vivo protocol:	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. PMID: 26301462. 2. 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. PMID: 23489295; PMCID: PMC3764859.

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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.

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