Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H28N2O |
| Molecular Weight | 312.4491 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C(CN1CCCCC1)C#CC2=CC(CN3CCOCC3)=CC=C2
InChI
InChIKey=HDRIBIYPLKZUDQ-UHFFFAOYSA-N
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
| Molecular Formula | C20H28N2O |
| Molecular Weight | 312.4491 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/19345233
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19345233
JNJ-10181457 is a histamine H3 receptor antagonist, which was developed by Johnson & Johnson. Selective blockade of histamine H3 receptors might have therapeutic utility for the treatment of working memory deficits and learning disorders, especially those in which ACh neurotransmission is compromised.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19345233
Curator's Comment: Known to be CNS penetrant in rats. Human data not available
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL264 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19345233 |
1.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines. | 2009-10 |
|
| JNJ-10181457, a selective non-imidazole histamine H(3) receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition. | 2009-06 |
|
| 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. | 2006-08 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19345233
in rats: A single administration of 10 mg/kg
Route of Administration:
Intraperitoneal
| Substance Class |
Chemical
Created
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JD270971QC
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