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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
Structure of JNJ-10181457

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

HIDE SMILES / InChI

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

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

Curator's Comment: Known to be CNS penetrant in rats. Human data not available

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
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 Aug
JNJ-10181457, a selective non-imidazole histamine H(3) receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition.
2009 Jun
Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.
2009 Oct
Patents

Patents

Sample Use Guides

in rats: A single administration of 10 mg/kg
Route of Administration: Intraperitoneal
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Sat Dec 16 08:36:14 GMT 2023
Edited
by admin
on Sat Dec 16 08:36:14 GMT 2023
Record UNII
JD270971QC
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
JNJ-10181457
Common Name English
4-(3-(4-(PIPERIDINYL)BUT-1-YNYL)BENZYL)MORPHOLINE
Systematic Name English
MORPHOLINE, 4-((3-(4-(1-PIPERIDINYL)-1-BUTYN-1-YL)PHENYL)METHYL)-
Systematic Name English
MORPHOLINE, 4-((3-(4-(1-PIPERIDINYL)-1-BUTYNYL)PHENYL)METHYL)-
Systematic Name English
Code System Code Type Description
PUBCHEM
9944610
Created by admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
PRIMARY
CAS
544707-19-9
Created by admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
PRIMARY
CAS
1188547-18-3
Created by admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
SUPERSEDED
FDA UNII
JD270971QC
Created by admin on Sat Dec 16 08:36:14 GMT 2023 , Edited by admin on Sat Dec 16 08:36:14 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY