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Details

Stereochemistry ACHIRAL
Molecular Formula C17H21N5O
Molecular Weight 311.3822
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of NOBERASTINE

SMILES

Cc1ccc(Cn2c3c(cccn3)[nH]c2=NC4CCNCC4)o1

InChI

InChIKey=VNIOQSAWKLOGLY-UHFFFAOYSA-N
InChI=1S/C17H21N5O/c1-12-4-5-14(23-12)11-22-16-15(3-2-8-19-16)21-17(22)20-13-6-9-18-10-7-13/h2-5,8,13,18H,6-7,9-11H2,1H3,(H,20,21)

HIDE SMILES / InChI

Molecular Formula C17H21N5O
Molecular Weight 311.3822
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Noberastine (NOB), a histamine H1 antagonist, has potent and specific peripheral antihistaminic activity. Noberastine, a furan derivative of nor-astemizole (an astemizole metabolite), has been shown to have a more rapid onset, and shorter duration of action than astemizole with peak antihistaminic activity at 4h following ingestion. Noberastine is rapidly absorbed and the peak plasma levels are obtained within 2 h of oral dosing. In preclinical studies Noberastine has been shown to lack central nervous system effects. After subacute (steady-state) administration of noberastine, there was increasing inhibition of weal and flare formation with higher doses of the drug. The 30 mg daily dose showed maximum antihistaminic effects.

Approval Year

PubMed

PubMed

TitleDatePubMed
A double-blind placebo controlled dose response study of noberastine on histamine induced weal and flare.
1991
The time course of action of three differing doses of noberastine, a novel H1-receptor antagonist, on histamine-induced skin wheals and the relationship to plasma drug concentrations in normal human volunteers.
1993 Feb
Effects of acrivastine, azelastine, cetirizine and noberastine on rat peritoneal mast cells.
1995 Apr

Sample Use Guides

Preliminary studies in volunteers indicate that effective antihistaminic actions occur with oral doses in the range of 10 to 40 mg as a single daily dose.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Sat Jun 26 01:30:54 UTC 2021
Edited
by admin
on Sat Jun 26 01:30:54 UTC 2021
Record UNII
9HPD98OUWN
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
NOBERASTINE
INN   MART.   USAN  
USAN   INN  
Official Name English
NOBERASTINE [INN]
Common Name English
R 64947
Code English
NOBERASTINE [MART.]
Common Name English
NOBERASTINE [USAN]
Common Name English
3H-IMIDAZO(4,5-B)PYRIDIN-2-AMINE, 3-((5-METHYL-2-FURANYL)METHYL)-N-4-PIPERIDINYL-
Systematic Name English
R-64947
Code English
3-(5-METHYLFURFURYL)-2-(4-PIPERIDYLAMINO)-3H-IMIDAZO(4,5-B)PYRIDINE
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C29578
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
Code System Code Type Description
MESH
C069596
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
NCI_THESAURUS
C74582
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
EVMPD
SUB09337MIG
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
INN
6235
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
EPA CompTox
110588-56-2
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
ChEMBL
CHEMBL2104704
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
FDA UNII
9HPD98OUWN
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
CAS
110588-56-2
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
PUBCHEM
60531
Created by admin on Sat Jun 26 01:30:54 UTC 2021 , Edited by admin on Sat Jun 26 01:30:54 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
SALT/SOLVATE -> PARENT
Related Record Type Details
ACTIVE MOIETY