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Details

Stereochemistry ACHIRAL
Molecular Formula C17H21N5O.C6H8O7
Molecular Weight 503.506
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of NOBERASTINE CITRATE

SMILES

Cc1ccc(Cn2c3c(cccn3)[nH]c2=NC4CCNCC4)o1.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

InChI

InChIKey=VXIJMTRTCJNTMW-UHFFFAOYSA-N
InChI=1S/C17H21N5O.C6H8O7/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;7-3(8)1-6(13,5(11)12)2-4(9)10/h2-5,8,13,18H,6-7,9-11H2,1H3,(H,20,21);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)

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

Molecular Formula C6H8O7
Molecular Weight 192.1238
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 01:14:22 UTC 2021
Edited
by admin
on Sat Jun 26 01:14:22 UTC 2021
Record UNII
2T9WRO4KJM
Record Status Validated (UNII)
Record Version
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Name Type Language
NOBERASTINE CITRATE
Common Name English
R-83546
Code English
Code System Code Type Description
PUBCHEM
21695212
Created by admin on Sat Jun 26 01:14:22 UTC 2021 , Edited by admin on Sat Jun 26 01:14:22 UTC 2021
PRIMARY
FDA UNII
2T9WRO4KJM
Created by admin on Sat Jun 26 01:14:22 UTC 2021 , Edited by admin on Sat Jun 26 01:14:22 UTC 2021
PRIMARY
CAS
139751-07-8
Created by admin on Sat Jun 26 01:14:22 UTC 2021 , Edited by admin on Sat Jun 26 01:14:22 UTC 2021
PRIMARY
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