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Details

Stereochemistry ACHIRAL
Molecular Formula C17H21N5O
Molecular Weight 311.3815
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of NOBERASTINE

SMILES

CC1=CC=C(CN2C(NC3CCNCC3)=NC4=C2N=CC=C4)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 311.3815
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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.

Originator

Approval Year

PubMed

Sample Use Guides

In Vivo Use Guide
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
Record UNII
9HPD98OUWN
Record Status Validated (UNII)
Record Version