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
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)
Molecular Formula | C17H21N5O |
Molecular Weight | 311.3815 |
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.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
A double-blind placebo controlled dose response study of noberastine on histamine induced weal and flare. | 1991 |
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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
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/1676366
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
Edited
Sat Dec 16 16:27:03 GMT 2023
by
admin
on
Sat Dec 16 16:27:03 GMT 2023
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Record UNII |
9HPD98OUWN
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Record Status |
Validated (UNII)
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NCI_THESAURUS |
C29578
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C069596
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C74582
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DD-33
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SUB09337MIG
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6235
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DTXSID50149317
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CHEMBL2104704
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9HPD98OUWN
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110588-56-2
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100000083563
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60531
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |