Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H11Cl2N3 |
Molecular Weight | 244.12 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=C(Cl)C=C(CC2=NCCN2)C=C1Cl
InChI
InChIKey=FXNNRWAIGIEAST-UHFFFAOYSA-N
InChI=1S/C10H11Cl2N3/c11-7-3-6(4-8(12)10(7)13)5-9-14-1-2-15-9/h3-4H,1-2,5,13H2,(H,14,15)
Molecular Formula | C10H11Cl2N3 |
Molecular Weight | 244.12 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Nemazoline (A-57219) is a nasal decongestant. It has alpha 1-agonist/alpha 2-antagonist activity and was more effective and long-acting than oxymetazoline on canine nasal mucosa, in-vitro and in-vivo. Upon intranasal administration to dogs, the compound was devoid of systemic effects up to a concentration 1000 times that needed for local decongestant effect (1.65 micrograms, atomized from a 1 microgram mL-1 solution) suggesting limited mucosal absorption. After nasal administration to rats for 15 days at a concentration 1000 times greater than that required for nasal decongestion, no mucosal tissue toxicity or systemic effects were seen.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2445950
Upon intranasal administration to dogs, the compound was devoid of systemic effects up to a concentration 1000 times that needed for local decongestant effect (1.65 ugrams, atomized from a 1 ugram mL-1 solution) suggesting limited mucosal absorption.
Route of Administration:
Nasal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2445950
In radioligand binding
experiments, Nemazoline (A-57219) exhibited affinity for both the alpha 1 (Ki=553 nM), as well as the alpha 2 receptor (Ki=25 nM).
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 17:00:38 GMT 2023
by
admin
on
Fri Dec 15 17:00:38 GMT 2023
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Record UNII |
QUV3YCP28R
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C29578
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NCI_THESAURUS |
C29709
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60469
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CHEMBL2110957
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130759-56-7
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6609
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100000084131
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QUV3YCP28R
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C83997
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SUB09190MIG
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DTXSID10156729
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PRIMARY |
Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |