Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H11Cl2N3.ClH |
Molecular Weight | 280.581 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.NC1=C(Cl)C=C(CC2=NCCN2)C=C1Cl
InChI
InChIKey=ASIGTNNPGBMHLP-UHFFFAOYSA-N
InChI=1S/C10H11Cl2N3.ClH/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);1H
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).
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NCI_THESAURUS |
C29578
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NCI_THESAURUS |
C29709
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DTXSID80911983
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EX1KDR36JS
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111073-18-8
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C83998
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CHEMBL2110957
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60468
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BB-96
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ACTIVE MOIETY
SUBSTANCE RECORD