Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | 2C17H19N3.H2O4S |
| Molecular Weight | 628.784 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OS(O)(=O)=O.C(N(CC1=CC=CC=C1)C2=CC=CC=C2)C3=NCCN3.C(N(CC4=CC=CC=C4)C5=CC=CC=C5)C6=NCCN6
InChI
InChIKey=UKNPBFRSHRDSCJ-UHFFFAOYSA-N
InChI=1S/2C17H19N3.H2O4S/c2*1-3-7-15(8-4-1)13-20(14-17-18-11-12-19-17)16-9-5-2-6-10-16;1-5(2,3)4/h2*1-10H,11-14H2,(H,18,19);(H2,1,2,3,4)
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/68000865
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/68000865
Antazoline is an antagonist of histamine H1 receptors. It selectively bind to but does not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Antazoline in combination with naphazoline (VASOCON-A®) is indicated to relieve the symptoms of allergic conjunctivitis.
CNS Activity
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Pharmacometric analysis of alpha1-adrenoceptor function in rat tail artery pretreated with lipopolysaccharides. | 2001 Nov-Dec |
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| The thermodynamic dissociation constants of ambroxol, antazoline, naphazoline, oxymetazoline and ranitidine by the regression analysis of spectrophotometric data. | 2004 Feb 27 |
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| Net analyte signal-based simultaneous determination of antazoline and naphazoline using wavelength region selection by experimental design-neural networks. | 2006 Feb 15 |
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| A rapid derivative spectrophotometric method for simultaneous determination of naphazoline and antazoline in eye drops. | 2006 Jan |
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| Demand for food and cocaine in Fischer and Lewis rats. | 2009 Feb |
|
| Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011 Jul 14 |
Patents
Sample Use Guides
The antihistaminic agent, antazoline, was tested for its ability to compete for [3H]pyrilamine, [3H]tiotidine and [3H]N-methyl histamine binding to rodent brain H1, H2 and H3 histamine receptors, respectively. Antazoline exhibited the highest affinity for H1-receptors (dissociation constant, Ki = 38.4 +/- 4.4 nM), and was considerably weaker at H2- (K1 = 44,433 +/- 1,763 nM) and H3-receptors (Ki = 42,400 +/- 7,527 nM).
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84803-70-3
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DTXSID701005096
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PHS9SV397D
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57354328
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ACTIVE MOIETY
SUBSTANCE RECORD
