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 |
|---|---|---|
| Interactions of ligands at angiotensin II-receptors and imidazoline receptors. | 2001 Feb |
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| Inhibition of voltage-gated Ca2+ channels by antazoline. | 2002 Oct 7 |
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| Neuroprotective activity of antazoline against neuronal damage induced by limbic status epilepticus. | 2003 |
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| Conjunctival allergen challenge: models in the investigation of ocular allergy. | 2003 Jul |
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| Influence of antazoline and ketotifen on the anticonvulsant activity of conventional antiepileptics against maximal electroshock in mice. | 2004 Aug |
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| The effects of imidazoline agents on the aggregation of human platelets. | 2004 Feb |
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| Effect of histamine receptor antagonists on aminophylline-induced seizures and lethality in mice. | 2005 Jul-Aug |
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| Simple HPLC determination of benzalkonium chloride in ophthalmic formulations containing antazoline and tetrahydrozoline. | 2005 Sep-Oct |
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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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| [Histamine and the convulsive threshold or effectiveness of antiepileptic drugs]. | 2008 |
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| Demand for food and cocaine in Fischer and Lewis rats. | 2009 Feb |
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| Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands. | 2009 Oct 23 |
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| Evidence for the involvement of the noradrenergic system, dopaminergic and imidazoline receptors in the antidepressant-like effect of tramadol in mice. | 2010 May |
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| Simultaneous determination of antazoline and naphazoline by the net analyte signal standard addition method and spectrophotometric technique. | 2010 Nov-Dec |
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| Treatment of allergic conjunctivitis: results of a 1-month, single-masked randomized study. | 2010 Sep-Oct |
|
| 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
Created by
admin on Sat Dec 16 11:09:23 UTC 2023 , Edited by admin on Sat Dec 16 11:09:23 UTC 2023
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ACTIVE MOIETY
SUBSTANCE RECORD
