Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H19N3.CH4O3S |
Molecular Weight | 361.459 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(O)(=O)=O.C(N(CC1=CC=CC=C1)C2=CC=CC=C2)C3=NCCN3
InChI
InChIKey=PIEHFGHAWYGNCY-UHFFFAOYSA-N
InChI=1S/C17H19N3.CH4O3S/c1-3-7-15(8-4-1)13-20(14-17-18-11-12-19-17)16-9-5-2-6-10-16;1-5(2,3)4/h1-10H,11-14H2,(H,18,19);1H3,(H,2,3,4)
Molecular Formula | CH4O3S |
Molecular Weight | 96.106 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C17H19N3 |
Molecular Weight | 265.3529 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.drugbank.ca/drugs/DB08799Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/68000865
Sources: https://www.drugbank.ca/drugs/DB08799
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3943 Sources: https://www.drugbank.ca/drugs/DB08799 |
38.4 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | VASOCON-A Approved UseTemporary relief of ocular redness and itching. Launch Date6.414336E11 |
PubMed
Title | Date | PubMed |
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Pharmacometric analysis of alpha1-adrenoceptor function in rat tail artery pretreated with lipopolysaccharides. | 2001 Nov-Dec |
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Inhibition of voltage-gated Ca2+ channels by antazoline. | 2002 Oct 7 |
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Conjunctival allergen challenge: models in the investigation of ocular allergy. | 2003 Jul |
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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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A rapid derivative spectrophotometric method for simultaneous determination of naphazoline and antazoline in eye drops. | 2006 Jan |
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Evidence for imidazoline receptors involvement in the agmatine antidepressant-like effect in the forced swimming test. | 2007 Jun 22 |
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Demand for food and cocaine in Fischer and Lewis rats. | 2009 Feb |
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Simultaneous determination of antazoline and naphazoline by the net analyte signal standard addition method and spectrophotometric technique. | 2010 Nov-Dec |
|
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
In Vivo Use Guide
Sources: http://www.empr.com/vasocon-a/drug/1227/
1-2 drops up to 4 times daily.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7714409
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).
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:40:57 UTC 2023
by
admin
on
Fri Dec 15 16:40:57 UTC 2023
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Record UNII |
KU470J7TY6
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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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C95311
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3131-32-6
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25138-84-5
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18419
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KU470J7TY6
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DTXSID70953352
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