Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H19N3.ClH |
Molecular Weight | 301.814 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.C(N(CC1=CC=CC=C1)C2=CC=CC=C2)C3=NCCN3
InChI
InChIKey=SWKDMSRRIBZZAY-UHFFFAOYSA-N
InChI=1S/C17H19N3.ClH/c1-3-7-15(8-4-1)13-20(14-17-18-11-12-19-17)16-9-5-2-6-10-16;/h1-10H,11-14H2,(H,18,19);1H
Molecular Formula | ClH |
Molecular Weight | 36.461 |
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 |
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Target ID: CHEMBL3943 Sources: https://www.drugbank.ca/drugs/DB08799 |
38.4 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Palliative | VASOCON-A Approved UseTemporary relief of ocular redness and itching. Launch Date1990 |
PubMed
Title | Date | PubMed |
---|---|---|
Pharmacometric analysis of alpha1-adrenoceptor function in rat tail artery pretreated with lipopolysaccharides. | 2001 Nov-Dec |
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Evaluation of the phencyclidine-like discriminative stimulus effects of novel NMDA channel blockers in rats. | 2003 Nov |
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The effects of imidazoline agents on the aggregation of human platelets. | 2004 Feb |
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Simple HPLC determination of benzalkonium chloride in ophthalmic formulations containing antazoline and tetrahydrozoline. | 2005 Sep-Oct |
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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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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 |
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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 16:08:47 GMT 2023
by
admin
on
Fri Dec 15 16:08:47 GMT 2023
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Record UNII |
FP8Q8F72JH
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Record Status |
Validated (UNII)
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Record Version |
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C29578
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CHEMBL1305
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2508-72-7
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m1942
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C76668
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219-719-8
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Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE |
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (TLC)
EP
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ACTIVE MOIETY |