Antazoline

{{Short description|Chemical compound}}

{{cs1 config|name-list-style=vanc}}

{{Drugbox

| Verifiedfields = changed

| Watchedfields = changed

| verifiedrevid = 443208622

| IUPAC_name = N-(4,5-Dihydro-1H-imidazol-2-ylmethyl)-N-(phenylmethyl)aniline

| image = Antazoline.svg

| width = 215

| tradename = Vasocon-a

| Drugs.com = {{drugs.com|CONS|vasocon-a}}

| routes_of_administration = Topical (nasal, eye drops)

| IUPHAR_ligand = 7116

| CAS_number_Ref = {{cascite|correct|??}}

| CAS_number = 91-75-8

| ATC_prefix = R01

| ATC_suffix = AC04

| ATC_supplemental = {{ATC|R06|AX05}}

| PubChem = 2200

| DrugBank_Ref = {{drugbankcite|correct|drugbank}}

| DrugBank = DB08799

| ChEBI_Ref = {{ebicite|changed|EBI}}

| ChEBI = 84115

| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}

| ChemSpiderID = 2115

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = DHA8014SS1

| KEGG_Ref = {{keggcite|correct|kegg}}

| KEGG = D07458

| ChEMBL_Ref = {{ebicite|correct|EBI}}

| ChEMBL = 1305

| C=17 | H=19 | N=3

| smiles = N\1=C(\NCC/1)CN(c2ccccc2)Cc3ccccc3

| StdInChI_Ref = {{stdinchicite|correct|chemspider}}

| StdInChI = 1S/C17H19N3/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)

| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}

| StdInChIKey = REYFJDPCWQRWAA-UHFFFAOYSA-N

}}

Antazoline is a 1st generation antihistamine with anticholinergic properties used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis.{{cite journal | vauthors = Abelson MB, Allansmith MR, Friedlaender MH | title = Effects of topically applied occular decongestant and antihistamine | journal = American Journal of Ophthalmology | volume = 90 | issue = 2 | pages = 254–257 | date = August 1980 | pmid = 7425039 | doi = 10.1016/s0002-9394(14)74864-0 }} To treat allergic conjunctivitis, antazoline can be combined in a solution with tetryzoline.{{cite journal | vauthors = Castillo M, Scott NW, Mustafa MZ, Mustafa MS, Azuara-Blanco A | title = Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis | journal = The Cochrane Database of Systematic Reviews | volume = 2015 | issue = 6 | pages = CD009566 | date = June 2015 | pmid = 26028608 | doi = 10.1002/14651858.CD009566.pub2 | pmc = 10616535 | hdl-access = free | hdl = 2164/6048 }} The drug is a Histamine H1 receptor antagonist:{{cite journal | vauthors = Noguchi S, Inukai T, Kuno T, Tanaka C | title = The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking | journal = Physiology & Behavior | volume = 51 | issue = 6 | pages = 1123–1127 | date = June 1992 | pmid = 1353628 | doi = 10.1016/0031-9384(92)90297-f | s2cid = 29562845 }} selectively binding to but not activating the receptor, thereby blocking the actions of endogenous histamine and subsequently leading to the temporary relief of the negative symptoms brought on by histamine.

A large study on people 65 years old or older linked the development of Alzheimer's disease and other forms of dementia to the "higher cumulative" use of first-generation antihistamines, due to their anticholinergic properties.{{cite journal | vauthors = Gray SL, Anderson ML, Dublin S, Hanlon JT, Hubbard R, Walker R, Yu O, Crane PK, Larson EB | display-authors = 6 | title = Cumulative use of strong anticholinergics and incident dementia: a prospective cohort study | journal = JAMA Internal Medicine | volume = 175 | issue = 3 | pages = 401–407 | date = March 2015 | pmid = 25621434 | pmc = 4358759 | doi = 10.1001/jamainternmed.2014.7663 | author5-link = Rebecca Hubbard }}