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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
4
|
| pubmed:dateCreated |
1997-2-20
|
| pubmed:abstractText |
AL-4943A (Olopatadine) is a new antihistaminic and anti-allergic drug. It was tested for its ability to compete for [3H]pyrilamine, [3H]tiotidine and [3H]N-methyl histamine binding to H1, H2 and H3 histamine receptors, respectively. AL-4943A exhibited the highest affinity (Ki = 41.1 +/- 6.0 nM) for H1-receptors and a significantly lower affinity for H2- (Ki = 43,437 +/- 6,257 nM) and H3-receptors (Ki = 171,666 +/- 6,774 nM), respectively. These data showed AL-4943A to be an H1-selective compound, being 1,059- and 4,177-times more selective for H1- than H2- and H3-receptors. AL-4943A was more H1-selective than levocabastine, ketotifen, antazoline and pheniramine and, also, exhibited a low affinity for 38 nonhistamine receptor binding sites. AL-4943A antagonized histamine-induced phosphoinositide (PI) turnover in cultured human conjunctival epithelial cells (IC50 = 9.5 +/- 1.5 nM, n = 3), human corneal fibroblasts (IC50 = 19 nM) and transformed human trabecular meshwork cells (IC50 = 39.9 nM). These data have shown AL-4943A to be a high affinity, high potency H1-selective histamine antagonist. This information, coupled with a long duration of action in an in vivo model of allergic conjunctivitis, suggests that AL-4943A may be a useful drug to treat various ocular allergic diseases, including allergic conjunctivitis.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Allergic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Dibenzoxepins,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine H1 Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphatidylinositols,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Histamine,
http://linkedlifedata.com/resource/pubmed/chemical/olopatadine
|
| pubmed:status |
MEDLINE
|
| pubmed:issn |
1080-7683
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
12
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
401-7
|
| pubmed:dateRevised |
2004-11-17
|
| pubmed:meshHeading |
pubmed-meshheading:8951676-Anti-Allergic Agents,
pubmed-meshheading:8951676-Binding, Competitive,
pubmed-meshheading:8951676-Cell Line,
pubmed-meshheading:8951676-Cells, Cultured,
pubmed-meshheading:8951676-Conjunctiva,
pubmed-meshheading:8951676-Conjunctivitis, Allergic,
pubmed-meshheading:8951676-Cornea,
pubmed-meshheading:8951676-Dibenzoxepins,
pubmed-meshheading:8951676-Epithelium,
pubmed-meshheading:8951676-Fibroblasts,
pubmed-meshheading:8951676-Histamine,
pubmed-meshheading:8951676-Histamine H1 Antagonists,
pubmed-meshheading:8951676-Humans,
pubmed-meshheading:8951676-Hydrolysis,
pubmed-meshheading:8951676-Ligands,
pubmed-meshheading:8951676-Phosphatidylinositols,
pubmed-meshheading:8951676-Receptors, Histamine,
pubmed-meshheading:8951676-Trabecular Meshwork
|
| pubmed:year |
1996
|
| pubmed:articleTitle |
Olopatadine (AL-4943A): ligand binding and functional studies on a novel, long acting H1-selective histamine antagonist and anti-allergic agent for use in allergic conjunctivitis.
|
| pubmed:affiliation |
Molecular Pharmacology Unit, Alcon Laboratories, Inc., Fort Worth, Texas, USA.
|
| pubmed:publicationType |
Journal Article
|