fluparoxan
Sign in to saveAlso known as GR-50,360
Fluparoxan (developmental code name GR50360A) is a potent α2-adrenergic receptor antagonist (pKB = 7.9) with excellent selectivity for this receptor over the α1-adrenergic receptor (2,630-fold), and is the only well-studied α2-adrenergic receptor antagonist in its structural family which does not antagonize any variant of the imidazoline receptor. It was shown to possess central α2-adrenoceptor antagonist activity after oral doses in man and was patented as an antidepressant by Glaxo in the early 1980s, but its development was discontinued when the compound failed to show a clear clinical adva
Wikidata facts
- Subclass of
- chemical compound
- Mass
- 195.069557
Show 5 more facts
- chemical formula
- C₁₀H₁₀FNO₂
- isomeric SMILES
- C1[C@H]2[C@H](CN1)OC3=C(O2)C=CC=C3F
- canonical SMILES
- C1C2C(CN1)OC3=C(O2)C=CC=C3F
- Commons category
- Fluparoxan
- physically interacts with
- 5-hydroxytryptamine receptor 1A
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Encyclopedic overview
10 sectionsContents
- Pharmacology
- Pharmacodynamics
- Pharmacokinetics
- Metabolism
- Chemistry
- Synthesis
- History
- See also
- References
- External links
Fluparoxan (developmental code name GR50360A) is a potent α2-adrenergic receptor antagonist (pKB = 7.9) with excellent selectivity for this receptor over the α1-adrenergic receptor (2,630-fold), and is the only well-studied α2-adrenergic receptor antagonist in its structural family which does not antagonize any variant of the imidazoline receptor. It was shown to possess central α2-adrenoceptor antagonist activity after oral doses in man and was patented as an antidepressant by Glaxo in the early 1980s, but its development was discontinued when the compound failed to show a clear clinical advantage over existing therapies.
==Pharmacology==
Excerpted from Wikipedia’s “fluparoxan” article, available under the CC BY-SA 4.0 licence.