Benzodioxans

Silibinin (INN), also known as silybin (both from Silybum, the generic name of the plant from which it is extracted), is the major active constituent of silymarin, a standardized extract of the milk thistle, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silychristin, silidianin, and others. Silibinin itself is a mixture of two diastereomers, silybin A and silybin B, in approximately equimolar ratio. Silibinin is used in pure forms as a medication, and more frequently as an active ingredient in milk thistle–derived herbal supplements.

Spiroxatrine (Spiroxamide, R5188) is a drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2C adrenergic receptor. It is an analog of spiperone and also has some dopamine antagonist effects and a relatively weak opioid action.

Piperoxan, also known as benodaine, was the first antihistamine to be discovered. This compound, derived from benzodioxan, was prepared in the early 1930s by Daniel Bovet and Ernest Fourneau at the Pasteur Institute in France. Formerly investigated by Fourneau as an α-adrenergic-blocking agent, they demonstrated that it also antagonized histamine-induced bronchospasm in guinea pigs, and published their findings in 1933. Bovet went on to win the 1957 Nobel Prize in Physiology or Medicine for his contribution. One of Bovet and Fourneau's students, Anne-Marie Staub, published the first structure–

Binospirone (MDL-73,005-EF) is a drug which acts as a partial agonist at 5-HT1A somatodendritic autoreceptors but as an antagonist at postsynaptic 5-HT1A receptors. It has anxiolytic effects.

Guanoxan is a sympatholytic drug that was marketed as Envacar by Pfizer in the UK to treat high blood pressure. It was not widely used and was eventually withdrawn from the market due to liver toxicity.

Osemozotan (MKC-242) is a selective 5-HT1A receptor agonist with some functional selectivity, acting as a full agonist at presynaptic and a partial agonist at postsynaptic 5-HT1A receptors. 5-HT1A receptor stimulation influences the release of various neurotransmitters including serotonin, dopamine, norepinephrine, and acetylcholine. 5-HT1A receptors are inhibitory G protein-coupled receptor.

The benzodioxans are a group of isomeric chemical compounds with the molecular formula C8H8O2. There are three isomers of benzodioxan, as the second atom of oxygen of the dioxane can be in a second, third or fourth position: 1,2-dioxane, 1,3-dioxane and 1,4-dioxane, which respectively give 1,2-benzodioxan, 1,3-benzodioxan and 1,4-benzodioxan.

Aplindore (DAB-452) is a drug which acts as a partial agonist selective for the dopamine receptor D2. It is being developed by the pharmaceutical company Neurogen as a treatment for Parkinson's disease and restless legs syndrome.

Imiloxan is a drug which is used in scientific research. It acts as a selective antagonist for the α2B adrenergic receptor, and has been useful for distinguishing the actions of the different α2 adrenergic subtypes.

Domoxin (INN) is a hydrazine derivative monoamine oxidase inhibitor (MAOI) antidepressant which was never marketed.

CX-546 is an ampakine drug developed by Cortex Pharmaceuticals.