Azapirones

Buspirone, sold under the name Buspar among others, is an anxiolytic medication primarily used for the treatment of generalized anxiety disorder. Unlike benzodiazepines, buspirone does not produce significant sedation, dependence, or withdrawal symptoms.

Tandospirone, sold under the brand name Sediel, is an anxiolytic and antidepressant medication used in Japan and China, where it is marketed by Dainippon Sumitomo Pharma. It is a member of the azapirone class of drugs and is closely related to other azapirones like buspirone and gepirone.

Perospirone (Lullan) is an atypical antipsychotic of the azapirone family. It was introduced in Japan by Dainippon Sumitomo Pharma in 2001 for the treatment of schizophrenia and acute cases of bipolar mania.

Gepirone, sold under the brand name Exxua, is a medication used for the treatment of major depressive disorder. It is taken orally.

Alnespirone (S-20,499) is a selective 5-HT1A receptor full agonist of the azapirone chemical class. It produces antidepressant, anxiolytic, and antiaggressive effects.

thumb|right|250px|class=skin-invert-image|Buspirone, the prototypical azapirone anxiolytic, which contains [[azaspirodecanedione and pyrimidinylpiperazine bound via a butyl chain.]]

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.

Tiospirone (BMY-13,859), also sometimes called tiaspirone or tiosperone, is an atypical antipsychotic of the azapirone class. It was investigated as a treatment for schizophrenia in the late 1980s and was found to have an effectiveness equivalent to those of typical antipsychotics in clinical trials but without causing extrapyramidal side effects. However, development was halted and it was not marketed. Perospirone, another azapirone derivative with antipsychotic properties, was synthesized and assayed several years after tiospirone. It was found to be both more potent and more selective in co

Azaspirodecane is a chemical compound.

Azaspirodecanedione is a chemical compound with the formula C9H13NO2. It is a component of the chemical structures of several of the azapirones. ==Concrete List== Alnespirone Binospirone BMY-7,378 Buspirone Gepirone (Dimethyl variation) Mdl-72832 [113777-33-6] MDL73975 [159650-30-3] MJ-7378 [21103-03-7] Ref: ORG13514 ORG12653 SNAP-8719 [255893-38-0] Patent: Tiospirone

Revospirone (Bay Vq 7813) is an azapirone drug which was patented as a veterinary tranquilizer but was never marketed. It acts as a selective 5-HT1A receptor partial agonist. Similarly to other azapirones such as buspirone, revospirone produces 1-(2-pyrimidinyl)piperazine (1-PP) as an active metabolite. As a result, it also acts as an α2-adrenergic receptor antagonist to an extent.

Umespirone (KC-9172) is a drug of the azapirone class which possesses anxiolytic and antipsychotic properties. It behaves as a 5-HT1A receptor partial agonist (Ki = 15 nM), D2 receptor partial agonist (Ki = 23 nM), and α1-adrenoceptor receptor antagonist (Ki = 14 nM), and also has weak affinity for the sigma receptor (Ki = 558 nM). Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation, cognitive/memory impairment, catalepsy, and extrapyramidal symptoms.

Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone family. Its affinity for the 5-HT1A receptor was reported to be 4.8 nM (Ki) (or 8.33 (pKi)), and its intrinsic activity approximately equal to that of serotonin (i.e., 100%).