azapirone


Also found in: Wikipedia.

azapirone

(āz-ah-pēr-ōn),
A class of drugs with anxiolytic activity.
See also: buspirone hydrochloride.
References in periodicals archive ?
Buspirone is an anxiolytic psychoactive drug of the azapirone chemical class and is primarily used to treat generalised anxiety disorder.
In contrast, PRX-00023 is designed to have minimal affinity for the GPCRs believed to be associated with the side effects of 5-HT1A agonists that are in the azapirone chemical class, and to have a more convenient dosing profile than azapirones.
However, most of these drugs belong to a chemical class of drugs called azapirones, and their development has been hindered by poor tolerability at therapeutic doses, need for dosing up to three times daily, and by the requirement of gradual dose escalation to effective doses because of side effects such as nausea, dizziness, and restlessness which are thought to be caused by azapirones binding to non-5-HT1A GPCRs.
15,16] However, there is evidence for a range of other agents, including pregabalin, agomelatine, older antidepressants such as tricylics (TCAs), benzodiazepines, the azapirone buspirone, the antihistamine agent hydroxyzine, the first-generation antipsychotic trifluoperazine and the second-generation antipsychotic quetiapine.
In contrast, PRX-00023 is designed to be highly selective for the 5-HT1A receptor and has minimal affinity for the GPCRs believed to be associated with the side effects of 5-HT1A agonists that are in the azapirone chemical class, and to have a more convenient dosing profile than azapirones.
However, most of these drugs belong to a chemical class of drugs called azapirones and their development has been hindered by poor tolerability at therapeutic doses, rapid metabolism, and the requirement of slow dose escalation to effective doses because of nausea and lightheadedness, which are thought to be caused by their binding to off-target GPCRs.
In contrast, PRX-00023 is designed to have minimal affinity for the GPCRs associated with the side effects of 5-HT1A agonists that are in the azapirone chemical class, and to have a more convenient dosing profile than azapirones.
However, most of these drugs belong to a chemical class of drugs called azapirones and their development has been hindered by poor tolerability at therapeutic doses, rapid metabolism, resulting in a short half-life and, therefore, requiring multiple daily dosing, and the requirement of slow dose escalation to effective doses because of nausea and lightheadedness, which are thought to be caused by their binding to off-target G-Protein Coupled Receptors (GPCRs).
However, most of these drugs belong to a chemical class of drugs called azapirones, and their development has been hindered by poor tolerability at therapeutic doses, need for dosing up to three times daily, and the requirement of gradual dose escalation to effective doses because of side effects such as nausea, dizziness, and restlessness which are thought to be caused by azapirones binding to non-5-HT1A GPCRs.