azapirones

a·za·pir·ones

(ā'za-pī'rōnz),
Anxiolytics acting through agonist action at serotonin 1-A receptors.
References in periodicals archive ?
91,92) Currently, data are particularly scarce for the management of anxiety in patients with COPD, with inconclusive or contradictory findings reported for SSRIs, azapirones (including buspirone), and tricyclic antidepressants.
Buspirone (Buspar) is the only drug available in the class called azapirones.
Although anecdotally some psychiatrists may report limited clinical utility, many analyses found azapirones, including buspirone, were effective for GAD, (16), (17) particularly for patients with comorbid depressions.
Tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs), and azapirones must be given continuously, and require several weeks to reach full effectiveness.
30] Buspirone (BuSpar) and related azapirones are thought to exert anxiolytic effects by action at the 5-[HT.
PRX-00023 is targeting a significant unmet medical need for a selective 5-HT1A agonist used in the treatment of depression that avoids the sexual dysfunction, withdrawal symptoms and sleep disturbances typically associated with selective serotonin reuptake inhibitors (SSRIs) and serotonin noradrenaline reuptake inhibitors (SNRIs), lacks the addictive and sedative effects of the benzodiazepines, and does not have the slow onset, short half-life, and side effects of a chemical class of 5-HT1A agonists called azapirones.
PRX-00023 is targeting a significant unmet medical need and commercial opportunity for a selective, once-daily, 5-HT1A agonist used in the treatment of depression that avoids the sexual dysfunction, withdrawal symptoms and sleep disturbances typically associated with selective serotonin reuptake inhibitors (SSRIs) and serotonin noradrenaline reuptake inhibitors (SNRIs), lacks the addictive and sedative effects of the benzodiazepines, and does not have the slow onset, short half-life, and side effects of a chemical class of 5-HT1A agonists called azapirones.
Several studies have demonstrated that azapirones are effective in anxiety disorders.
With PRX-00023, which entered human clinical trials in February 2004, the company is targeting a significant unmet medical need and commercial opportunity for a selective, once-daily, agonist of the specific GPCR known as 5-HT1A that avoids the sexual dysfunction and sleep disorders associated with SSRIs, lacks the addictive and sedative effects of the benzodiazepines, and does not have the slow onset, short half-life, and side effects of a chemical class of 5-HT1A agonists called azapirones (most of which have failed in clinical development due to poor tolerability at effective doses).
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.
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.
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.