Lesopitron (E-4424) is a
selective full agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agoni ...
of the
5-HT1A receptor which is
structurally
A structure is an arrangement and organization of interrelated elements in a material object or system, or the object or system so organized. Material structures include man-made objects such as buildings and machines and natural objects such as ...
related to the
azapirone
Azapirones are a class of drugs used as anxiolytics, antidepressants, and antipsychotics. They are commonly used as Augmentation (psychiatry), add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs).
List of ...
s.
In 2001 it was under development by
Esteve
Esteve is a Spanish international pharmaceutical company headquartered in Barcelona with more than 90 years of experience. Since its founding in 1929, Esteve has extended its pharmaceutical operations to Spain, Portugal, Germany, France, and the ...
as an
anxiolytic
An anxiolytic (; also antipanic or anti-anxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxie ...
for the treatment of
generalized anxiety disorder
Generalized anxiety disorder (GAD) is an anxiety disorder characterized by excessive, uncontrollable and often irrational worry about events or activities. Worry often interferes with daily functioning. Individuals with GAD are often overly con ...
(GAD).
It made it to
phase II clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
s but was apparently discontinued as no new information on lesopitron has surfaced since.
See also
*
Sunepitron
References
{{Serotonergics
Piperazines
Pyrazoles
Aminopyrimidines
Chloroarenes