Eltoprazine (developmental code name DU-28,853) is a
serotonergic
A serotonergic substance, medication, or receptor protein is one that affects neurotransmission pathways that involve serotonin, as follows:
* Serotonergic drugs
** Serotonin receptor agonists
** Serotonin receptor antagonists
** Serotonin reupta ...
drug
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug i ...
of the
phenylpiperazine
1-Phenylpiperazine (1-PP or PP) is a simple chemical compound and drug featuring a phenyl group bound to a piperazine ring. The suffix ‘-piprazole’ is sometimes used in the names of drugs to indicate they belong to this class.
It is a rigid ...
class which is described as a
serenic
A serenic, or anti-aggressive drug, is a type of drug which reduces the capacity for aggression.
Examples Serotonergic agents
The recreational drug MDMA ("ecstasy") and a variety of related drugs have been described as '' empathogen-entactogens ...
, or anti-aggressive agent.
It acts as an
agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
of the
serotonin
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...
antagonist
An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.5-HT2C receptor. The drug is closely related to
fluprazine
Fluprazine (developmental code name DU-27,716) is a drug of the phenylpiperazine class. It is a so-called serenic or antiaggressive agent. It is closely related to several other piperazines, including eltoprazine and batoprazine, and TFMPP, as we ...
and
batoprazine
Batoprazine is a drug of the phenylpiperazine class which has been described as a serenic or antiaggressive agent. It acts as a 5-HT1A and 5-HT1B receptor agonist. It is closely related to eltoprazine, fluprazine, and naphthylpiperazine, of wh ...
, which are similarly acting agents, and is also a known
chemical precursor
In chemistry, a precursor is a compound that participates in a chemical reaction that produces another compound.
In biochemistry, the term "precursor" often refers more specifically to a chemical compound preceding another in a metabolic pathway, ...
to
S-15535
S-15535 is a phenylpiperazine drug which is a potent and highly selective 5-HT1A receptor ligand that acts as an agonist and antagonist (weak partial agonist) at the presynaptic and postsynaptic 5-HT1A receptors, respectively. It has anxiolyti ...
and
lecozotan
Lecozotan is an investigational drug by Wyeth tested for improvement of cognitive functions of Alzheimer's disease patients.
, the first Phase III clinical trial has been completed.
Method of action
Lecozotan is a competitive, selective 5-H ...
.
Eltoprazine was first described in the
scientific literature
Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical ...
by 1987.Olivier, B., Mos, J., Heyden, V. D. J. A., Zethof, T., Aken, V. H., Oorschot, V. R., & Ramirez, J. M. (1987). Effects of DU 28853, a new serenic drug, in several experimental models for aggression. Research on Aggression, 93. https://scholar.google.com/scholar?cluster=5474933454486255245Schipper, J., Olivier, B., Mos, J., Tulp, M. T. M., Sijbesma, H., & Bevan, P. (1987). Eltoprazine (DU 28853): Effects on aggressive behaviour and its serotonergic properties. In International Conference on the Behavioral Pharmacology of .. https://scholar.google.com/scholar?cluster=17685819389699199278 It is or was under development for the treatment of
aggression
Aggression is behavior aimed at opposing or attacking something or someone. Though often done with the intent to cause harm, some might channel it into creative and practical outlets. It may occur either reactively or without provocation. In h ...
,
attention deficit hyperactivity disorder
Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by symptoms of inattention, hyperactivity, impulsivity, and emotional dysregulation that are excessive and pervasive, impairing in multiple con ...
(ADHD),
cognitive disorder
Neurocognitive disorders (NCDs), also known as cognitive disorders (CDs), are a category of mental health disorders that primarily affect cognitive abilities including learning, memory, perception, and problem-solving. Neurocognitive disorders in ...
s, and drug-induced
dyskinesia
Dyskinesia refers to a category of movement disorders that are characterized by involuntary muscle movements, including movements similar to tics or chorea and diminished voluntary movements. Dyskinesia can be anything from a slight tremor of t ...
, but no recent development has been reported for these indications as of February 2022. It was also under development for the treatment of
psychotic disorder
In psychopathology, psychosis is a condition in which a person is unable to distinguish, in their experience of life, between what is and is not real. Examples of psychotic symptoms are delusions, hallucinations, and disorganized or incoher ...
s, but development for this indication was discontinued. Eltoprazine is said to have shown signs of effectiveness for treatment of aggression, but was rejected for marketing authorization on the basis of the fact that aggression is a symptom rather than a disorder. The drug was originated by
Solvay Solvay may refer to:
Companies and organizations
* Solvay Brussels School of Economics and Management, Brussels, Belgium
* Solvay Institute of Sociology, Brussels, Belgium, part of the Université Libre de Bruxelles
* Solvay Process Company (1880 ...
and was developed by Elto Pharma, PsychoGenics, and Solvay.
See also
*
List of investigational aggression drugs
This is a list of investigational aggression drugs, or drugs that are currently under development for clinical use in the treatment of aggression but are not yet approved. Drugs used to treat aggression may also be known as "serenics".
''Chemica ...