Fluperlapine
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Fluperlapine (NB 106-689), also known as fluoroperlapine, is a morphanthridine (11''H''-dibenzo ,ezepine) atypical antipsychotic with additional
antidepressant Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...
and
sedative A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but t ...
effects. It was first synthesized in 1979, and then subsequently studied in animals and humans in 1984 and beyond, but despite demonstrating efficacy in the treatment of a variety of medical conditions including
schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdra ...
,
psychosis Psychosis is a condition of the mind that results in difficulties determining what is real and what is not real. Symptoms may include delusions and hallucinations, among other features. Additional symptoms are incoherent speech and behavior ...
associated with
Parkinson's disease Parkinson's disease (PD), or simply Parkinson's, is a long-term degenerative disorder of the central nervous system that mainly affects the motor system. The symptoms usually emerge slowly, and as the disease worsens, non-motor symptoms becom ...
,
depressive symptoms Depression is a mental state of low Mood (psychology), mood and aversion to activity, which affects more than 280 million people of all ages (about 3.5% of the global population). Classified medically as a mental disorder, mental and Abnor ...
, and
dystonia Dystonia is a neurological hyperkinetic movement disorder in which sustained or repetitive muscle contractions result in twisting and repetitive movements or abnormal fixed postures. The movements may resemble a tremor. Dystonia is often inten ...
, it was never marketed. This was perhaps due to its capacity for producing potentially life-threatening
agranulocytosis Agranulocytosis, also known as agranulosis or granulopenia, is an acute condition involving a severe and dangerous lowered white blood cell count (leukopenia, most commonly of neutrophils) and thus causing a neutropenia in the circulating blood. ...
, similarly to clozapine, which it closely resembles both
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 ...
and
pharmacologically Pharmacology is a branch of medicine, biology and pharmaceutical sciences concerned with drug or medication action, where a drug may be defined as any artificial, natural, or endogenous (from within the body) molecule which exerts a biochemica ...
.


Pharmacology

Binding profile


Synthesis

3-fluoro-5,11-dihydro-6H-dibenz ,ezepin-6-one 2662-88-8(3)


See also

* Clozapine * Perlapine


References

{{Tricyclics Antipsychotics Dibenzazepines Muscarinic antagonists Piperazines Sedatives Tricyclic antidepressants Substances discovered in the 1970s