Lenperone
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Lenperone (Elanone-V) is a
typical antipsychotic Typical antipsychotics (also known as major tranquilizers, and first generation antipsychotics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia). Typical antipsychotics ma ...
of the
butyrophenone Butyrophenone is an organic compound with the formula C6H5C(O)C3H7. It is a colorless liquid. The butyrophenone structure—a ketone flanked by a phenyl ring and a butyl chain—forms the basis for many other chemicals containing various sub ...
chemical class Chemical classification systems attempt to classify elements or compounds according to certain chemical functional or structural properties. Whereas the structural properties are largely intrinsic, functional properties and the derived classificati ...
. It was first reported as an
anti-emetic An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer. They may b ...
in 1974, and its use in treatment of acute
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 w ...
was reported in 1975. Related early antipsychotic agents include declenperone and milenperone. Lenperone was never approved by the FDA for use in humans in the United States, but prior to 1989 it was approved for use in veterinary medicine for sedation.


Synthesis

The alkylation between 2-(3-chloropropyl)-2-(4-fluorophenyl)-1,3-dioxolane 308-94-9(1) and 4-(4-fluorobenzoyl)piperidine 6346-57-7(2) gives 2-(p-fluorophenyl)-2--1,3-dioxolane
CID:20318874
(3). Deprotection of the ketal function completes the synthesis of lenperone (4).


See also

* Glemanserin * Pruvanserin * Roluperidone * Volinanserin Chemically related drugs containing the same 4-(''p''-fluorobenzoyl)piperidine group: *
Altanserin Altanserin is a compound that Binding (molecular), binds to the 5-HT2A receptor, 5-HT2A receptor (5-Hydroxytryptamine (serotonin) 2A receptor). Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) ...
* Ketanserin *
Setoperone Setoperone is a compound that is a ligand to the 5-HT2A receptor. It can be radiolabeled with the radioisotope fluorine-18 and used as a radioligand with positron emission tomography (PET). Several research studies have used the radiolabeled seto ...
* Lidanserin


References

Butyrophenone antipsychotics Fluoroarenes Piperidines Typical antipsychotics Veterinary drugs {{nervous-system-drug-stub