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Fluperlapine

Chemical compound

Summary

Chemical compound

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Fluperlapine (NB 106-689), also known as fluoroperlapine, is a morphanthridine (11H-dibenzo[b,e]azepine) atypical antipsychotic with additional antidepressant and sedative 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, psychosis associated with Parkinson's disease, depressive symptoms, and dystonia, it was never marketed. This was perhaps due to its capacity for producing potentially life-threatening agranulocytosis, similarly to clozapine, which it closely resembles both structurally and pharmacologically.

Pharmacology

Binding profile

Receptor	Ki (nM)
5-HT2A	7.9
5-HT2C	18.2
5-HT6	29
5-HT7	4.6
M1	8.8
M2	71
M3	41
M4	14
M5	17
D1	85
D2	316.2
D3	254.7
D4	21

Synthesis

4406900}} (1983 to Fidelity Union Bank).</ref>

3-fluoro-5,11-dihydro-6H-dibenz[b,e]azepin-6-one [62662-88-8] (3)

References

(1985). "Treatment of drug-induced exogenous psychosis in parkinsonism with clozapine and fluperlapine". European Archives of Psychiatry and Neurological Sciences.
(March 2000). "Bioactivation and covalent binding of hydroxyfluperlapine in human neutrophils: implications for fluperlapine-induced agranulocytosis". Drug Metabolism and Disposition.
(12 January 2011). "PDSP K_i Database". University of North Carolina at Chapel Hill and the United States National Institute of Mental Health.
Fritz Hunziker, Rudolf Fischer, {{US patent. 4308207 (1981 to Sandoz Ltd.).
Fritz Hunziker & Rudolf Fischer, {{US patent. 4406900 (1983 to Fidelity Union Bank).

Wikipedia Source

This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

4-methylpiperazin-1-yl-compounds antipsychotics dibenzazepines m1-receptor-antagonists m2-receptor-antagonists m3-receptor-antagonists m4-receptor-antagonists m5-receptor-antagonists sedatives substances-discovered-in-the-1970s tricyclic-antidepressants

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