Английская Википедия:Fluperlapine

Материал из Онлайн справочника
Перейти к навигацииПерейти к поиску

Шаблон:Short description Шаблон:Cs1 config Шаблон:Drugbox

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,[1] but despite demonstrating efficacy in the treatment of a variety of medical conditions including schizophrenia,[2][3][4][5] psychosis associated with Parkinson's disease,[6] depressive symptoms, and dystonia,[7] it was never marketed.[1] This was perhaps due to its capacity for producing potentially life-threatening agranulocytosis, similarly to clozapine,[8] which it closely resembles both structurally and pharmacologically.

Pharmacology

Binding profile[9]

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

Файл:Fluperlapine synthesis.svg
Patents:[10][11]

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

See also

References

Шаблон:Reflist

Шаблон:Antipsychotics Шаблон:Navboxes Шаблон:Tricyclics