Blonanserin

Common name: Blonanserin; AD 5423; AD-5423; Lonasen
Trademarks: Lonasen
Molecular Formula: C23H30FN3
CAS Registry Number: 132810-10-7
CAS Name:2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
Molecular Weight: 367.502
SMILES: CCN1CCN(CC1)C2=NC3=C(CCCCCC3)C(=C2)C4=CC=C(C=C4)F
InChI Key: XVGOZDAJGBALKS-UHFFFAOYSA-N
InChI: InChI=1S/C23H30FN3/c1-2-26-13-15-27(16-14-26)23-17-21(18-9-11-19(24)12-10-18)20-7-5-3-4-6-8-22(20)25-23/h9-12,17H,2-8,13-16H2,1H3
Activity:  Atypical Antipsychotic; D2 preferring Dual D2/5-HT2A Antagonist; Treatment of Schizophrenia
Status: Launched 2008 (Japan); 2009 (Korea)
Originator: Dainippon Sumitomo/Almirall

Blonanserin synthesis: EP0385237A2

Blonanserin was developed as an antipsychotic drug in Japan and approved for the treatment of schizophrenia. It belongs to a series of 4-phenyl-2-(1-piperazinyl)pyridines and acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors. Blonanserin has low affinity for 5-HT2C, adrenergic a1, histamine H1, and muscarinic M1 receptors, but displays relatively high affinity for 5-HT6 receptors. In several short-term double-blind clinical trials, blonanserin had equal efficacy as haloperidol and risperidone for positive symptoms in patients with chronic schizophrenia and was also superior to haloperidol for improving negative symptoms. Blonanserin is generally well tolerated and has a low propensity to cause metabolic side effects and prolactin elevation [2].

Blonanserin was approved in Japan in year 2008 and Korea in 2009 for the treatment of schizophrenia. It is currently under clinical investigation in a Phase III trial in the People’s Republic of China.

References:
1. Hino, K.; et. al. 2-(1-piperazinyl)-4-phenylcycloalkanopyridine derivatives, processes for the production thereof, and pharmaceutical composition containing the same. EP0385237A2
2. Tenjin, T.; et. al. Profile of blonanserin for the treatment of schizophrenia. Neuropsychiatr Dis Treat 2013, 9, 587-594.