9-hydroxy risperidone 9-OH-risperidone CHEMBL1621 PALIPERIDONE Invega 3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one BDBM50252513
5-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-6-methyl-1,3-dihydro-indol-2-one(Norastemizole) 3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one(risperidone) RISPERIDONE (risperidone)3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one US10174011, risperidone US10167256, Risperidone 3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one 3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one 3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one (Resperidone) BDBM50001885 RISPERDAL 2-(2-(4-(benzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-7,8,9,9a-tetrahydro-1H-pyrido[1,2-a]pyrimidin-4(6H)-one US10501452, Compound risperidone WO2023288027, Cmpd Risperidone US10259786, Risperidone 2-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-6,7,8,8a-tetrahydro-5H-naphthalen-1-one 1-(2-Allyl-phenoxy)-3-isopropylamino-propan-2-ol US8802672, Risperidone R 64 766 3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one (risperidone) CHEMBL85
- Schotte, A; Janssen, PF; Gommeren, W; Luyten, WH; Van Gompel, P; Lesage, AS; De Loore, K; Leysen, JE Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl) 124: 57-73 (1996)
- Leysen, JE; Janssen, PM; Megens, AA; Schotte, A Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry 5-12 (1994)
- ChEMBL_2023529 (CHEMBL4677342) Displacement of [3H]risperidone from alpha1 adrenergic receptor in rat cortex membrane incubated for 60 mins by competitive radioligand binding assay
- D2 Receptor Antagonism Activity Test The D2 receptor antagonism activity test (The antagonism activity of test compounds on D2 receptor expressing human recombinant D2 receptor in HEK293 cells) was performed using LANCE cAMP 384 Kit (Product of USA PerkinElmer Inc.). The D2 antagonism activity of test compounds was evaluated through their inhibition on dopamine-induced decrease of cAMP production in HEK293 cells. cAMP concentration test was performed according to the method documented in the kit instructions. The concentration of the test compounds was 0.1 nM-10000 nM, risperidone was used as a positive control, IC50 value was calculated by the Excelfit software
- Test for 5-HT2A Antagonistic Activity CHO-K1/5-HT2A cells in the logarithmic growth phase were seeded into a 384-well plate at a density of 10000 cells per well, and cultured in a 37° C., 5% CO2 incubator for 16-24 h. After that, centrifugation was performed to remove the culture medium in the cell culture plate. Dye was added, and the cells were incubated in a 37° C., 5% CO2 incubator for another 1 h. The cell culture plate was placed on the FLIPR. A compound to be tested was added, and the Ca2+ signal was detected, wherein the compound to be tested was subjected to 3-fold gradient dilution with PBS to obtain 10 concentrations, with the highest concentration of 10 uM, and double replicate wells were set up. 100 nM a-methyl-5-HT was added 15 min later, and the Ca2+ signal was detected again, wherein the value obtained by only adding 100 nM a-methyl-5-HT was taken as the maximum signal. In order to determine the test stability, risperidone was used as a positive control. The data were processed with GraphPad Prism 7.0 to obtain a cell inhibition rate curve, and the IC50 was calculated.
- 5-HT2A Receptor Antagonism Activity Test The 5-HT2A receptor antagonism activity test (The antagonism activity of test compounds on 5-HT2A receptor expressing human recombinant 5-HT2A receptor in CHO-K1 cells) was performed using FLIPR Calcium 5 Assay Kit (Product of Molecular Devices USA Inc.) according to the method documented in the kit instructions. The concentration of the test compounds was 0.1 nM-10000 nM and risperidone was used as a positive control. Test method is as follows: On the first day the seed cells are placed in T-175 flask containing 25 ml growth medium (F-12 nutrient mixture+10% FBS+1% penicillin/streptomycin+1.2% 50 mg/ml Geneticin) at a density of 14 million per bottle, cells were cultured under 37° C./5% CO2/humidified conditions for 24 hours; On the next day the seed cells were inoculated to the 384-well cell culture plate (each well containing 20,000 cells), the growth medium was replaced by 50 μL detecting medium (F-12 nutrient mixture+1.5% activated carbon-treated FBS), the cells were cultured under 37° C./5% CO2/humidified conditions for 16 hours; On the third day the medium was removed, each well of the cells plates were added with 24 μL freshly prepared loading dye solution (formulated according to the instructions), the plates were placed in an incubator and incubated under 37° C./5% CO2/humidified conditions for 120 minutes; transfer 6 μL test compound solution to the assay plate and gently shaking for one minute, incubated under 37° C./5% CO2/humidified conditions for 30 minutes; each well of the assay plate was added with 10 μL freshly prepared α-methyl-5-hydroxytryptamine solution (1.2 M, the final concentration of α-methyl-5-hydroxytryptamine is 300 nM), data were detected and analyzed by FLIPR (Product of US Molecular Devices Corporation). Inhibition rate of the compounds at different concentrations was calculated, IC50 value was calculated by the Excelfit software