BUSPIRONE 8-[4-(4-Pyrimidin-2-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione : (Hydrochloride) 8-[4-(4-pyrimidin-2-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione BUSPAR CHEMBL49 US10562853, Compound Buspirone (buspirone) 8-[4-(4-Pyrimidin-2-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione 8-[4-(4-Pyrimidin-2-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione; Hydrochloride(Buspirone) BDBM50001859
buspirone analogue, 2 1-{4-[2-methyl-4-(quinolin-2-yl)piperazin-1-yl]butyl}piperidine-2,6-dione BDBM25871
2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}-2,3-dihydro-1H-isoindole-1,3-dione BDBM25874 buspirone analogue, 5
buspirone analogue, 7 4,4-dimethyl-1-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}piperidine-2,6-dione CHEMBL297702 BDBM25876
8-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione BDBM25875 CHEMBL299638 buspirone analogue, 6
2-{3-[2-methyl-4-(quinolin-2-yl)piperazin-1-yl]propyl}-2,3-dihydro-1H-isoindole-1,3-dione BDBM25872 buspirone analogue, 3
2-{4-[2-methyl-4-(quinolin-2-yl)piperazin-1-yl]butyl}-2,3-dihydro-1H-isoindole-1,3-dione BDBM25869 buspirone analogue, 1
BDBM25873 8-{4-[2-methyl-4-(quinolin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione buspirone analogue, 4
- Chilmonczyk, Z; Les, A; Wozniakowska, A; Cybulski, J; Koziol, AE; Gdaniec, M Buspirone analogues as ligands of the 5-HT1A receptor. 1. The molecular structure of buspirone and its two analogues. J Med Chem 38: 1701-10 (1995)
- Jaro&ngrave;czyk, M; Chilmonczyk, Z; Mazurek, AP; Nowak, G; Ravna, AW; Kristiansen, K; Sylte, I The molecular interactions of buspirone analogues with the serotonin transporter. Bioorg Med Chem 16: 9283-94 (2008)
- New, JS; Yevich, JP; Eison, MS; Taylor, DP; Eison, AS; Riblet, LA; VanderMaelen, CP; Temple, DL Buspirone analogues. 2. Structure-activity relationships of aromatic imide derivatives. J Med Chem 29: 1476-82 (1986)
- Yevich, JP; Temple, DL; New, JS; Taylor, DP; Riblet, LA Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives. J Med Chem 26: 194-203 (1983)
- Mokrosz, JL; Deren-Wesolek, A; Tatarczynska, E; Duszynska, B; Bojarski, AJ; Mokrosz, MJ; Chojnacka-Wójcik, E 8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as buspirone. J Med Chem 39: 1125-9 (1996)
- ChEMBL_839 Binding affinity to 5-hydroxytryptamine 1A receptor in rat hippocampus membranes,3H-8-OH-DPAT and buspirone for nonspecific binding (NSB)
- ChEMBL_3400 Compound was evaluated for binding affinity on 5-hydroxytryptamine 1A receptor in rat hippocampus membranes,3H-8-OH-DPAT and buspirone for nonspecific binding
- ChEMBL_1093 Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding.
- Extracellular Cytochrome P450 Inhibition Assay Specific aspects of the incubation conditions for each assay (e.g., protein concentration, incubation time, etc.) are defined in Walsky & Obach, 2004 (Walsky, R. L., and Obach, R. S. Validated assays for human Cytochrome P450 activities. Drug Met. Disp. 32:647-660, 2004.). In general, microsomes at protein concentrations as defined in Table 12 were mixed with buffer (100 mM KH2PO4, pH 7.4), MgCl2 (6 mM)) and substrate, and were kept on ice. Aliquots of this mixture (89 μL) were delivered to each well of a 96-well polypropylene plate which contained an aliquot of inhibitor (1 μL) in acetonitrile:water (1:1). Final solvent concentrations were less than 1% (v/v). Incubations were initiated with the addition of 10 μL β-NADPH (10 mM stock) to a final volume of 100 μL. Incubations were terminated by the addition of 1.5-2× volume of acetonitrile containing internal standard (buspirone). Samples were centrifuged at 4° C., and supernatant was transferred for LC-MS/MS analysis.