A solution-phase combinatorial synthesis of selective dopamine D4 ligands

Combinatorial Chemistry and High Throughput Screening

Volumn 3, Issue 1, 2000, Pages 43-50

  Williams, John P ^a,b   Lavrador, Karine ^a,b  

^a Formerly CombiChem Inc   (United States)

^b NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHLORPROMAZINE; CLOZAPINE; DOPAMINE 1 RECEPTOR BLOCKING AGENT; DOPAMINE 4 RECEPTOR; EMONAPRIDE; HALOPERIDOL; N 4 CHLOROBENZYL 4 [2 [3 (2 THIENYL) 1,2,4 OXADIAZOLYL]]PIPERIDINE; PIPERIDINE DERIVATIVE; SPIPERONE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CHO CELL; CONTROLLED STUDY; DRUG COMPETITION; DRUG PURIFICATION; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION;

ANIMALIA;

EID: 0034078255     PISSN: 13862073     EISSN: None     Source Type: Journal    
DOI: 10.2174/1386207003327710     Document Type: Article

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67. 1H NMR spectra were recorded using Bruker AM (500 MHz) in the deuterated solvent as indicated. Analytical and preparative LC-MS spectra were recorded using a PE Sciex 150EX single quadrupole mass spectrometer equipped with an API (electrospray) ion source. Aliquots of the purified products were injected onto a 4.6-mm I.D. X 5-cm column and analyzed. The compounds with greater the 85% purity were screened for biological activity.
68. 2). The compounds were tested at concentrations ranging from 0.3-10000 nM. Nonspecific binding was measured in the presence of 10 μM butaclamol (Cerep) or 1 μM haloperidol (Novascreen). Incubation was run at 22°C for 60 min and stopped by rapid filtration through GF/B glass filters. Filters were washed several times with an ice-cold buffer using a cell harvester (Packard, Meriden, CT) and counted with a scintillation counter (Topcount, Packard, Meriden, CT).
69. 2-Ar), 7.19 (m, 1H), 7.51-7.59 (m, 4H), 7.47-7.77 (m, 6H).