Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABAA receptor

Journal of Medicinal Chemistry

Volumn 45, Issue 23, 2002, Pages 5043-5051

  Albaugh, Pamela A ^a   Marshall, Lu ^a   Gregory, James ^a   White, Geoff ^a   Hutchison, Alan ^a   Ross, Phil C ^a   Gallagher, Dorothy W ^a   Tallman, John F ^a   Crago, Matt ^a   Cassella, James V ^a  

^a NEUROGEN CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID RECEPTOR; 7,8,9,10 TETRAHYDROIMIDAZO[1,2 C]PYRIDO[3,4 E]PYRIMIDIN 5(6H) ONE; BENZODIAZEPINE RECEPTOR; ION CHANNEL; LIGAND; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CENTRAL NERVOUS SYSTEM; DRUG RECEPTOR BINDING; DRUG SCREENING; GABAERGIC TRANSMISSION; NERVE EXCITABILITY; NEUROTRANSMITTER RELEASE; POSTSYNAPTIC POTENTIAL; RECEPTOR AFFINITY; SYNTHESIS;

ANIMALS; BINDING, COMPETITIVE; CEREBRAL CORTEX; ELECTROPHYSIOLOGY; GABA AGONISTS; IMIDAZOLES; LIGANDS; MALE; MOTOR ACTIVITY; OOCYTES; PYRIMIDINONES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-A; STRUCTURE-ACTIVITY RELATIONSHIP; XENOPUS LAEVIS;

EID: 0037038333     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0202019     Document Type: Article

References (23)

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22. Subsequent HPLC analysis indicated the presence of starting material 24. Because 24 is inactive up to the concentrations tested here, the presence of it was deemed relatively unimportant with regard to the binding affinity of 41, since 41 is already potent.
23. HPLC analysis confirmed the purity of organic material. Thus, subsequent analogues with various fractionals in the elemental analysis were not cross-validated.