Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach

Journal of Medicinal Chemistry

Volumn 58, Issue 5, 2015, Pages 2275-2289

  Ratni, Hasane ^a   Rogers Evans, Mark ^a   Bissantz, Caterina ^a   Grundschober, Christophe ^a   Moreau, Jean Luc ^a   Schuler, Franz ^a   Fischer, Holger ^a   Alvarez Sanchez, Ruben ^a   Schnider, Patrick ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

RO 5028442; UNCLASSIFIED DRUG; VASOPRESSIN ANTAGONIST; (1-BENZYL-2-METHYLINDOL-3-YL)-SPIRO(1H-ISOBENZOFURAN-3,4′-PIPERIDINE)-1'-YL-METHANONE; (6-CHLORO-1-(2-(DIMETHYLAMINO)ETHYL)INDOL-3-YL)-SPIRO(1H-ISOBENZOFURAN-3,4'-PIPERIDINE)-1'-YL-METHANONE; INDOLE DERIVATIVE; MULTIDRUG RESISTANCE PROTEIN; SPIRO COMPOUND; VASOCONSTRICTOR AGENT; VASOPRESSIN DERIVATIVE; VASOPRESSIN RECEPTOR; VASOPRESSIN RECEPTOR ANTAGONIST;

ARTICLE; AUTISM; BLOOD BRAIN BARRIER; CLINICAL STUDY; COMPETITIVE BINDING ASSAY; DRUG PENETRATION; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; LIPOPHILICITY; PHYSICAL CHEMISTRY; PRINCIPAL COMPONENT ANALYSIS; PROCESS OPTIMIZATION; VOLUME OF DISTRIBUTION; ANIMAL; AUTISTIC DISORDER; BRAIN; CHEMICAL STRUCTURE; CHEMICALLY INDUCED; CHEMISTRY; GENETICS; GENOMICS; HUMAN; MALE; METABOLISM; MOUSE; PROCEDURES; PRURITUS;

ANIMALS; ANTIDIURETIC HORMONE RECEPTOR ANTAGONISTS; AUTISTIC DISORDER; BRAIN; GENOMICS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INDOLES; MALE; MICE; MOLECULAR STRUCTURE; P-GLYCOPROTEIN; PRURITUS; RECEPTORS, VASOPRESSIN; SPIRO COMPOUNDS; VASOCONSTRICTOR AGENTS; VASOPRESSINS;

EID: 84924664740     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501745f     Document Type: Article

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