Discovery and preclinical characterization of (+)-3-[4-(1-piperidinoethoxy)phenyl]spiro[indene-1,1′-indane]-5, 5′-diol hydrochloride: A promising nonsteroidal estrogen receptor agonist for hot flush

Journal of Medicinal Chemistry

Volumn 46, Issue 19, 2003, Pages 3961-3964

  Watanabe, Nobuhide ^a   Ikeno, Akihisa ^a   Minato, Hisao ^a   Nakagawa, Hiroshi ^a   Kohayakawa, Chie ^a   Tsuji, Jun Ichi ^a  

^a DAINIPPON SUMITOMO PHARMA CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

3 [4 (1 PIPERIDINOETHOXY)PHENYL]SPIRO[INDENE 1,1' INDANE] 5,5' DIOL; CHOLESTEROL; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; NALOXONE; OS 689; RALOXIFENE; RHODIUM; SELECTIVE ESTROGEN RECEPTOR MODULATOR; SPIRO[INDENE 1,1' INDANE]; TAMOXIFEN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BONE DENSITY; BONE METABOLISM; BONE MINERAL; BREAST; CELL STRAIN MCF 7; CHOLESTEROL BLOOD LEVEL; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HOT FLUSH; HUMAN; HUMAN CELL; LIPID METABOLISM; MALE; NONHUMAN; OSTEOPOROSIS; OVARIECTOMY; RADIOMETRY; RAT; RECEPTOR AFFINITY; SKIN TEMPERATURE; THERMOREGULATION; UTERUS;

ANIMALS; BONE DENSITY; BREAST NEOPLASMS; CHOLESTEROL; DRUG EVALUATION, PRECLINICAL; ESTRADIOL; FEMALE; HOT FLASHES; INDANS; MALE; MORPHINE DEPENDENCE; NALOXONE; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ESTROGEN; SELECTIVE ESTROGEN RECEPTOR MODULATORS; SKIN TEMPERATURE; SPIRO COMPOUNDS; STEREOISOMERISM; TUMOR CELLS, CULTURED; UTERUS;

EID: 0141455199     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm034134+     Document Type: Article

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43. 2: 1, 1200 nM; RAL, 5.1 nM; TAM, 8.2 nM.