Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene

被引:123
作者
Rosati, RL [1 ]
Jardine, PD
Cameron, KO
Thompson, DD
Ke, HZ
Toler, SM
Brown, TA
Pan, LC
Ebbinghaus, CF
Reinhold, AR
Elliott, NC
Newhouse, BN
Tjoa, CM
Sweetnam, PM
Cole, MJ
Arriola, MW
Gauthier, JW
Crawford, DT
Nickerson, DF
Pirie, CM
Qi, H
Simmons, HA
Tkalcevic, GT
机构
[1] Pfizer Inc, Div Cent Res, Med Chem, Groton, CT 06340 USA
[2] Pfizer Inc, Div Cent Res, Metab Dis, Groton, CT 06340 USA
[3] Pfizer Inc, Div Cent Res, Drug Metab, Groton, CT 06340 USA
[4] Pfizer Inc, Div Cent Res, Mol Sci, Groton, CT 06340 USA
[5] Pfizer Inc, Div Cent Res, New Leads, Groton, CT 06340 USA
关键词
D O I
10.1021/jm980048b
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
引用
收藏
页码:2928 / 2931
页数:4
相关论文
共 34 条
[1]   NASAL ABSORPTION OF 17-ALPHA-ETHINYLOESTRADIOL IN THE RAT [J].
BAWARSHINASSAR, RN ;
HUSSAIN, A ;
CROOKS, PA .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1989, 41 (03) :214-215
[2]   1,2-DIARYL-3,4-DIHYDRONAPHTHALENES - PHOTOFLUOROGENIC LIGANDS FOR THE ESTROGEN-RECEPTOR [J].
BINDAL, RD ;
KATZENELLENBOGEN, JA .
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1985, 23 (6A) :929-937
[3]   RALOXIFENE (LY139481 HCL) PREVENTS BONE LOSS AND REDUCES SERUM-CHOLESTEROL WITHOUT CAUSING UTERINE HYPERTROPHY IN OVARIECTOMIZED RATS [J].
BLACK, LJ ;
SATO, M ;
ROWLEY, ER ;
MAGEE, DE ;
BEKELE, A ;
WILLIAMS, DC ;
CULLINAN, GJ ;
BENDELE, R ;
KAUFFMAN, RF ;
BENSCH, WR ;
FROLIK, CA ;
TERMINE, JD ;
BRYANT, HU .
JOURNAL OF CLINICAL INVESTIGATION, 1994, 93 (01) :63-69
[4]  
BLACK LJ, 1994, Patent No. 605193
[5]   FUNCTIONAL-HETEROGENEITY OF UDP-GLUCURONYLTRANSFERASE IN RAT-TISSUES [J].
BOCK, KW ;
CLAUSBRUCH, UCV ;
KAUFMANN, R ;
LILIENBLUM, W ;
OESCH, F ;
PFEIL, H ;
PLATT, KL .
BIOCHEMICAL PHARMACOLOGY, 1980, 29 (04) :495-500
[6]  
BOLGER JW, 1974, Patent No. 3822287
[7]   Molecular basis of agonism and antagonism in the oestrogen receptor [J].
Brzozowski, AM ;
Pike, ACW ;
Dauter, Z ;
Hubbard, RE ;
Bonn, T ;
Engstrom, O ;
Ohman, L ;
Greene, GL ;
Gustafsson, JA ;
Carlquist, M .
NATURE, 1997, 389 (6652) :753-758
[8]  
CAMERON KO, 1995, Patent No. 10513
[9]  
CASTANER J, 1978, Drugs of the Future, V3, P211
[10]   SEX-RELATED DIFFERENCES IN REGULATION OF CYTOPLASMIC ESTROGEN-RECEPTOR LEVELS IN RESPONSIVE TISSUES OF RAT [J].
CIDLOWSKI, JA ;
MULDOON, TG .
ENDOCRINOLOGY, 1976, 98 (04) :833-841