메뉴 건너뛰기




Volumn 111, Issue 2, 1998, Pages 273-278

Activity of 17β-(N-alkyl/arylformamido) and 17β-[(N-alkyl/aryl) alkyl/arylamido]-4-methyl-4-aza-50α-androstan-3-ones as 50α-reductase inhibitors in the hamster flank organ and ear

Author keywords

Acne; Androgens; Costovertebral organ; Sebaceous glands

Indexed keywords

17BETA (N AMYLFORMAMIDO) 4 METHYL 4 AZA 5ALPHA ANDROSTAN 3 ONE; 17BETA (N HEPTYLFORMAMIDO) 4 METHYL 4 AZA 5ALPHA ANDROSTAN 3 ONE; 17BETA (N HEXYLFORMAMIDO) 4 METHYL 4 AZA 5ALPHA ANDROSTAN 3 ONE; ANDROSTANOLONE; ANDROSTANOLONE DERIVATIVE; EM 401; EM 402; EM 540; STEROID 5ALPHA REDUCTASE; STEROID 5ALPHA REDUCTASE INHIBITOR; TESTOSTERONE; UNCLASSIFIED DRUG; ANTIANDROGEN; CHOLESTENONE 5ALPHA REDUCTASE; ENZYME INHIBITOR; OXIDOREDUCTASE;

EID: 0031596333     PISSN: 0022202X     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1523-1747.1998.00271.x     Document Type: Article
Times cited : (10)

References (43)
  • 1
    • 0025303307 scopus 로고
    • Structural and biochemical properties of cloned and expressed human and rat steroid 5α-reductases
    • Andersson S, Russel DW: Structural and biochemical properties of cloned and expressed human and rat steroid 5α-reductases. Proc Natl Acad Sci USA 87:3640-3644, 1990
    • (1990) Proc Natl Acad Sci USA , vol.87 , pp. 3640-3644
    • Andersson, S.1    Russel, D.W.2
  • 2
    • 0026055914 scopus 로고
    • Deletion of steroid 5α-reductase 2 gene in male pseudophermaphroditism
    • Andersson S, Bergman DM, Jenkins EP, Russel DW: Deletion of steroid 5α-reductase 2 gene in male pseudophermaphroditism. Nature 354:159-161, 1991
    • (1991) Nature , vol.354 , pp. 159-161
    • Andersson, S.1    Bergman, D.M.2    Jenkins, E.P.3    Russel, D.W.4
  • 3
    • 0023742408 scopus 로고
    • Alopecia and hirsuties. Current concepts in pathogenesis and management
    • Barth JH: Alopecia and hirsuties. Current concepts in pathogenesis and management. Drugs 35:83-91, 1988
    • (1988) Drugs , vol.35 , pp. 83-91
    • Barth, J.H.1
  • 4
    • 0022599534 scopus 로고
    • Effect of a new topically active antiandrogen (RU38882) on the rat sebaceous gland: Comparison with cyproterone acetate
    • Bouton MM, Lecaque D, Secchi J, Tournemine C: Effect of a new topically active antiandrogen (RU38882) on the rat sebaceous gland: comparison with cyproterone acetate. J Invest Dermatol 86:163-167, 1986
    • (1986) J Invest Dermatol , vol.86 , pp. 163-167
    • Bouton, M.M.1    Lecaque, D.2    Secchi, J.3    Tournemine, C.4
  • 6
    • 0028850199 scopus 로고
    • Local and systemic reduction by topical finasteride or flutamide on hamster flank organ size and enzyme activity
    • Chen C, Puy LA, Simard J, Li X, Singh SM, Labrie F: Local and systemic reduction by topical finasteride or flutamide on hamster flank organ size and enzyme activity. J Invest Dermatol 105:678-682, 1995
    • (1995) J Invest Dermatol , vol.105 , pp. 678-682
    • Chen, C.1    Puy, L.A.2    Simard, J.3    Li, X.4    Singh, S.M.5    Labrie, F.6
  • 7
    • 0014664484 scopus 로고
    • Pathogenesis of acne
    • Cunliffe WJ, Shuster S: Pathogenesis of acne. Lancet i:685-687, 1969a
    • (1969) Lancet , vol.1 , pp. 685-687
    • Cunliffe, W.J.1    Shuster, S.2
  • 8
    • 0014569553 scopus 로고
    • The rate of sebum secretion in man
    • Cunliffe WJ, Shuster S: The rate of sebum secretion in man. Br J Dermatol 81:697-704, 1969b
    • (1969) Br J Dermatol , vol.81 , pp. 697-704
    • Cunliffe, W.J.1    Shuster, S.2
  • 10
    • 0242412099 scopus 로고
    • Flutamide in the treatment of female androgenic alopecia
    • Cusan L, Dupont A, Cossette M, Labrie F: Flutamide in the treatment of female androgenic alopecia. Can J Dermatol 5:421-427, 1993
    • (1993) Can J Dermatol , vol.5 , pp. 421-427
    • Cusan, L.1    Dupont, A.2    Cossette, M.3    Labrie, F.4
  • 11
    • 0028140279 scopus 로고
    • Comparison of flutamide and spironolactone in the treatment of hirsutism: A randomized controlled trial
    • Cusan L, Dupont A, Gomez JL, Tremblay RR, Labrie F: Comparison of flutamide and spironolactone in the treatment of hirsutism: a randomized controlled trial. Fertil Steril 61:281-287, 1994
    • (1994) Fertil Steril , vol.61 , pp. 281-287
    • Cusan, L.1    Dupont, A.2    Gomez, J.L.3    Tremblay, R.R.4    Labrie, F.5
  • 12
    • 0020049421 scopus 로고
    • Circulating testosterone, sex hormone binding globulin and prolactin in women with the late onset or persistent acne vulgaris
    • Darley CR, Kirby JD, Besser GM, Munro DD, Edwards CR, Rees LH: Circulating testosterone, sex hormone binding globulin and prolactin in women with the late onset or persistent acne vulgaris. Br J Dermatol 106:517-522, 1982
    • (1982) Br J Dermatol , vol.106 , pp. 517-522
    • Darley, C.R.1    Kirby, J.D.2    Besser, G.M.3    Munro, D.D.4    Edwards, C.R.5    Rees, L.H.6
  • 13
    • 0026607813 scopus 로고
    • Hair growth effects of oral administration of finasteride, a steroid 5α-reductase inhibitor, alone and in combination with topical minoxidil in the balding stumptail macaque
    • Diani AR, Mulholland MJ, Shull KL, et al: Hair growth effects of oral administration of finasteride, a steroid 5α-reductase inhibitor, alone and in combination with topical minoxidil in the balding stumptail macaque. J Clin Endocrinol Metab 74:345-350, 1992
    • (1992) J Clin Endocrinol Metab , vol.74 , pp. 345-350
    • Diani, A.R.1    Mulholland, M.J.2    Shull, K.L.3
  • 14
    • 0025037581 scopus 로고
    • Testosterone at high concentrations interacts with the human androgen receptor similarly to dihydrotestosterone
    • Grino P, Griffin J, Wilson J: Testosterone at high concentrations interacts with the human androgen receptor similarly to dihydrotestosterone. Endocrinology 126:1165-1172, 1990
    • (1990) Endocrinology , vol.126 , pp. 1165-1172
    • Grino, P.1    Griffin, J.2    Wilson, J.3
  • 15
    • 0000725194 scopus 로고
    • The sebaceous glands of the hamster. Morphological effects of androgens on integumentary structure
    • Hamilton JB, Montagna W: The sebaceous glands of the hamster. Morphological effects of androgens on integumentary structure. Am J Anat 86:191-233, 1950
    • (1950) Am J Anat , vol.86 , pp. 191-233
    • Hamilton, J.B.1    Montagna, W.2
  • 16
    • 0026447995 scopus 로고
    • Identification and selective inhibition of an isoenzyme of steroid 5α-reductase in human scalp
    • Harris G, Azzolina B, Baginsky W, et al: Identification and selective inhibition of an isoenzyme of steroid 5α-reductase in human scalp. Proc Natl Acad Sci USA 89:10787-10791, 1992
    • (1992) Proc Natl Acad Sci USA , vol.89 , pp. 10787-10791
    • Harris, G.1    Azzolina, B.2    Baginsky, W.3
  • 17
    • 0026793638 scopus 로고
    • Comparison of the effects of the 5α-reductase inhibitor finasteride and the antiandrogen flutamide on prostate and genital differentiation: Dose-response studies
    • Imperato-McIngley J, Sanchez R, Spencer JR, Yee B, Vaughan ED: Comparison of the effects of the 5α-reductase inhibitor finasteride and the antiandrogen flutamide on prostate and genital differentiation: dose-response studies. Endocrinolgy 131:1149-1156, 1992
    • (1992) Endocrinolgy , vol.131 , pp. 1149-1156
    • Imperato-McIngley, J.1    Sanchez, R.2    Spencer, J.R.3    Yee, B.4    Vaughan, E.D.5
  • 18
    • 0000882795 scopus 로고
    • Extension of multiple range tests to group means with unique numbers of replications
    • Kramer CY: Extension of multiple range tests to group means with unique numbers of replications. Biometrics 12:307-310, 1956
    • (1956) Biometrics , vol.12 , pp. 307-310
    • Kramer, C.Y.1
  • 21
    • 0026194822 scopus 로고
    • Combination of an antiandrogen and a 5α-reductase inhibitor: A further step towards total androgen blockade?
    • Labrie C, Trudel C, Li S, Martel C, Couet J, Labrie F: Combination of an antiandrogen and a 5α-reductase inhibitor: A further step towards total androgen blockade? Endocrinology 129:566-568, 1991
    • (1991) Endocrinology , vol.129 , pp. 566-568
    • Labrie, C.1    Trudel, C.2    Li, S.3    Martel, C.4    Couet, J.5    Labrie, F.6
  • 22
    • 0026787734 scopus 로고
    • Structure of human type II 5α-reductase
    • Labrie F, Sugimoto Y, Luu-The V, et al: Structure of human type II 5α-reductase. Endocrinology 131:1571-1573, 1992
    • (1992) Endocrinology , vol.131 , pp. 1571-1573
    • Labrie, F.1    Sugimoto, Y.2    Luu-The, V.3
  • 23
    • 2442767348 scopus 로고    scopus 로고
    • Androgen receptor
    • Adashi EY, Rock JA, Rosenwaks Z (eds). Lippincott-Raven Publishers, Philadelphia
    • Labrie F, Cusan L, Dupont A, et al: Androgen receptor. In: Adashi EY, Rock JA, Rosenwaks Z (eds). Reproductive Endocrinology, Surgery and Technology. Lippincott-Raven Publishers, Philadelphia, 1996, pp. 560-583
    • (1996) Reproductive Endocrinology, Surgery and Technology , pp. 560-583
    • Labrie, F.1    Cusan, L.2    Dupont, A.3
  • 24
    • 0028906285 scopus 로고
    • Synthesis and in vitro activity of 17β-(N-alkyl/arolformamido)- and 17β-[(N-alkyl/aryl) alkyl/arylamido]-4-methyl-4-aza-3-oxo-5α-androstan-3-ones as inhibitors of human 5α-reductases and antagonist of the androgen receptor
    • Li X, Singh SM, Labrie F: Synthesis and in vitro activity of 17β-(N-alkyl/arolformamido)- and 17β-[(N-alkyl/aryl) alkyl/arylamido]-4-methyl-4-aza-3-oxo-5α-androstan-3-ones as inhibitors of human 5α-reductases and antagonist of the androgen receptor. J Med Chem 38:1158-1173, 1995
    • (1995) J Med Chem , vol.38 , pp. 1158-1173
    • Li, X.1    Singh, S.M.2    Labrie, F.3
  • 26
    • 0021688977 scopus 로고
    • 17α-propylmesterolone (SH-434): An antiandrogenic sebosuppresive substance not influencing circulating testosterone concentrations. Experimental studies in Syrian hamsters
    • Luderschmidt C, Eiermann W, Jawny J, Bidlingmaier F, Ring J: 17α-propylmesterolone (SH-434): an antiandrogenic sebosuppresive substance not influencing circulating testosterone concentrations. Experimental studies in Syrian hamsters. Nauynyn Schmiedebergs Arch Pharmacol 328:214-218, 1984
    • (1984) Nauynyn Schmiedebergs Arch Pharmacol , vol.328 , pp. 214-218
    • Luderschmidt, C.1    Eiermann, W.2    Jawny, J.3    Bidlingmaier, F.4    Ring, J.5
  • 27
  • 28
    • 0028152349 scopus 로고
    • Characterization, expression and immunohistochemical localization of 5α-reductase in human skin
    • Luu-The V, Sugimoto Y, Puy L, Labrie Y, Lopez I, Singh M, Labrie F: Characterization, expression and immunohistochemical localization of 5α-reductase in human skin. J Invest Dermatol 102:221-226, 1994
    • (1994) J Invest Dermatol , vol.102 , pp. 221-226
    • Luu-The, V.1    Sugimoto, Y.2    Puy, L.3    Labrie, Y.4    Lopez, I.5    Singh, M.6    Labrie, F.7
  • 29
    • 0027500026 scopus 로고
    • Blockade of androstenedione-induced stimulation of androgen-sensitive parameters in the rat prostate by combination of Flutamide and 4-MA
    • Martel C, Trudel C, Couet J, Labrie C, Bélanger A, Labrie F: Blockade of androstenedione-induced stimulation of androgen-sensitive parameters in the rat prostate by combination of Flutamide and 4-MA. Mol Cell Endocrinol 91:43-49, 1993
    • (1993) Mol Cell Endocrinol , vol.91 , pp. 43-49
    • Martel, C.1    Trudel, C.2    Couet, J.3    Labrie, C.4    Bélanger, A.5    Labrie, F.6
  • 31
    • 0029026925 scopus 로고
    • Local inhibition of sebaceous gland growth by topically applied (RU 58841)
    • Matias JR, Gaillard M: Local inhibition of sebaceous gland growth by topically applied (RU 58841). Ann N Y Acad Sci 761:56-65, 1995
    • (1995) Ann N Y Acad Sci , vol.761 , pp. 56-65
    • Matias, J.R.1    Gaillard, M.2
  • 32
    • 7344267661 scopus 로고
    • Eichler O, Farh A, Herken H, Weleh AD (eds). Berlin Heidelberg, Springer-Verlag, New York
    • Neumann F, Steinback H: Androgens and antiandrogens. In: Eichler O, Farh A, Herken H, Weleh AD (eds). Berlin Heidelberg, Springer-Verlag, New York, 1991, p. 236
    • (1991) Androgens and Antiandrogens , pp. 236
    • Neumann, F.1    Steinback, H.2
  • 33
    • 0017616998 scopus 로고
    • Hamster car model for sebaceous glands
    • Plewig G, Luderschmidt C: Hamster car model for sebaceous glands. J Invest Dermatol 68:171-176, 1982
    • (1982) J Invest Dermatol , vol.68 , pp. 171-176
    • Plewig, G.1    Luderschmidt, C.2
  • 34
    • 7344264254 scopus 로고
    • Effect of antiandrogen on sebaceous glands and acne vulgaris. Animal experiments and studies in acne patients
    • Hammerstein J, Lachnia-Fixon U (eds). Excerpta Medica, Amsterdam, Oxford
    • Plewig G, Luderschmidt C: Effect of antiandrogen on sebaceous glands and acne vulgaris. Animal experiments and studies in acne patients. In: Hammerstein J, Lachnia-Fixon U (eds). Androgenization in Women. Excerpta Medica, Amsterdam, Oxford, 1991, pp. 96-102
    • (1991) Androgenization in Women , pp. 96-102
    • Plewig, G.1    Luderschmidt, C.2
  • 35
    • 0001563029 scopus 로고
    • Sebum production, casual sebum levels, titrable acidity of sebum, and urinary fractional, 17-ketosteroid excretion in males with acne
    • Pochi PE, Straus JS: Sebum production, casual sebum levels, titrable acidity of sebum, and urinary fractional, 17-ketosteroid excretion in males with acne. J Invest Dermatol 43:383-388, 1964
    • (1964) J Invest Dermatol , vol.43 , pp. 383-388
    • Pochi, P.E.1    Straus, J.S.2
  • 36
    • 0024098369 scopus 로고
    • Topical antiandrogens in the treatment of male pattern baldness
    • Rittmaster RS: Topical antiandrogens in the treatment of male pattern baldness. Clin Dermatol 6:122-128, 1988
    • (1988) Clin Dermatol , vol.6 , pp. 122-128
    • Rittmaster, R.S.1
  • 37
    • 0023185333 scopus 로고
    • The effects of N,N-diethyl-4-methyl-3-oxo-4-aza-5α-androstane-17β-carboxamide, a 5α-reductase inhibitor and antiandrogen, on the development of baldness in the stumptail macaque
    • Rittmaster RS, Vno, H, Povar ML, Mellin T, Loriaux D: The effects of N,N-diethyl-4-methyl-3-oxo-4-aza-5α-androstane-17β-carboxamide, a 5α-reductase inhibitor and antiandrogen, on the development of baldness in the stumptail macaque. J Clin Endocrinol Metab 65:188-193, 1987
    • (1987) J Clin Endocrinol Metab , vol.65 , pp. 188-193
    • Rittmaster, R.S.1    Vno, H.2    Povar, M.L.3    Mellin, T.4    Loriaux, D.5
  • 38
    • 0025689849 scopus 로고
    • The clinical development of a 5α-reductase inhibitor, finasteride
    • Stoner E: The clinical development of a 5α-reductase inhibitor, finasteride. J Steroid Biochem Mol Biol 37:375-378, 1990
    • (1990) J Steroid Biochem Mol Biol , vol.37 , pp. 375-378
    • Stoner, E.1
  • 39
    • 0018874772 scopus 로고
    • The antiandrogenic effect of progesterone on the hamster flank organ
    • Vermorken AJM, Goos CMAA, Roelofs HMJ: The antiandrogenic effect of progesterone on the hamster flank organ. Br J Dermatol 102:455-460, 1980
    • (1980) Br J Dermatol , vol.102 , pp. 455-460
    • Vermorken, A.J.M.1    Goos, C.M.A.A.2    Roelofs, H.M.J.3
  • 40
    • 0020030151 scopus 로고
    • Evaluation of the hamster flank organ test for the screening of antiandrogens
    • Vermorken AJM, Goos CMAA, Wirtz P: Evaluation of the hamster flank organ test for the screening of antiandrogens. Br J Dermatol 106:99-101, 1982
    • (1982) Br J Dermatol , vol.106 , pp. 99-101
    • Vermorken, A.J.M.1    Goos, C.M.A.A.2    Wirtz, P.3
  • 41
    • 0015605430 scopus 로고
    • The antiandrogen action of 4-androsten-3-one 17a-carboxyl acid and its methyl ester in hamster flank organ
    • Voigt W, Hsia SI: The antiandrogen action of 4-androsten-3-one 17a-carboxyl acid and its methyl ester in hamster flank organ. Endocrinology 92:1216-1222, 1973
    • (1973) Endocrinology , vol.92 , pp. 1216-1222
    • Voigt, W.1    Hsia, S.I.2
  • 42
    • 84943435168 scopus 로고
    • Antiandrogenic effects of topically applied spironolactone on the hamster flank organ
    • Weissmann A, Bowden J, Frank BL, Horwitz SN, Frost P: Antiandrogenic effects of topically applied spironolactone on the hamster flank organ. Arch Dermatol 121:57-62, 1985
    • (1985) Arch Dermatol , vol.121 , pp. 57-62
    • Weissmann, A.1    Bowden, J.2    Frank, B.L.3    Horwitz, S.N.4    Frost, P.5
  • 43
    • 0013986396 scopus 로고
    • Effect of an antiandrogen 17α-methyl-B-nortestosterone, on acne and hirsutism
    • Zarate A, Mahesh VB, Greenblatt RB: Effect of an antiandrogen 17α-methyl-B-nortestosterone, on acne and hirsutism. J Clin Endocrinol Metab 26:1394-4398, 1966
    • (1966) J Clin Endocrinol Metab , vol.26 , pp. 1394-4398
    • Zarate, A.1    Mahesh, V.B.2    Greenblatt, R.B.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.