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Template:Relative affinities of anabolic steroids and related steroids

Relative affinities (%) of anabolic steroids and related steroids

Compound Chemical name PR AR ER GR MR SHBG CBG
Androstanolone DHT 1.4–1.5 60–120 <0.1 <0.1, 0.3 0.15 100 0.8
Boldenone Δ1-T <1 50–75 ? <1 ? ? ?
Danazol 2,3-Isoxazol-17α-Ety-T 9 8 ? <0.1a ? 8 10
Dienolone 9-19-NT 17 134 <0.1 1.6 0.3 ? ?
Dimethyldienolone 9-7α,17α-DiMe-19-NT 198 122 0.1 6.1 1.7 ? ?
Dimethyltrienolone 9,11-7α,17α-DiMe-19-NT 306 180 0.1 22 52 ? ?
Drostanolone 2α-Me-DHT ? ? ? ? ? 39 ?
Ethisterone 17α-Ety-T 35 0.1 <1.0 <1.0 <1.0 25–92 0.3
Ethylestrenol 3-DeO-17α-Et-19-NT ? ? ? ? ? <1 ?
Fluoxymesterone 9α-F-11β-OH-17α-Me-T ? ? ? ? ? ≤3 ?
Gestrinone 9,11-17α-Ety-18-Me-19-NT 75–76 83–85 <0.1, 3–10 77 3.2 ? ?
Levonorgestrel 17α-Ety-18-Me-19-NT 170 84–87 <0.1 14 0.6–0.9 14–50 <0.1
Mestanolone 17α-Me-DHT 5–10 100–125 ? <1 ? 84 ?
Mesterolone 1α-Me-DHT ? ? ? ? ? 82–440 ?
Metandienone 1-17α-Me-T ? ? ? ? ? 2 ?
Metenolone 1-1-Me-DHT ? ? ? ? ? 3 ?
Methandriol 17α-Me-A5 ? ? ? ? ? 40 ?
Methasterone 2α,17α-DiMe-DHT ? ? ? ? ? 58 ?
Methyldienolone 9-17α-Me-19-NT 71 64 <0.1 6 0.4 ? ?
Methyltestosterone 17α-Me-T 3 45, 100–125 ? 1–5 ? 5–64 <0.1
Methyl-1-testosterone 1-17α-Me-DHT ? ? ? ? ? 69 ?
Metribolone 9,11-17α-Me-19-NT 208–210 199–210 <0.1 10–26 18 0.2–0.8 ≤0.4
Mibolerone 7α,17α-DiMe-19-NT 214 108 <0.1 1.4 2.1 6 ?
Nandrolone 19-NT 20 154–155 <0.1 0.5 1.6 1–16 0.1
Norethandrolone 17α-Et-19-NT ? ? ? ? ? 3 ?
Norethisterone 17α-Ety-19-NT 155–156 43–45 <0.1 2.7–2.8 0.2 5–21 0.3
Norgestrienone 9,11-17α-Ety-19-NT 63–65 70 <0.1 11 1.8 ? ?
Normethandrone 17α-Me-19-NT 100 146 <0.1 1.5 0.6 7 ?
Oxandrolone 2-Oxa-17α-Me-DHT ? ? ? ? ? <1 ?
Oxymetholone 2-OHMeEne-17α-Me-DHT ? ? ? ? ? ≤3 ?
RU-2309 (17α-Me-THG) 9,11-17α,18-DiMe-19-NT 230 143 <0.1 155 36 ? ?
Stanozolol 2,3-Pyrazol-17α-Me-DHT ? ? ? ? ? 1–36 ?
Testosterone T 1.0–1.2 100 <0.1 0.17 0.9 19–82 3–8
1-Testosterone 1-DHT ? ? ? ? ? 98 ?
Tibolone 7α-Me-17α-Ety-19-N-5(10)-T 12 12 1 ? ? ? ?
Δ4-Tibolone 7α-Me-17α-Ety-19-NT 180 70 1 <1 2 1–8 <1
Trenbolone 9,11-19-NT 74–75 190–197 <0.1 2.9 1.33 ? ?
Trestolone 7α-Me-19-NT 50–75 100–125 ? <1 ? 12 ?
Notes: Values are percentages (%). Reference ligands (100%) were progesterone for the PR, testosterone for the AR, estradiol for the ER, dexamethasone for the GR, aldosterone for the MR, dihydrotestosterone for SHBG, and cortisol for CBG. Footnotes: a = 1-hour incubation time (4 hours is standard for this assay; may affect affinity value). Sources: [1][2][3][4][5][6][7][8][9]

ReferencesEdit

  1. ^ Delettré J, Mornon JP, Lepicard G, Ojasoo T, Raynaud JP (January 1980). "Steroid flexibility and receptor specificity". J. Steroid Biochem. 13 (1): 45–59. doi:10.1016/0022-4731(80)90112-0. PMID 7382482.
  2. ^ Ojasoo T, Delettré J, Mornon JP, Turpin-VanDycke C, Raynaud JP (1987). "Towards the mapping of the progesterone and androgen receptors". J. Steroid Biochem. 27 (1–3): 255–69. doi:10.1016/0022-4731(87)90317-7. PMID 3695484.
  3. ^ Raynaud JP, Bouton MM, Moguilewsky M, Ojasoo T, Philibert D, Beck G, Labrie F, Mornon JP (January 1980). "Steroid hormone receptors and pharmacology". J. Steroid Biochem. 12: 143–57. doi:10.1016/0022-4731(80)90264-2. PMID 7421203.
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  6. ^ Saartok T, Dahlberg E, Gustafsson JA (June 1984). "Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin". Endocrinology. 114 (6): 2100–6. doi:10.1210/endo-114-6-2100. PMID 6539197.
  7. ^ Cunningham GR, Tindall DJ, Lobl TJ, Campbell JA, Means AR (September 1981). "Steroid structural requirements for high affinity binding to human sex steroid binding protein (SBP)". Steroids. 38 (3): 243–62. doi:10.1016/0039-128X(81)90061-1. PMID 7197818.
  8. ^ Pugeat MM, Dunn JF, Nisula BC (July 1981). "Transport of steroid hormones: interaction of 70 drugs with testosterone-binding globulin and corticosteroid-binding globulin in human plasma". J. Clin. Endocrinol. Metab. 53 (1): 69–75. doi:10.1210/jcem-53-1-69. PMID 7195405.
  9. ^ Kuhl H (2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 Suppl 1: 3–63. doi:10.1080/13697130500148875. PMID 16112947.