Konský estrogen - Equine estrogen
Konské estrogenynebo koňské estrogeny, jsou estrogeny nalezen v koně.[1][2][3] Zahrnují následující:[1][2][3]
- Estradiol
- Estrone
- Equilin (Δ7-estron)
- Ekvilenin (Δ6,8-estron)
- 17α-dihydroekvilin (Δ7-17α-estradiol)
- 17p-dihydroekvilin (Δ7-17β-estradiol)
- 17α-dihydroekvilenin (Δ6,8-17α-estradiol)
- 17p-dihydroekvilenin (Δ6,8-17β-estradiol)
- 8,9-dehydroestron (Δ8-estron)
- 8,9-dehydroestradiol (Δ8-17β-estradiol)
- Hippulin (Δ8-14-isoestron)
Stejně jako jejich konjugáty, jako estron sulfát.
Konské estrogeny se nacházejí v humánních lécích konjugované estrogeny (Premarin) a esterifikované estrogeny (Estratab, Menest).[1][2][3]
| Ligand | Ostatní jména | Relativní vazebné afinity (RBA,%)A | Absolutní vazebné afinity (K.i, nM)A | Akce | ||
|---|---|---|---|---|---|---|
| ERα | ERβ | ERα | ERβ | |||
| Estradiol | E2; 17p-estradiol | 100 | 100 | 0.115 (0.04–0.24) | 0.15 (0.10–2.08) | Estrogen |
| Estrone | E1; 17-Ketoestradiol | 16.39 (0.7–60) | 6.5 (1.36–52) | 0.445 (0.3–1.01) | 1.75 (0.35–9.24) | Estrogen |
| Estriol | E3; 16a-OH-17p-E2 | 12.65 (4.03–56) | 26 (14.0–44.6) | 0.45 (0.35–1.4) | 0.7 (0.63–0.7) | Estrogen |
| Estetrol | E4; 15a, 16a-Di-OH-17p-E2 | 4.0 | 3.0 | 4.9 | 19 | Estrogen |
| Alfatradiol | 17α-estradiol | 20.5 (7–80.1) | 8.195 (2–42) | 0.2–0.52 | 0.43–1.2 | Metabolit |
| 16-Epiestriol | 16p-hydroxy-17p-estradiol | 7.795 (4.94–63) | 50 | ? | ? | Metabolit |
| 17-Epiestriol | 16α-hydroxy-17a-estradiol | 55.45 (29–103) | 79–80 | ? | ? | Metabolit |
| 16,17-epiestriol | 16p-Hydroxy-17a-estradiol | 1.0 | 13 | ? | ? | Metabolit |
| 2-hydroxyestradiol | 2-OH-E2 | 22 (7–81) | 11–35 | 2.5 | 1.3 | Metabolit |
| 2-methoxyestradiol | 2-MeO-E2 | 0.0027–2.0 | 1.0 | ? | ? | Metabolit |
| 4-hydroxyestradiol | 4-OH-E2 | 13 (8–70) | 7–56 | 1.0 | 1.9 | Metabolit |
| 4-methoxyestradiol | 4-MeO-E2 | 2.0 | 1.0 | ? | ? | Metabolit |
| 2-hydroxyestron | 2-OH-E1 | 2.0–4.0 | 0.2–0.4 | ? | ? | Metabolit |
| 2-methoxyestron | 2-MeO-E1 | <0.001–<1 | <1 | ? | ? | Metabolit |
| 4-hydroxyestron | 4-OH-E1 | 1.0–2.0 | 1.0 | ? | ? | Metabolit |
| 4-methoxyestron | 4-MeO-E1 | <1 | <1 | ? | ? | Metabolit |
| 16α-hydroxyestron | 16a-OH-El; 17-Ketoestriol | 2.0–6.5 | 35 | ? | ? | Metabolit |
| 2-hydroxyestriol | 2-OH-E3 | 2.0 | 1.0 | ? | ? | Metabolit |
| 4-methoxyestriol | 4-MeO-E3 | 1.0 | 1.0 | ? | ? | Metabolit |
| Estradiol sulfát | E2S; Estradiol 3-sulfát | <1 | <1 | ? | ? | Metabolit |
| Estradiol disulfát | Estradiol 3,17p-disulfát | 0.0004 | ? | ? | ? | Metabolit |
| Estradiol 3-glukuronid | E2-3G | 0.0079 | ? | ? | ? | Metabolit |
| Estradiol 17β-glukuronid | E2-17G | 0.0015 | ? | ? | ? | Metabolit |
| Estradiol 3-gluc. 17p-sulfát | E2-3G-17S | 0.0001 | ? | ? | ? | Metabolit |
| Estrone sulfát | E1S; Estrone 3-sulfát | <1 | <1 | >10 | >10 | Metabolit |
| Estradiol benzoát | EB; Estradiol 3-benzoát | 10 | ? | ? | ? | Estrogen |
| Estradiol 17β-benzoát | E2-17B | 11.3 | 32.6 | ? | ? | Estrogen |
| Estrone methylether | Estron 3-methylether | 0.145 | ? | ? | ? | Estrogen |
| ent-Estradiol | 1-estradiol | 1.31–12.34 | 9.44–80.07 | ? | ? | Estrogen |
| Equilin | 7-dehydroestron | 13 (4.0–28.9) | 13.0–49 | 0.79 | 0.36 | Estrogen |
| Ekvilenin | 6,8-didehydroestron | 2.0–15 | 7.0–20 | 0.64 | 0.62 | Estrogen |
| 17p-dihydroekvilin | 7-dehydro-17p-estradiol | 7.9–113 | 7.9–108 | 0.09 | 0.17 | Estrogen |
| 17α-dihydroekvilin | 7-dehydro-17a-estradiol | 18.6 (18–41) | 14–32 | 0.24 | 0.57 | Estrogen |
| 17p-dihydroekvilenin | 6,8-didehydro-17p-estradiol | 35–68 | 90–100 | 0.15 | 0.20 | Estrogen |
| 17α-dihydroekvilenin | 6,8-didehydro-17a-estradiol | 20 | 49 | 0.50 | 0.37 | Estrogen |
| Δ8-Estradiol | 8,9-dehydro-17p-estradiol | 68 | 72 | 0.15 | 0.25 | Estrogen |
| Δ8-Estrone | 8,9-dehydroestron | 19 | 32 | 0.52 | 0.57 | Estrogen |
| Ethinylestradiol | EE; 17α-Ethynyl-17β-E2 | 120.9 (68.8–480) | 44.4 (2.0–144) | 0.02–0.05 | 0.29–0.81 | Estrogen |
| Mestranol | EE 3-methylether | ? | 2.5 | ? | ? | Estrogen |
| Moxestrol | RU-2858; Llp-methoxy-EE | 35–43 | 5–20 | 0.5 | 2.6 | Estrogen |
| Methylestradiol | 17a-methyl-17p-estradiol | 70 | 44 | ? | ? | Estrogen |
| Diethylstilbestrol | DES; Stilbestrol | 129.5 (89.1–468) | 219.63 (61.2–295) | 0.04 | 0.05 | Estrogen |
| Hexestrol | Dihydrodiethylstilbestrol | 153.6 (31–302) | 60–234 | 0.06 | 0.06 | Estrogen |
| Dienestrol | Dehydrostilbestrol | 37 (20.4–223) | 56–404 | 0.05 | 0.03 | Estrogen |
| Benzestrol (B2) | – | 114 | ? | ? | ? | Estrogen |
| Chlorotrianisen | TACE | 1.74 | ? | 15.30 | ? | Estrogen |
| Trifenyletylen | TPE | 0.074 | ? | ? | ? | Estrogen |
| Trifenylbromethylen | TPBE | 2.69 | ? | ? | ? | Estrogen |
| Tamoxifen | ICI-46 474 | 3 (0.1–47) | 3.33 (0.28–6) | 3.4–9.69 | 2.5 | SERM |
| Afimoxifen | 4-hydroxytamoxifen; 4-OHT | 100.1 (1.7–257) | 10 (0.98–339) | 2.3 (0.1–3.61) | 0.04–4.8 | SERM |
| Toremifen | 4-chlorotamoxifen; 4-CT | ? | ? | 7.14–20.3 | 15.4 | SERM |
| Klomifen | MRL-41 | 25 (19.2–37.2) | 12 | 0.9 | 1.2 | SERM |
| Cyklofenil | F-6066; Sexovid | 151–152 | 243 | ? | ? | SERM |
| Nafoxidin | U-11 000A | 30.9–44 | 16 | 0.3 | 0.8 | SERM |
| Raloxifen | – | 41.2 (7.8–69) | 5.34 (0.54–16) | 0.188–0.52 | 20.2 | SERM |
| Arzoxifen | LY-353 381 | ? | ? | 0.179 | ? | SERM |
| Lasofoxifen | CP-336 156 | 10.2–166 | 19.0 | 0.229 | ? | SERM |
| Ormeloxifen | Centchroman | ? | ? | 0.313 | ? | SERM |
| Levormeloxifen | 6720-CDRI; NNC-460 020 | 1.55 | 1.88 | ? | ? | SERM |
| Ospemifen | Deaminohydroxytoremifen | 2.63 | 1.22 | ? | ? | SERM |
| Bazedoxifen | – | ? | ? | 0.053 | ? | SERM |
| Etacstil | GW-5638 | 4.30 | 11.5 | ? | ? | SERM |
| ICI-164 384 | – | 63.5 (3.70–97.7) | 166 | 0.2 | 0.08 | Antiestrogen |
| Fulvestrant | ICI-182 780 | 43.5 (9.4–325) | 21.65 (2.05–40.5) | 0.42 | 1.3 | Antiestrogen |
| Propylpyrazoletriol | PPT | 49 (10.0–89.1) | 0.12 | 0.40 | 92.8 | Agonista ERα |
| 16α-LE2 | 16α-lakton-17p-estradiol | 14.6–57 | 0.089 | 0.27 | 131 | Agonista ERα |
| 16α-Iodo-E2 | 16a-jod-17p-estradiol | 30.2 | 2.30 | ? | ? | Agonista ERα |
| Methylpiperidinopyrazol | MPP | 11 | 0.05 | ? | ? | Antagonista ERα |
| Diarylpropionitril | DPN | 0.12–0.25 | 6.6–18 | 32.4 | 1.7 | Agonista ERp |
| 8β-VE2 | 8p-Vinyl-17p-estradiol | 0.35 | 22.0–83 | 12.9 | 0.50 | Agonista ERp |
| Prinaberel | ERB-041; WAY-202 041 | 0.27 | 67–72 | ? | ? | Agonista ERp |
| ERB-196 | WAY-202,196 | ? | 180 | ? | ? | Agonista ERp |
| Erteberel | SERBA-1; 500 500 LY | ? | ? | 2.68 | 0.19 | Agonista ERp |
| SERBA-2 | – | ? | ? | 14.5 | 1.54 | Agonista ERp |
| Coumestrol | – | 9.225 (0.0117–94) | 64.125 (0.41–185) | 0.14–80.0 | 0.07–27.0 | Xenoestrogen |
| Genistein | – | 0.445 (0.0012–16) | 33.42 (0.86–87) | 2.6–126 | 0.3–12.8 | Xenoestrogen |
| Equol | – | 0.2–0.287 | 0.85 (0.10–2.85) | ? | ? | Xenoestrogen |
| Daidzein | – | 0.07 (0.0018–9.3) | 0.7865 (0.04–17.1) | 2.0 | 85.3 | Xenoestrogen |
| Biochanin A | – | 0.04 (0.022–0.15) | 0.6225 (0.010–1.2) | 174 | 8.9 | Xenoestrogen |
| Kaempferol | – | 0.07 (0.029–0.10) | 2.2 (0.002–3.00) | ? | ? | Xenoestrogen |
| Naringenin | – | 0.0054 (<0.001–0.01) | 0.15 (0.11–0.33) | ? | ? | Xenoestrogen |
| 8-Prenylnaringenin | 8-PN | 4.4 | ? | ? | ? | Xenoestrogen |
| Quercetin | – | <0.001–0.01 | 0.002–0.040 | ? | ? | Xenoestrogen |
| Ipriflavon | – | <0.01 | <0.01 | ? | ? | Xenoestrogen |
| Miroestrol | – | 0.39 | ? | ? | ? | Xenoestrogen |
| Deoxymiroestrol | – | 2.0 | ? | ? | ? | Xenoestrogen |
| β-sitosterol | – | <0.001–0.0875 | <0.001–0.016 | ? | ? | Xenoestrogen |
| Resveratrol | – | <0.001–0.0032 | ? | ? | ? | Xenoestrogen |
| a-Zearalenol | – | 48 (13–52.5) | ? | ? | ? | Xenoestrogen |
| p-zearalenol | – | 0.6 (0.032–13) | ? | ? | ? | Xenoestrogen |
| Zeranol | a-Zearalanol | 48–111 | ? | ? | ? | Xenoestrogen |
| Taleranol | p-Zearalanol | 16 (13–17.8) | 14 | 0.8 | 0.9 | Xenoestrogen |
| Zearalenon | ZEN | 7.68 (2.04–28) | 9.45 (2.43–31.5) | ? | ? | Xenoestrogen |
| Zearalanon | ZAN | 0.51 | ? | ? | ? | Xenoestrogen |
| Bisfenol A | BPA | 0.0315 (0.008–1.0) | 0.135 (0.002–4.23) | 195 | 35 | Xenoestrogen |
| Endosulfan | EDS | <0.001–<0.01 | <0.01 | ? | ? | Xenoestrogen |
| Kepone | Chlordekon | 0.0069–0.2 | ? | ? | ? | Xenoestrogen |
| o, p '-DDT | – | 0.0073–0.4 | ? | ? | ? | Xenoestrogen |
| p, p '-DDT | – | 0.03 | ? | ? | ? | Xenoestrogen |
| Methoxychlor | p, p '-Dimethoxy-DDT | 0.01 (<0.001–0.02) | 0.01–0.13 | ? | ? | Xenoestrogen |
| HPTE | Hydroxychlor; p, p '-OH-DDT | 1.2–1.7 | ? | ? | ? | Xenoestrogen |
| Testosteron | T; 4-Androstenolone | <0.0001–<0.01 | <0.002–0.040 | >5000 | >5000 | Androgen |
| Dihydrotestosteron | DHT; 5α-Androstanolone | 0.01 (<0.001–0.05) | 0.0059–0.17 | 221–>5000 | 73–1688 | Androgen |
| Nandrolon | 19-nortestosteron; 19-NT | 0.01 | 0.23 | 765 | 53 | Androgen |
| Dehydroepiandrosteron | DHEA; Prasterone | 0.038 (<0.001–0.04) | 0.019–0.07 | 245–1053 | 163–515 | Androgen |
| 5-Androstendiol | A5; Androstendiol | 6 | 17 | 3.6 | 0.9 | Androgen |
| 4-Androstendiol | – | 0.5 | 0.6 | 23 | 19 | Androgen |
| 4-Androstendion | A4; Androstendion | <0.01 | <0.01 | >10000 | >10000 | Androgen |
| 3α-Androstandiol | 3α-Adiol | 0.07 | 0.3 | 260 | 48 | Androgen |
| 3β-Androstandiol | 3β-Adiol | 3 | 7 | 6 | 2 | Androgen |
| Androstandion | 5α-Androstandion | <0.01 | <0.01 | >10000 | >10000 | Androgen |
| Etiocholanedion | 5β-Androstandion | <0.01 | <0.01 | >10000 | >10000 | Androgen |
| Methyltestosteron | 17α-methyltestosteron | <0.0001 | ? | ? | ? | Androgen |
| Ethinyl-3α-androstandiol | 17a-Ethynyl-3a-adiol | 4.0 | <0.07 | ? | ? | Estrogen |
| Ethinyl-3β-androstandiol | 17a-Ethynyl-3p-adiol | 50 | 5.6 | ? | ? | Estrogen |
| Progesteron | P4; 4-Pregnendion | <0.001–0.6 | <0.001–0.010 | ? | ? | Progestogen |
| Norethisteron | SÍŤ; 17α-Ethynyl-19-NT | 0.085 (0.0015–<0.1) | 0.1 (0.01–0.3) | 152 | 1084 | Progestogen |
| Norethynodrel | 5 (10) -Norethisteron | 0.5 (0.3–0.7) | <0.1–0.22 | 14 | 53 | Progestogen |
| Tibolon | 7α-Methylnorethynodrel | 0.5 (0.45–2.0) | 0.2–0.076 | ? | ? | Progestogen |
| Δ4-Tibolon | 7α-methylnorethisteron | 0.069–<0.1 | 0.027–<0.1 | ? | ? | Progestogen |
| 3α-hydroxytibolon | – | 2.5 (1.06–5.0) | 0.6–0.8 | ? | ? | Progestogen |
| 3β-hydroxytibolon | – | 1.6 (0.75–1.9) | 0.070–0.1 | ? | ? | Progestogen |
| Poznámky pod čarou: A = (1) Vazebná afinita hodnoty mají formát „medián (rozsah)“ (# (# - #)), „rozsah“ (# - #) nebo „hodnota“ (#) v závislosti na dostupných hodnotách. Úplné sady hodnot v rozmezí najdete v kódu Wiki. (2) Vazebné afinity byly stanoveny pomocí studií vytěsnění u různých typů in-vitro systémy s označeno estradiol a člověk ERα a ERβ proteiny (s výjimkou hodnot ERp od Kuiper et al. (1997), které jsou krysí ERp). Zdroje: Viz stránka šablony. | ||||||
Viz také
Reference
- ^ A b C Kuhl H (2005). „Farmakologie estrogenů a progestogenů: vliv různých cest podání“ (PDF). Klimakterický. 8 Suppl 1: 3–63. doi:10.1080/13697130500148875. PMID 16112947.
- ^ A b C Bhavnani BR, Tam SP, Lu X (říjen 2008). „Vztahy mezi strukturní aktivitou a rozdílné interakce a funkční aktivita různých koňských estrogenů zprostředkovaných prostřednictvím estrogenových receptorů (ER) ERalpha a ERbeta“. Endokrinologie. 149 (10): 4857–70. doi:10.1210 / cs.2008-0304. PMID 18599548.
- ^ A b C Bhavnani BR (červen 2003). „Estrogeny a menopauza: farmakologie konjugovaných koňských estrogenů a jejich potenciální role v prevenci neurodegenerativních onemocnění, jako je Alzheimerova choroba“. J. Steroid Biochem. Mol. Biol. 85 (2–5): 473–82. doi:10.1016 / s0960-0760 (03) 00220-6. PMID 12943738.
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