From Wikipedia, the free encyclopedia
Chemical compound
ERB-196 , also known as WAY-202196 , is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of the ERβ .[ 1] [ 2] [ 3] [ 4] [ 5] [ 6] ERα .[ 1] Wyeth for the treatment of inflammation and sepsis starting in 2004 but development was discontinued by 2011.[ 2] [ 7]
^ a b Manas ES, MewshawRE, Harris HA, Malamas MS (2006). "Isoform Specificity: The Design of Estrogen Receptor-β Selective Compounds" . In Hubbard RE (ed.). Structure-based Drug Discovery: An Overview . Royal Society of Chemistry. pp. 241–. ISBN 978-0-85404-351-4 ^ a b "ERB 196" . AdisInsight . Springer Nature Switzerland AG. Archived from the original on 25 June 2018. Retrieved 15 January 2022 .^ Acton QA (2013). "Estradiol" . Estrogens—Advances in Research and Application . ScholarlyEditions. pp. 52–. ISBN 978-1-4816-8771-3 ^ Weatherman RV (8 September 2008). "Untangling the Estrogen Receptor Web: Tools to Selectively Study Estrogen-Binding Receptors" . In Ottow E, Weinmann H (eds.). Nuclear Receptors as Drug Targets . Methods and Principles in Medicinal Chemistry. John Wiley & Sons. pp. 66–. doi :10.1002/9783527623297.ch3 . ISBN 978-3-527-62330-3 ^ Mewshaw RE, Edsall RJ, Yang C, Manas ES, Xu ZB, Henderson RA, et al. (June 2005). "ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity". Journal of Medicinal Chemistry . 48 (12): 3953–3979. doi :10.1021/jm058173s . PMID 15943471 . ^ Cristofaro PA, Opal SM, Palardy JE, Parejo NA, Jhung J, Keith JC, Harris HA (August 2006). "WAY-202196, a selective estrogen receptor-beta agonist, protects against death in experimental septic shock". Critical Care Medicine . 34 (8): 2188–2193. doi :10.1097/01.CCM.0000227173.13497.56 . PMID 16755255 . S2CID 20876539 . ^ Adrie C, Azoulay E, Timsit JF (8 December 2007). "Influence of Gender on Outcome of Severe Sepsis" . In Vincent JL (ed.). Yearbook of Intensive Care and Emergency Medicine 2007 . Springer Science & Business Media. pp. 891–. ISBN 978-3-540-49433-1
ER Tooltip Estrogen receptor
Agonists
Steroidal: 2-Hydroxyestradiol 2-Hydroxyestrone 3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol 3α-Androstanediol 3α,5α-Dihydrolevonorgestrel 3β,5α-Dihydrolevonorgestrel 3α-Hydroxytibolone 3β-Hydroxytibolone 3β-Androstanediol 4-Androstenediol 4-Androstenedione 4-Fluoroestradiol 4-Hydroxyestradiol 4-Hydroxyestrone 4-Methoxyestradiol 4-Methoxyestrone 5-Androstenediol 7-Oxo-DHEA 7α-Hydroxy-DHEA 7α-Methylestradiol 7β-Hydroxyepiandrosterone 8,9-Dehydroestradiol 8,9-Dehydroestrone 8β-VE2 10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED) 11β-Chloromethylestradiol 11β-Methoxyestradiol 15α-Hydroxyestradiol 16-Ketoestradiol 16-Ketoestrone 16α-Fluoroestradiol 16α-Hydroxy-DHEA 16α-Hydroxyestrone 16α-Iodoestradiol 16α-LE2 16β-Hydroxyestrone 16β,17α-Epiestriol (16β-hydroxy-17α-estradiol) 17α-Estradiol (alfatradiol )17α-Dihydroequilenin 17α-Dihydroequilin 17α-Epiestriol (16α-hydroxy-17α-estradiol) 17α-Ethynyl-3α-androstanediol 17α-Ethynyl-3β-androstanediol 17β-Dihydroequilenin 17β-Dihydroequilin 17β-Methyl-17α-dihydroequilenin Abiraterone Abiraterone acetate Alestramustine Almestrone Anabolic steroids (e.g., testosterone and esters , methyltestosterone , metandienone (methandrostenolone) , nandrolone and esters , many others; via estrogenic metabolites)Atrimustine Bolandiol Bolandiol dipropionate Butolame Clomestrone Cloxestradiol
Conjugated estriol Conjugated estrogens Cyclodiol Cyclotriol DHEA DHEA-S ent -EstradiolEpiestriol (16β-epiestriol, 16β-hydroxy-17β-estradiol) Epimestrol Equilenin Equilin ERA-63 (ORG-37663) Esterified estrogens Estetrol Estradiol
Estramustine Estramustine phosphate Estrapronicate Estrazinol Estriol
Estrofurate Estrogenic substances Estromustine Estrone
Etamestrol (eptamestrol) Ethinylandrostenediol
Ethinylestradiol
Ethinylestriol Ethylestradiol Etynodiol Etynodiol diacetate Hexolame Hippulin Hydroxyestrone diacetate Lynestrenol Lynestrenol phenylpropionate Mestranol Methylestradiol Moxestrol Mytatrienediol Nilestriol Norethisterone Noretynodrel Orestrate Pentolame Prodiame Prolame Promestriene RU-16117 Quinestradol Quinestrol Tibolone Xenoestrogens: Anise -related (e.g., anethole , anol , dianethole , dianol , photoanethole )Chalconoids (e.g., isoliquiritigenin , phloretin , phlorizin (phloridzin) , wedelolactone )Coumestans (e.g., coumestrol , psoralidin )Flavonoids (incl. 7,8-DHF , 8-prenylnaringenin , apigenin , baicalein , baicalin , biochanin A , calycosin , catechin , daidzein , daidzin , ECG , EGCG , epicatechin , equol , formononetin , glabrene , glabridin , genistein , genistin , glycitein , kaempferol , liquiritigenin , mirificin , myricetin , naringenin , penduletin , pinocembrin , prunetin , puerarin , quercetin , tectoridin , tectorigenin )Lavender oil Lignans (e.g., enterodiol , enterolactone , nyasol (cis -hinokiresinol) )Metalloestrogens (e.g., cadmium )Pesticides (e.g., alternariol , dieldrin , endosulfan , fenarimol , HPTE , methiocarb , methoxychlor , triclocarban , triclosan )Phytosteroids (e.g., digitoxin (digitalis ), diosgenin , guggulsterone )Phytosterols (e.g., β-sitosterol , campesterol , stigmasterol )Resorcylic acid lactones (e.g., zearalanone , α-zearalenol , β-zearalenol , zearalenone , zeranol (α-zearalanol) , taleranol (teranol, β-zearalanol) )Steroid -like (e.g., deoxymiroestrol , miroestrol )Stilbenoids (e.g., resveratrol , rhaponticin )Synthetic xenoestrogens (e.g., alkylphenols , bisphenols (e.g., BPA , BPF , BPS ), DDT , parabens , PBBs , PHBA , phthalates , PCBs )Others (e.g., agnuside , rotundifuran ) MixedSERMs Tooltip Selective estrogen receptor modulators ) Antagonists
Coregulator-binding modulators: ERX-11
GPER Tooltip G protein-coupled estrogen receptor
Agonists Antagonists Unknown
