DOCSLIB.ORG

Androgen Receptor

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Androgen Receptor Androgen Receptor Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression. Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype. Mutations in this gene are also associated with complete androgen insensitivity (CAIS). www.MedChemExpress.com 1 Androgen Receptor Inhibitors, Agonists, Antagonists & Modulators (R)-UT-155 2,2,5,7,8-Pentamethyl-6-Chromanol Cat. No.: HY-112895A (PMC) Cat. No.: HY-111024 (R)-UT-155 (compound 11) is a selective androgen 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the receptor degrader (SARD) ligand. Less active than anti-oxidant moiety of vitamin E (α-tocopherol). the S-isomer. 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Size: 250 mg, 500 mg Size: 10 mM × 1 mL, 100 mg 3,3'-Diindolylmethane ACP-105 (DIM; Arundine; HB 236) Cat. No.: HY-15758 Cat. No.: HY-112256 3,3'-Diindolylmethane is a strong, pure androgen ACP-105 is an orally available, selective amd receptor (AR) antagonist. potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively. Purity: 98.74% Purity: 98.37% Clinical Data: Phase 4 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 200 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Ailanthone Andarine (Δ13-Dehydrochaparrinone) Cat. No.: HY-N1943 (GTx-007; S-4) Cat. No.: HY-12023 Ailanthone (Δ13-Dehydrochaparrinone) is a potent Andarine (S-4) is an investigational selective inhibitor of both full-length androgen receptor androgen receptor modulator (SARM) and an active (AR) (IC50=69nM) and constitutively active partial agonist. truncated AR splice variants (AR1-651 IC50=309nM). Purity: 99.71% Purity: 99.51% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- Androstanolone acetate (Androst-4-ene-3β,17β-diol, dipropionate) Cat. No.: HY-U00272 Cat. No.: HY-111847 Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- Androstanolone acetate is an androgen ligand, is the dipropanoate of 4-Androstenediol, a which targets androgen receptor (AR). metabolite of testosterone. Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 5 mg Apalutamide AZD3514 (ARN-509) Cat. No.: HY-16060 Cat. No.: HY-16079 Apalutamide (ARN-509) is a potent and competitive AZD3514 is a potent and oral androgen receptor androgen receptor (AR) antagonist, binding AR downregulator with Ki of 2.2 μM and has ability of with an IC50 of 16 nM. reducing AR protein expression. Purity: 99.69% Purity: 98.77% Clinical Data: Phase 3 Clinical Data: Phase 1 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Bicalutamide Bifluranol Cat. No.: HY-14249 (BX341) Cat. No.: HY-U00229 Bicalutamide is a non-steroidal androgen Bifluranol (BX341) is an anti-androgen. receptor inhibitor. Purity: 99.61% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 200 mg, 500 mg, 1 g, 5 g Size: 1 mg, 5 mg, 10 mg, 20 mg BMS-564929 Boldenone Cypionate Cat. No.: HY-12111 Cat. No.: HY-118603 BMS-564929 is an androgen receptor (AR) agonist, Boldenone Cypionate is an androgenic anabolic binds to androgen receptor (AR) with a Ki of steroid. 2.11±0.16 nM. Purity: 98.70% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Boldenone Undecylenate Clascoterone (Cortexolone 17 alpha-propionate; Cortexolone (Ba 29038) Cat. No.: HY-17434 17α-propionate; CB-03-01) Cat. No.: HY-13331 Boldenone Undecylenate (Ba 29038) is a synthetic Clascoterone is a new topical and peripherally steroid which has a similar effect as the natural selective androgen antagonist. steroid testosterone; it is frequently used in veterinary medicine, though it is also used in humans. Purity: 96.33% Purity: 98.76% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Cyproterone acetate D4-abiraterone Cat. No.: HY-13604 (Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite) Cat. No.: HY-109619 Cyproterone acetate is an androgen receptor (AR) D4-abiraterone is a major metabolite of antagonist with IC50 of 7.1 nM, as well as a weak abiraterone. D4-abiraterone is an inhibitor of progesterone receptor agonist with weak CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) pro-gestational and glucocorticoid activity. and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor. Purity: 99.71% Purity: 99.42% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 250 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Danazol Darolutamide Cat. No.: HY-B1029 (ODM-201; BAY-1841788) Cat. No.: HY-16985 Danazol is a derivative of the synthetic steroid Darolutamide (ODM-201;BAY-1841788) is a potent ethisterone, that suppresses the production of androgen receptor (AR) antagonist with an IC50 of gonadotrophins, and has some weak androgenic 26 nM in in vitro assay. effects. Purity: 99.91% Purity: 97.72% Clinical Data: Launched Clinical Data: Phase 3 Size: 10 mM × 1 mL, 100 mg, 250 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg www.MedChemExpress.com 3 Dehydroisoandrosterone 3-acetate DHEA (Prasterone; Dehydroisoandrosterone; (Dehydroepiandrosterone 3-acetate; DHEA acetate) Cat. No.: HY-B1405 Dehydroepiandrosterone) Cat. No.: HY-14650 Dehydroepiandrosterone 3-acetate is a DHEA (Prasterone) is one of the most abundant testosterone/estrogen precursor and known steroid hormones. DHEA (Prasterone) mediates its modulator of vertebrate aggression. action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g. Purity: >98.0% Purity: >98.0% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10 mM × 1 mL, 1 g, 5 g Size: 10 mM × 1 mL, 100 mg, 500 mg Dimethylcurcumin DJ-V-159 (ASC-J9; GO-Y025) Cat. No.: HY-15194 Cat. No.: HY-114165 Dimethylcurcumin (ASC-J9) is an androgen DJ-V-159 is an agonist for G protein-coupled receptor degradation enhancer that effectively receptor family C group 6 member A (GPRC6A). suppresses castration resistant prostate cancer cell proliferation and invasion. Purity: 98.06% Purity: 99.99% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Enzalutamide Epiandrosterone (MDV3100) Cat. No.: HY-70002 (3β-Androsterone; trans-Androsterone; iso-Androsterone) Cat. No.: HY-I0352 Enzalutamide (MDV3100) is an androgen receptor Epiandrosterone is a steroid hormone with weak (AR) antagonist with an IC50 of 36 nM in LNCaP androgenic activity. Epiandrosterone is naturally prostate cells. produced by the enzyme 5α-reductase from the adrenal hormone DHEA. Purity: 99.71% Purity: >98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg Size: 10 mM × 1 mL, 1 g, 5 g Flutamide GLPG0492 (SCH 13521) Cat. No.: HY-B0022 Cat. No.: HY-18102 Flutamide is an antiandrogen drug, with its active GLPG0492 is a novel selective androgen receptor metablolite binding at androgen receptor with Ki modulator; exhibited anabolic activity on muscle, values of 55 nM, and primarily used to treat strongly dissociated from the androgenic activity prostate cancer. on prostate after oral dosing. Purity: 99.01% Purity: 99.66% Clinical Data: Launched Clinical Data: Phase 1 Size: 10 mM × 1 mL, 1 g, 5 g Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg GLPG0492 R enantiomer GSK-2881078 Cat. No.: HY-18102A Cat. No.: HY-100186 GLPG0492 R enantiomer is the R enantiomer of GSK 2881078 is a selective androgen receptor GLPG-0492, which is a novel selective androgen modulator potentially for the treatment of receptor modulator. cachexia. Purity: 99.51% Purity: 99.39% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg 4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Isosilybin B Leelamine hydrochloride Cat. No.: HY-N7045 Cat. No.: HY-110028 Isosilybin B, a flavonolignan isolated from Leelamine hydrochloride is a tricyclic diterpene silymarin, has anti-prostate cancer (PCA) activity molecule that is extracted from the bark of pine via inhibiting proliferation and inducing G1 phase trees.
Load more

Recommended publications
  • WADA Technical Letter – TL07 ANDARINE
    WADA Technical Letter – TL07 Document Number: TL07 Version Number: 3.0 Written by: WADA Science Approved by: WADA Executive Committee Reviewed by: WADA Laboratory Expert Group Date: 21 December 2020 Effective Date: 1 January 2021 ANDARINE - FLUTAMIDE 1.0 Introduction WADA wishes to draw the attention of the Laboratories to the following observations and instructions on the analysis and reporting of SARM S4 (Andarine) Metabolites O-dephenylandarine and O- dephenylandarine glucuronide. The andarine Metabolites O-dephenylandarine and of O-dephenylandarine glucuronide may also be present in a Sample as a Metabolite of the anti-androgen Flutamide (Drogenil®, Eulexin®, Euflex®, Flutamin®, Flugere®), used primarily in the treatment of prostate cancer [1]. Since flutamide is not a Prohibited Substance in sports, the Laboratories shall not report an Adverse Analytical Finding (AAF) for andarine based on the monitoring of O-dephenylandarine [2]. Figure 1. Proposed metabolic pathway of flutamide and andarine (adapted from Perrenoud et al. [1]). 2.0 Analysis and Reporting Requirements Report the result as an AAF for andarine only when the presence of andarine (parent compound), and/or its glucuronic acid conjugate, and/or its deacetylated and/or hydroxylated Metabolites, and/or its bishydroxylated product [2] are confirmed in the Sample (regardless of the presence of flutamide and/or its Metabolite 2-hydroxyflutamide); [Comment: Laboratories shall not report an AAF for andarine based only on the presence of O- dephenylandarine.] 3.0 References [1] Perrenoud L. et al. Risk of false positive results to SARM S4 in case of therapeutic use of antineoplastic/antiandrogen drug containing flutamide: a case study.
    [Show full text]
  • The 2021 List of Pharmacological Classes of Doping Agents and Doping Methods
    BGBl. III - Ausgegeben am 8. Jänner 2021 - Nr. 1 1 von 23 The 2021 list of pharmacological classes of doping agents and doping methods www.ris.bka.gv.at BGBl. III - Ausgegeben am 8. Jänner 2021 - Nr. 1 2 von 23 www.ris.bka.gv.at BGBl. III - Ausgegeben am 8. Jänner 2021 - Nr. 1 3 von 23 THE 2021 PROHIBITED LIST WORLD ANTI-DOPING CODE DATE OF ENTRY INTO FORCE 1 January 2021 Introduction The Prohibited List is a mandatory International Standard as part of the World Anti-Doping Program. The List is updated annually following an extensive consultation process facilitated by WADA. The effective date of the List is 1 January 2021. The official text of the Prohibited List shall be maintained by WADA and shall be published in English and French. In the event of any conflict between the English and French versions, the English version shall prevail. Below are some terms used in this List of Prohibited Substances and Prohibited Methods. Prohibited In-Competition Subject to a different period having been approved by WADA for a given sport, the In- Competition period shall in principle be the period commencing just before midnight (at 11:59 p.m.) on the day before a Competition in which the Athlete is scheduled to participate until the end of the Competition and the Sample collection process. Prohibited at all times This means that the substance or method is prohibited In- and Out-of-Competition as defined in the Code. Specified and non-Specified As per Article 4.2.2 of the World Anti-Doping Code, “for purposes of the application of Article 10, all Prohibited Substances shall be Specified Substances except as identified on the Prohibited List.
    [Show full text]
  • Selective Androgen Receptor Modulators: the Future of Androgen Therapy?
    148 Review Article Selective androgen receptor modulators: the future of androgen therapy? Andrew R. Christiansen1, Larry I. Lipshultz2,3, James M. Hotaling4, Alexander W. Pastuszak4 1University of Utah School of Medicine, Salt Lake City, UT, USA; 2Scott Department of Urology; 3Center for Reproductive Medicine, Baylor College of Medicine, Houston, TX, USA; 4Division of Urology, Department of Surgery, University of Utah School of Medicine, Salt Lake City, UT, USA Contributions: (I) Conception and design: AR Christiansen; (II) Administrative support: AW Pastuszak; (III) Provision of study material or patients: AR Christiansen; (IV) Collection and assembly of data: AR Christiansen; (V) Data analysis and interpretation: AR Christiansen; (VI) Manuscript writing: All authors; (VII) Final approval of manuscript: All authors. Correspondence to: Alexander W. Pastuszak, MD, PhD. Assistant Professor, Division of Urology, Department of Surgery, University of Utah School of Medicine, Salt Lake City, UT, USA. Email: [email protected]. Abstract: Selective androgen receptor modulators (SARMs) are small molecule drugs that function as either androgen receptor (AR) agonists or antagonists. Variability in AR regulatory proteins in target tissues permits SARMs to selectively elicit anabolic benefits while eschewing the pitfalls of traditional androgen therapy. SARMs have few side effects and excellent oral and transdermal bioavailability and may, therefore, represent viable alternatives to current androgen therapies. SARMs have been studied as possible therapies for many conditions, including osteoporosis, Alzheimer’s disease, breast cancer, stress urinary incontinence (SUI), prostate cancer (PCa), benign prostatic hyperplasia (BPH), male contraception, hypogonadism, Duchenne muscular dystrophy (DMD), and sarcopenia/muscle wasting/cancer cachexia. While there are no indications for SARMs currently approved by the Food and Drug Administration (FDA), many potential applications are still being explored, and results are promising.
    [Show full text]
  • Campro Catalog Stable Isotope
    Introduction & Welcome Dear Valued Customer, We are pleased to present to you our Stable Isotopes Catalog which contains more than three thousand (3000) high quality labeled compounds. You will find new additions that are beneficial for your research. Campro Scientific is proud to work together with Isotec, Inc. for the distribution and marketing of their stable isotopes. We have been working with Isotec for more than twenty years and know that their products meet the highest standard. Campro Scientific was founded in 1981 and we provide services to some of the most prestigious universities, research institutes and laboratories throughout Europe. We are a research-oriented company specialized in supporting the requirements of the scientific community. We are the exclusive distributor of some of the world’s leading producers of research chemicals, radioisotopes, stable isotopes and environmental standards. We understand the requirements of our customers, and work every day to fulfill them. In working with us you are guaranteed to receive: - Excellent customer service - High quality products - Dependable service - Efficient distribution The highly educated staff at Campro’s headquarters and sales office is ready to assist you with your questions and product requirements. Feel free to call us at any time. Sincerely, Dr. Ahmad Rajabi General Manager 180/280 = unlabeled 185/285 = 15N labeled 181/281 = double labeled (13C+15N, 13C+D, 15N+18O etc.) 186/286 = 12C labeled 182/282 = d labeled 187/287 = 17O labeled 183/283 = 13C labeleld 188/288 = 18O labeled 184/284 = 16O labeled, 14N labeled 189/289 = Noble Gases Table of Contents Ordering Information.................................................................................................. page 4 - 5 Packaging Information ..............................................................................................
    [Show full text]
  • Download Product Insert (PDF)
    Product Information Boldenone Cypionate Item No. 15158 CAS Registry No.: 106505-90-2 O Formal Name: 17β-hydroxy-androsta-1,4-dien-3-one O cyclopentanepropionate MF: C27H38O3 FW: 410.6 H Purity: ≥95% Stability: ≥2 years at -20°C H H Supplied as: A crystalline solid λ O UV/Vis.: max: 244 nm Laboratory Procedures For long term storage, we suggest that boldenone cypionate be stored as supplied at -20°C. It should be stable for at least two years. Boldenone cypionate is supplied as a crystalline solid. A stock solution may be made by dissolving the boldenone cypionate in the solvent of choice. Boldenone cypionate is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of boldenone cypionate in these solvents is approximately 15, 5, and 25 mg/ml, respectively. Boldenone cypionate is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, boldenone cypionate should first be dissolved in ethanol and then diluted with the aqueous buffer of choice. Boldenone cypionate has a solubility of approximately 0.3 mg/ml in a 1:2 solution of ethanol:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day. Boldenone is an anabolic androgenic steroid and synthetic derivative of testosterone that was originally developed for veterinary use.1 It can increase nitrogen retention, protein synthesis, and appetite, and also stimulates the release of erythropoietin in the kidneys.1 Boldenone cypionate was synthesized as an ester of boldenone in an attempt to alter boldenone’s very long half-life.2 Anabolic androgenic steroid compounds such as boldenone cypionate have been used illicitly by bodybuilders and other athletes.3 This compound is intended for forensic and research purposes only.
    [Show full text]
  • Novel Derivatives of Bio-Affecting Phenolic Compounds and Pharmaceutical Composition Containing Them
    Europaisches Patentamt European Patent Office © Publication number: 0046 270 A1 Office europeen des brevets ™ EUROPEAN PATENT APPLICATION @ Application number: 81106277.7 © Int. CI.3: C 07 C 103/78, C 07 C 93/26, C 07 C 69/24, C 07 C 1 53/07, @ Date of filing: 12.08.81 C07C 69/28 // C07C1 25/065 <§) Priority: 13.08.80 US 177825 © Applicant: INTERx RESEARCH CORPORATION, 2201 West 21 st Street, Lawrence Kansas 66044 (US) © I nventor : Bodor, Nicholas S., 31 5 Southwest 91 st Street, ® Dateofpublicationofapplication:24.02.82 S^^S^mHariMBM Bulletin m/b Terrace, Gainesville, Florida 32605 (US) Inventor: Pogany, Stefano A., 520 Louisiana Street, Lawrence Kansas 66044 (US) @ Designated Contracting States : AT BE CH DE FR GB IT ® Representative: Abitz, Walter, Dr.-lng. et al, Abitz, Mori, LI LU NL SE Gritschneder P.O. Box 86 01 09, D-8000 Munchen 86 (DE) Novel derivatives of bio-affecting phenolic compounds and pharmaceutical composition containing them. Novel@ Novel transient prodrug forms of bio-affecting phe- amyl, CH2ONO2,CH2ON02, -CH2OCOR2 or any non-heterocyclic nolic compounds are selected from the group consisting of member of the group defined by R2Rz above; and n.isn is at least those having the structural formula (I): one and equals the total number of phenolic hydroxyl functions comprising the non-steroidal bioaffecting phenol o etherified via a R2COXCH(R3)0-moiety; those having the structural formula (II): R2-C-X-CH-0- (I) I O R, II R2-C-X-CH-0- -RM-i-O-C-R2 (II) wherein X is O, S or NR5 wherein R5 is hydrogen or lower alkyl;alky!;
    [Show full text]
  • Customs Tariff - Schedule
    CUSTOMS TARIFF - SCHEDULE 99 - i Chapter 99 SPECIAL CLASSIFICATION PROVISIONS - COMMERCIAL Notes. 1. The provisions of this Chapter are not subject to the rule of specificity in General Interpretative Rule 3 (a). 2. Goods which may be classified under the provisions of Chapter 99, if also eligible for classification under the provisions of Chapter 98, shall be classified in Chapter 98. 3. Goods may be classified under a tariff item in this Chapter and be entitled to the Most-Favoured-Nation Tariff or a preferential tariff rate of customs duty under this Chapter that applies to those goods according to the tariff treatment applicable to their country of origin only after classification under a tariff item in Chapters 1 to 97 has been determined and the conditions of any Chapter 99 provision and any applicable regulations or orders in relation thereto have been met. 4. The words and expressions used in this Chapter have the same meaning as in Chapters 1 to 97. Issued January 1, 2020 99 - 1 CUSTOMS TARIFF - SCHEDULE Tariff Unit of MFN Applicable SS Description of Goods Item Meas. Tariff Preferential Tariffs 9901.00.00 Articles and materials for use in the manufacture or repair of the Free CCCT, LDCT, GPT, UST, following to be employed in commercial fishing or the commercial MT, MUST, CIAT, CT, harvesting of marine plants: CRT, IT, NT, SLT, PT, COLT, JT, PAT, HNT, Artificial bait; KRT, CEUT, UAT, CPTPT: Free Carapace measures; Cordage, fishing lines (including marlines), rope and twine, of a circumference not exceeding 38 mm; Devices for keeping nets open; Fish hooks; Fishing nets and netting; Jiggers; Line floats; Lobster traps; Lures; Marker buoys of any material excluding wood; Net floats; Scallop drag nets; Spat collectors and collector holders; Swivels.
    [Show full text]
  • Part I Biopharmaceuticals
    1 Part I Biopharmaceuticals Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 3 1 Analogs and Antagonists of Male Sex Hormones Robert W. Brueggemeier The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus, Ohio 43210, USA 1Introduction6 2 Historical 6 3 Endogenous Male Sex Hormones 7 3.1 Occurrence and Physiological Roles 7 3.2 Biosynthesis 8 3.3 Absorption and Distribution 12 3.4 Metabolism 13 3.4.1 Reductive Metabolism 14 3.4.2 Oxidative Metabolism 17 3.5 Mechanism of Action 19 4 Synthetic Androgens 24 4.1 Current Drugs on the Market 24 4.2 Therapeutic Uses and Bioassays 25 4.3 Structure–Activity Relationships for Steroidal Androgens 26 4.3.1 Early Modifications 26 4.3.2 Methylated Derivatives 26 4.3.3 Ester Derivatives 27 4.3.4 Halo Derivatives 27 4.3.5 Other Androgen Derivatives 28 4.3.6 Summary of Structure–Activity Relationships of Steroidal Androgens 28 4.4 Nonsteroidal Androgens, Selective Androgen Receptor Modulators (SARMs) 30 4.5 Absorption, Distribution, and Metabolism 31 4.6 Toxicities 32 Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 4 Analogs and Antagonists of Male Sex Hormones 5 Anabolic Agents 32 5.1 Current Drugs on the Market 32 5.2 Therapeutic Uses and Bioassays
    [Show full text]
  • CAS Number Index
    2334 CAS Number Index CAS # Page Name CAS # Page Name CAS # Page Name 50-00-0 905 Formaldehyde 56-81-5 967 Glycerol 61-90-5 1135 Leucine 50-02-2 596 Dexamethasone 56-85-9 963 Glutamine 62-44-2 1640 Phenacetin 50-06-6 1654 Phenobarbital 57-00-1 514 Creatine 62-46-4 1166 α-Lipoic acid 50-11-3 1288 Metharbital 57-22-7 2229 Vincristine 62-53-3 131 Aniline 50-12-4 1245 Mephenytoin 57-24-9 1950 Strychnine 62-73-7 626 Dichlorvos 50-23-7 1017 Hydrocortisone 57-27-2 1428 Morphine 63-05-8 127 Androstenedione 50-24-8 1739 Prednisolone 57-41-0 1672 Phenytoin 63-25-2 335 Carbaryl 50-29-3 569 DDT 57-42-1 1239 Meperidine 63-75-2 142 Arecoline 50-33-9 1666 Phenylbutazone 57-43-2 108 Amobarbital 64-04-0 1648 Phenethylamine 50-34-0 1770 Propantheline bromide 57-44-3 191 Barbital 64-13-1 1308 p-Methoxyamphetamine 50-35-1 2054 Thalidomide 57-47-6 1683 Physostigmine 64-17-5 784 Ethanol 50-36-2 497 Cocaine 57-53-4 1249 Meprobamate 64-18-6 909 Formic acid 50-37-3 1197 Lysergic acid diethylamide 57-55-6 1782 Propylene glycol 64-77-7 2104 Tolbutamide 50-44-2 1253 6-Mercaptopurine 57-66-9 1751 Probenecid 64-86-8 506 Colchicine 50-47-5 589 Desipramine 57-74-9 398 Chlordane 65-23-6 1802 Pyridoxine 50-48-6 103 Amitriptyline 57-92-1 1947 Streptomycin 65-29-2 931 Gallamine 50-49-7 1053 Imipramine 57-94-3 2179 Tubocurarine chloride 65-45-2 1888 Salicylamide 50-52-2 2071 Thioridazine 57-96-5 1966 Sulfinpyrazone 65-49-6 98 p-Aminosalicylic acid 50-53-3 426 Chlorpromazine 58-00-4 138 Apomorphine 66-76-2 632 Dicumarol 50-55-5 1841 Reserpine 58-05-9 1136 Leucovorin 66-79-5
    [Show full text]
  • Pharmacology on Your Palms CLASSIFICATION of the DRUGS
    Pharmacology on your palms CLASSIFICATION OF THE DRUGS DRUGS FROM DRUGS AFFECTING THE ORGANS CHEMOTHERAPEUTIC DIFFERENT DRUGS AFFECTING THE NERVOUS SYSTEM AND TISSUES DRUGS PHARMACOLOGICAL GROUPS Drugs affecting peripheral Antitumor drugs Drugs affecting the cardiovascular Antimicrobial, antiviral, Drugs affecting the nervous system Antiallergic drugs system antiparasitic drugs central nervous system Drugs affecting the sensory Antidotes nerve endings Cardiac glycosides Antibiotics CNS DEPRESSANTS (AFFECTING THE Antihypertensive drugs Sulfonamides Analgesics (opioid, AFFERENT INNERVATION) Antianginal drugs Antituberculous drugs analgesics-antipyretics, Antiarrhythmic drugs Antihelminthic drugs NSAIDs) Local anaesthetics Antihyperlipidemic drugs Antifungal drugs Sedative and hypnotic Coating drugs Spasmolytics Antiviral drugs drugs Adsorbents Drugs affecting the excretory system Antimalarial drugs Tranquilizers Astringents Diuretics Antisyphilitic drugs Neuroleptics Expectorants Drugs affecting the hemopoietic system Antiseptics Anticonvulsants Irritant drugs Drugs affecting blood coagulation Disinfectants Antiparkinsonian drugs Drugs affecting peripheral Drugs affecting erythro- and leukopoiesis General anaesthetics neurotransmitter processes Drugs affecting the digestive system CNS STIMULANTS (AFFECTING THE Anorectic drugs Psychomotor stimulants EFFERENT PART OF THE Bitter stuffs. Drugs for replacement therapy Analeptics NERVOUS SYSTEM) Antiacid drugs Antidepressants Direct-acting-cholinomimetics Antiulcer drugs Nootropics (Cognitive
    [Show full text]
  • Androgenic-Anabolic Steroid (Boldenone)
    Genera of l P l r a a n c r t u i c o e J Kalmanovich et al., J Gen Pract 2014, 2:3 Journal of General Practice DOI: 10.4172/2329-9126.1000153 ISSN: 2329-9126 Case Report Open Access Androgenic-Anabolic Steroid (Boldenone) Abuse as a Cause of Dilated Cardiomyopathy Eran Kalmanovich*, Sa'ar Minha, Marina Leitman, Zvi Vered and Alex Blatt Assaf Harofeh Medical Center, Aviv University, Israel *Corresponding author: Eran Kalmanovich, Department of Cardiology, Assaf Harofeh Medical Center, Zerifin, Sackler School of Medicine, Tel Aviv University, Israel, Tel: +972-50-5191121; E-mail: [email protected] Received date: Feb 27, 2014, Accepted date: Mar 27, 2014, Published date: Apr 3, 2014 Copyright: © 2014 Kalmanovich E, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Case Presentation At admission 1-year follow up A 34-year old, previously healthy male, presented to the ER with EF% 20% 40% worsening dyspnea over a period of three weeks and the appearance of blood tinged sputum. Soon after presentation, the patient was LA diameter (mm) 3.9 3.8 hypoxemic and required mechanical ventilation. Chest X-ray LA area (cm2) 14.0 20 demonstrated bilateral infiltrates and he was admitted to the ICU with the tentative diagnosis of acute respiratory distress syndrome. LVEDD (cm) 6.1 5.6 Investigation by PICCO, Suggested the presence of heart failure were LVESD (cm) 5.1 3.3 and the patient was transferred to the ICCU.
    [Show full text]
  • WO 2018/190970 Al 18 October 2018 (18.10.2018) W !P O PCT
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2018/190970 Al 18 October 2018 (18.10.2018) W !P O PCT (51) International Patent Classification: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, CI2Q 1/32 (2006.01) UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (21) International Application Number: EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, PCT/US2018/021 109 MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (22) International Filing Date: TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, 06 March 2018 (06.03.2018) KM, ML, MR, NE, SN, TD, TG). (25) Filing Language: English Declarations under Rule 4.17: (26) Publication Langi English — as to applicant's entitlement to apply for and be granted a patent (Rule 4.1 7(H)) (30) Priority Data: — as to the applicant's entitlement to claim the priority of the 62/484,141 11 April 2017 ( 11.04.2017) US earlier application (Rule 4.17(Hi)) (71) Applicant: REGENERON PHARMACEUTICALS, Published: INC. [US/US]; 777 Old Saw Mill River Road, Tarrytown, — with international search report (Art. 21(3)) New York 10591-6707 (US). — with sequence listing part of description (Rule 5.2(a)) (72) Inventors: STEVIS, Panayiotis; 777 Old Saw Mill Riv er Road, Tarrytown, New York 10591-6707 (US).
    [Show full text]