Literature DB >> 17710

Determination of aqueous solubility and pKa values of estrogens.

A R Hurwitz, S T Liu.   

Abstract

Reported estrone pKa and solubility data show wide variation. Improved experimental procedures were designed and used to obtain reproducible results. The pKa values for several estrogens and related compounds also were determined to assess the effects of structural differences on ionization. No evidence was obtained for long-range D to A ring electronic transmission affecting pKa. Significant differences in pKa values resulted only when conjugated unsaturation was added into the B ring of estrone or estradiol. The aqueous solubilities of estrone and 17alpha-estradiol were 0.8 and 3.9 microgram/ml, respectively, at 25degrees.

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Year:  1977        PMID： 17710     DOI： 10.1002/jps.2600660504

Source DB:  PubMed          Journal:  J Pharm Sci        ISSN： 0022-3549            Impact factor:   3.534


  10 in total

1.  Physicochemical characterization of NPC 1161C, a novel antimalarial 8-aminoquinoline, in solution and solid state.

Authors:  Asish Kumar Dutta; Steven P Stodghill; Christy M Wyandt
Journal:  AAPS PharmSciTech       Date:  2010-12-30       Impact factor: 3.246

2.  Simultaneous measurement of total estradiol and testosterone in human serum by isotope dilution liquid chromatography tandem mass spectrometry.

Authors:  Hui Zhou; Yuesong Wang; Matthew Gatcombe; Jacob Farris; Julianne C Botelho; Samuel P Caudill; Hubert W Vesper
Journal:  Anal Bioanal Chem       Date:  2017-08-11       Impact factor: 4.142

3.  Evaluation of an Isotope Dilution HPLC Tandem Mass Spectrometry Candidate Reference Measurement Procedure for Total 17-β Estradiol in Human Serum.

Authors:  Julianne Cook Botelho; Ashley Ribera; Hans C Cooper; Hubert W Vesper
Journal:  Anal Chem       Date:  2016-10-27       Impact factor: 6.986

4.  The Conformations of 17β-Estradiol (E2) and 17α-Estradiol as Determined by Solution NMR.

Authors:  Jianxin Guo; Richard I Duclos; V Kiran Vemuri; Alexandros Makriyannis
Journal:  Tetrahedron Lett       Date:  2010-07-07       Impact factor: 2.415

5.  Aqueous and cosolvent solubility data for drug-like organic compounds.

Authors:  Erik Rytting; Kimberley A Lentz; Xue-Qing Chen; Feng Qian; Srini Vakatesh
Journal:  AAPS J       Date:  2005-04-26       Impact factor: 4.009

6.  Prediction of Membrane Permeation of Drug Molecules by Combining an Implicit Membrane Model with Machine Learning.

Authors:  Stephanie A Brocke; Alexandra Degen; Alexander D MacKerell; Bercem Dutagaci; Michael Feig
Journal:  J Chem Inf Model       Date:  2018-12-27       Impact factor: 4.956

7.  Non-genomic mechanism of 17 beta-oestradiol-induced inhibition of contraction in mammalian vascular smooth muscle.

Authors:  T Kitazawa; E Hamada; K Kitazawa; A K Gaznabi
Journal:  J Physiol       Date:  1997-03-01       Impact factor: 5.182

8.  Mobilization of endocrine-disrupting chemicals and estrogenic activity in simulated rainfall runoff from land-applied biosolids.

Authors:  Ben D Giudice; Thomas M Young
Journal:  Environ Toxicol Chem       Date:  2011-08-22       Impact factor: 3.742

9.  The prodrug DHED selectively delivers 17β-estradiol to the brain for treating estrogen-responsive disorders.

Authors:  Laszlo Prokai; Vien Nguyen; Szabolcs Szarka; Puja Garg; Gauri Sabnis; Heather A Bimonte-Nelson; Katie J McLaughlin; Joshua S Talboom; Cheryl D Conrad; Paul J Shughrue; Todd D Gould; Angela Brodie; Istvan Merchenthaler; Peter Koulen; Katalin Prokai-Tatrai
Journal:  Sci Transl Med       Date:  2015-07-22       Impact factor: 17.956

10.  Quantitative Assessment of Levonorgestrel Binding Partner Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling.

Authors:  Brian Cicali; Karthik Lingineni; Rodrigo Cristofoletti; Thomas Wendl; Joachim Hoechel; Herbert Wiesinger; Ayyappa Chaturvedula; Valvanera Vozmediano; Stephan Schmidt
Journal:  CPT Pharmacometrics Syst Pharmacol       Date:  2020-12-13
  10 in total

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