Breakthroughs in neuroactive steroid drug discovery.
Blanco MJ, La D, Coughlin Q, Newman CA, Griffin AM, Harrison BL, Salituro FG.
Bioorg Med Chem Lett · review; journal article · DOI 10.1016/j.bmcl.2017.11.043 PUBLIKATIONSREGISTRET
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17 träffarThe development of benzo- and naphtho-fused quinoline-2,4-dicarboxylic acids as vesicular glutamate transporter (VGLUT) inhibitors reveals a possible role for neuroactive steroids.
Carrigan CN, Patel SA, Cox HD, Bolstad ES, Gerdes JM, Smith WE, Bridges RJ, Thompson CM.
Bioorg Med Chem Lett · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2013.12.086Factorizing the role of a critical leucine residue in the binding of substrate to human 20alpha-hydroxysteroid dehydrogenase (AKR1C1): molecular modeling and kinetic studies of the Leu308Val mutant enzyme.
Dhagat U, Endo S, Soda M, Hara A, El-Kabbani O.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2010.06.137Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Obach RS, Lombardo F, Waters NJ.
Drug Metab Dispos · journal article · DOI 10.1124/dmd.108.020479Synthesis and GABA(A) receptor activity of oxygen-bridged neurosteroid analogs.
Alvarez LD, Veleiro AS, Baggio RF, Garland MT, Edelsztein VC, Coirini H, Burton G.
Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2008.01.048Neurosteroid analogues. 12. Potent enhancement of GABA-mediated chloride currents at GABAA receptors by ent-androgens.
Katona BW, Krishnan K, Cai ZY, Manion BD, Benz A, Taylor A, Evers AS, Zorumski CF, Mennerick S, Covey DF.
Eur J Med Chem · research support, non-u.s. gov't; journal article; research support, n.i.h., extramural · DOI 10.1016/j.ejmech.2007.02.017Neurosteroid analogues. 11. Alternative ring system scaffolds: gamma-aminobutyric acid receptor modulation and anesthetic actions of benz[f]indenes.
Scaglione JB, Manion BD, Benz A, Taylor A, DeKoster GT, Rath NP, Evers AS, Zorumski CF, Mennerick S, Covey DF.
J Med Chem · research support, non-u.s. gov't; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/jm0602920Activity of B-nor analogues of neurosteroids on the GABA(A) receptor in primary neuronal cultures.
Suñol C, García DA, Bujons J, Kristofíková Z, Matyás L, Babot Z, Kasal A.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm060002fNeurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (3alpha,5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one.
Zeng CM, Manion BD, Benz A, Evers AS, Zorumski CF, Mennerick S, Covey DF.
J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm049027+[Drug-induced liver injury; fourteenth updated edition of the bibliographic database of liver injuries and related drugs].
Biour M, Ben Salem C, Chazouillères O, Grangé JD, Serfaty L, Poupon R.
Gastroenterol Clin Biol · bibliography; journal article · DOI 10.1016/s0399-8320(04)95062-2Neurosteroid analogues. 9. Conformationally constrained pregnanes: structure-activity studies of 13,24-cyclo-18,21-dinorcholane analogues of the GABA modulatory and anesthetic steroids (3alpha,5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one.
Jiang X, Manion BD, Benz A, Rath NP, Evers AS, Zorumski CF, Mennerick S, Covey DF.
J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/jm030302mConformationally constrained anesthetic steroids that modulate GABA(A) receptors.
Anderson A, Boyd AC, Clark JK, Fielding L, Gemmell DK, Hamilton NM, Maidment MS, May V, McGuire R, McPhail P, Sansbury FH, Sundaram H, Taylor R.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm000977eNeurosteroid analogues. 8. Structure-activity studies of N-acylated 17a-aza-D-homosteroid analogues of the anesthetic steroids (3alpha, 5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one.
Covey DF, Han M, Kumar AS, de La Cruz MA, Meadows ES, Hu Y, Tonnies A, Nathan D, Coleman M, Benz A, Evers AS, Zorumski CF, Mennerick S.
J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm0002477Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
Tukey RH, Strassburg CP.
Annu Rev Pharmacol Toxicol · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; review; journal article · DOI 10.1146/annurev.pharmtox.40.1.581Anesthetic activity of novel water-soluble 2 beta-morpholinyl steroids and their modulatory effects at GABAA receptors.
Anderson A, Boyd AC, Byford A, Campbell AC, Gemmell DK, Hamilton NM, Hill DR, Hill-Venning C, Lambert JJ, Maidment MS, May V, Marshall RJ, Peters JA, Rees DC, Stevenson D, Sundaram H.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm960733nSynthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.
Hogenkamp DJ, Tahir SH, Hawkinson JE, Upasani RB, Alauddin M, Kimbrough CL, Acosta-Burruel M, Whittemore ER, Woodward RM, Lan NC, Gee KW, Bolger MB.
J Med Chem · journal article · DOI 10.1021/jm960021xNeurosteroid analogues. 4. The effect of methyl substitution at the C-5 and C-10 positions of neurosteroids on electrophysiological activity at GABAA receptors.
Han M, Zorumski CF, Covey DF.
J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm960304p