Neurosteroid Analogues. 16. A New Explanation for the Lack of Anesthetic Effects of Δ16-Alphaxalone and Identification of a Δ17(20) Analogue with Potent Anesthetic Activity

Eva Stastna; Kathiresan Krishnan; Brad D. Manion; Amanda Taylor; Nigam P. Rath; Zi-Wei Chen; Alex. S. Evers; Charles F. Zorumski; Steven Mennerick; Douglas F. Covey

doi:10.1021/jm2002487

Neurosteroid Analogues. 16. A New Explanation for the Lack of Anesthetic Effects of Δ16-Alphaxalone and Identification of a Δ17(20) Analogue with Potent Anesthetic Activity

Eva Stastna
, Kathiresan Krishnan
, Brad D. Manion
, Amanda Taylor
, Nigam P. Rath
, Zi-Wei Chen
, Alex. S. Evers
, Charles F. Zorumski
, Steven Mennerick
, Douglas F. Covey

University of Missouri-St. Louis

Research output: Contribution to journal › Article › peer-review

Original language	American English
Journal	Journal of Medicinal Chemistry
Volume	54
DOIs	https://doi.org/10.1021/jm2002487
State	Published - Jun 9 2011

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Biochemistry

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Stastna, E., Krishnan, K., Manion, B. D., Taylor, A., Rath, N. P., Chen, Z.-W., Evers, A. S., Zorumski, C. F., Mennerick, S., & Covey, D. F. (2011). Neurosteroid Analogues. 16. A New Explanation for the Lack of Anesthetic Effects of Δ16-Alphaxalone and Identification of a Δ17(20) Analogue with Potent Anesthetic Activity. Journal of Medicinal Chemistry, 54. https://doi.org/10.1021/jm2002487

Stastna, E, Krishnan, K, Manion, BD, Taylor, A , Rath, NP, Chen, Z-W, Evers, AS, Zorumski, CF, Mennerick, S & Covey, DF 2011, 'Neurosteroid Analogues. 16. A New Explanation for the Lack of Anesthetic Effects of Δ16-Alphaxalone and Identification of a Δ17(20) Analogue with Potent Anesthetic Activity', Journal of Medicinal Chemistry, vol. 54. https://doi.org/10.1021/jm2002487

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title = "Neurosteroid Analogues. 16. A New Explanation for the Lack of Anesthetic Effects of Δ16-Alphaxalone and Identification of a Δ17(20) Analogue with Potent Anesthetic Activity",

author = "Eva Stastna and Kathiresan Krishnan and Manion, \{Brad D.\} and Amanda Taylor and Rath, \{Nigam P.\} and Zi-Wei Chen and Evers, \{Alex. S.\} and Zorumski, \{Charles F.\} and Steven Mennerick and Covey, \{Douglas F.\}",

note = "This study addresses the hypothesis that the lack of anesthetic activity for (3α,5α)-3-hydroxypregn-16-ene-11,20-dione (Δ 16-alphaxalone) is explained by the steroid Δ 16 double bond constraining the steroid 20-carbonyl group to a position that prevents it from favorably interacting with γ-aminobutyric acid type A (GABA A) receptors.",

year = "2011",

month = jun,

day = "9",

doi = "10.1021/jm2002487",

language = "American English",

volume = "54",

journal = "Journal of Medicinal Chemistry",

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T1 - Neurosteroid Analogues. 16. A New Explanation for the Lack of Anesthetic Effects of Δ16-Alphaxalone and Identification of a Δ17(20) Analogue with Potent Anesthetic Activity

AU - Stastna, Eva

AU - Krishnan, Kathiresan

AU - Manion, Brad D.

AU - Taylor, Amanda

AU - Rath, Nigam P.

AU - Chen, Zi-Wei

AU - Evers, Alex. S.

AU - Zorumski, Charles F.

AU - Mennerick, Steven

AU - Covey, Douglas F.

N1 - This study addresses the hypothesis that the lack of anesthetic activity for (3α,5α)-3-hydroxypregn-16-ene-11,20-dione (Δ 16-alphaxalone) is explained by the steroid Δ 16 double bond constraining the steroid 20-carbonyl group to a position that prevents it from favorably interacting with γ-aminobutyric acid type A (GABA A) receptors.

PY - 2011/6/9

Y1 - 2011/6/9

UR - https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3794474/

U2 - 10.1021/jm2002487

DO - 10.1021/jm2002487

M3 - Article

VL - 54

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

ER -

Neurosteroid Analogues. 16. A New Explanation for the Lack of Anesthetic Effects of Δ16-Alphaxalone and Identification of a Δ17(20) Analogue with Potent Anesthetic Activity

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