Structure-activity relationships in steroidal anaesthetics

doi:10.1016/0022-4731(75)90041-2

Journal of Steroid Biochemistry

Volume 6, Issue 5, May 1975, Pages 607-613

https://doi.org/10.1016/0022-4731(75)90041-2 Get rights and content

Abstract

Many steroids have been shown to possess anaesthetic activity and the properties which led to the selection of a mixture of 3α-hydroxy-5α-pregnane-11,20-dione (Alphaxalone) and 21-acetoxy-3α-hydroxy-5α-pregnane-11, 20-dione for clinical use are described. Further studies have revealed that the introduction of double bonds and substituents into Alphaxalone modify its anaesthetic activity, as determined in mice, and these modifications are discussed with particular reference to the conformation of the A-ring. A variety of side chains may be present at the 17β-position. Some water-soluble steroids which show instantaneous induction of anaesthesia are described.

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Structure-activity relationships in steroidal anaesthetics

Abstract

Postgrad. med. J.

Endocrinology

Science N.Y.

J. Pharmac. exp. Ther.

J. Pharmac. exp. Ther.

Z. Vit. Horm. Ferm.

J. med. Chem.