Grootenhuis M de Gooyer J van der Louw R Bursi and D Leysen

Contents

22.1

Introduction

22.2

Synthesis of nandrolone derivatives and reference steroids

22.2.1

Preparation of nandrolone, MENT and reference steroids

22.2.2

Preparation of nandrolone derivatives

22.3

Methods of pharmacological evaluation

22.3.1

Androgen receptor transactivation and binding

22.3.2

Determination of metabolic stability with human hepatocytes

22.3.3

Aromatase susceptibility of new androgens

22.3.4

Effects on bone, LH/FSH, ventral prostate and muscle in castrated male rats

22.3.5

Effects on plasma testosterone of intact male monkeys

22.3.6

Pharmacokinetic evaluation in different animals

22.4

Pharmacological profile

22.4.1

Androgen receptor binding and transactivation

22.4.2

Metabolic stability in human hepatocytes

22.4.3

Susceptibility for human aromatase

22.4.4

Efficacy in castrated rats: effects on bone, LH/FSH, ventral prostate

and muscle

22.4.5

Efficacy in intact monkeys: effects on serum testosterone

22.4.6

Pharmacokinetic evaluation in different species

22.5

Interpretation of results

22.6

Key messages

22.7

References

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