RELATIVE EFFECTIVENESS OF VARIOUS STEROIDS IN AN ANDROGEN ASSAY USING THE EXORBITAL LACRIMAL GLAND OF THE CASTRATED RAT.

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Abstract
The morphological transforma-tion of the exorbital lacrimal gland of the castrated rat following subcutaneous injection of steroids, described in detail in the preceding paper, was employed as the end-point of androgenic activity. The relative effectiveness of androsterone and of 13 derivatives of the 5a-androstane series was then determined using testosterone as reference standard. Androsterone proved one-half as active as the standard; 5a-androstan-17[beta]-ol, 5[alpha]a-androstane-3[alpha], 3[beta]7[beta]-diol and 5a-androst-l-ene-3, 17-dione were much less active, whereas 5[alpha]-andro-stane-3[alpha], 17[beta]-diol was 3 times as potent as testosterone. Introduction of a conjugated double bond at C 1, 2 of 17[beta]-hydroxy-5[alpha]-androstan-3-one produced a four-fold increase of activity from a level a little lower than that of testosterone; a further increase in androgenicity was obtained on methyl substitution at C 1 of the [DELTA]1-5[alpha]-isomer of testosterone. Esterification consistently increased the activities of the 5[alpha]-androstane derivatives tested.