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STIMULATION OF UTERINE RNA SYNTHESIS IN MICE BY THE POST-COITAL ANTIFERTILITY AGENT, ORF 3858

Ortho Research Foundation, Raritan, New Jersey 08869, U.S.A.

(Received 18th March 1975)

Oestrogens, according to Emmens & Miller (1969), may be pharmacologically categorized into three classes: (1) compounds which occupy receptor sites and thereby elicit immediate physiological responses, (2) compounds which weakly or briefly occupy receptors and therefore result in impeded responses, and (3) pro-oestrogens, compounds which must undergo metabolic transformation in order to elicit oestrogenic responses.

The compound 2-methyl-3-ethyl-4-phenyl-4-cylohexene carboxylic acid (ORF 3858) is non-steroidal and has post-coital antifertility and oestrogenic properties (Blye & Homm, 1967; Blye, 1970). During studies of the mechanism of the antifertility activity of this compound, two interesting experimental observations were made. First, when metabolic transformation of ORF 3858 to a p-hydroxylated form was inhibited, the antifertility activity of the compound was lost (Yard et al., 1969). Second, ORF 3858 was found not to bind to uterine cytosol oestrogen receptors, whereas the p-hydroxylated