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C. W. EMMENS

Summary.

Mated female rabbits were injected subcutaneously on Days 5 to 7 or 7 to 9 of pregnancy with various substances in nut oil, and examined on Days 9 to 11. Approximately 50% failure of normal implantation was caused by 30 μg of oestradiol, 25 mg of dimethylstilboestrol or 10 mg of 17-ethinyl-19-nortestosterone daily. mer 25 in doses of up to 25 mg, and 17-ethyl-19-nortestosterone in doses of up to 10 mg daily were ineffective.

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C. W. EMMENS

Summary.

The activities of twelve steroids and fifteen non-steroids are reported for tests in mice of oestrogenic and anti-oestrogenic activity (vaginal smear) and antifertility activity (administration in early pregnancy). No steroid, with the possible exception of 17α-(2'-methallyl)-9β,10α-androst-4-en-17-ol-3-one (SAP 104), had antifertility effects not explained by its oestrogenic activity. Among the non-steroids, mesoα,α'-dimethyl-4,4'-dihydroxybibenzyl (meso-dma), 1 - [p- (2-diethylaminoethoxy) phenyl]-2-(p-methoxyphenyl)-1-phenylethane (MRL 37) and possibly 1-[p-(2-diethylaminoethoxy)phenyl]-2-(p-methoxyphenyl)1-phenylethanol (MER 25) may have antifertility effects unrelated or incompletely related to oestrogenic activity and possibly related to antioestrogenic activity.

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C. W. EMMENS

Summary.

The postcoital antifertility activity of a series of triarylalkenes and triarylalkanols with basic ether groups has been examined in mice and rats. The triarylalkenes were, in general, more potent than the others, and more potent orally than by injection. Apart from having a greater sensitivity than the mouse, the rat appears to give essentially the same information about relative potency and oestrogenic properties. Most compounds examined were weak to very weak oestrogens of an `impeded' type, not antioestrogenic in conventional tests, and many had a much higher antifertility potency than could be expected from their oestrogenic activity. The general pattern of results suggests that preimplantation rather than postimplantation stages are affected, or more readily affected. The most potent compound examined (4h) was effective in the mouse at an injected ED50 of 14μg/kg/day after coitus, with an oestrogenic (vaginal smear) ED50 of 250 times that dose. Several other compounds were effective at a dosage around 70 μg/kg/day.

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C. W. EMMENS

Summary.

Various triarylalkene derivatives which are weakly oestrogenic and not antioestrogenic at any dosage in conventional tests in mice and rats cause refractoriness to oestradiol for several weeks after injection in vaginal smear tests.

The same compounds, administered in a single injection of 1 mg before mating, caused complete sterility for up to several weeks, although mating still occurred, sometimes at a slower rate than in controls. Daily injections of effective doses (5 to 50 μg) produced similar effects, but reduced mating frequencies more severely.

Oral administration was not followed by refractoriness to oestradiol. When a single dose of 1 mg was fed however, mating was normal but fertility was reduced by up to 85 % compared with controls. Daily oral dosing in the vehicle used (50% aqueous propylene glycol) or even of the vehicle alone upset the animals and reduced both mating and fertility.

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C. W. EMMENS and L. MARTIN

Summary.

U-11100A is oestrogenic in vaginal smear tests in rats and mice with a subcutaneous med of ca. 500 μg and 50 to 100 μg respectively. It is also oestrogenic orally and intravaginally and in the tetrazolium reduction test. In all tests, however, the dose-response line turns down again with higher dosage, and full responses were not obtained at the highest dose levels tested. The compound is weakly anti-oestrogenic in both vaginal smear and tetrazolium tests in mice, but exhibits complex interactions with oestradiol, the oestrogen used.

U-11100A has an antifertility action when injected on Days 1 to 3 or 4 to 6 of pregnancy in the mouse, 50 μg/day being effective on either schedule. It is felt that this is an expression of its oestrogenicity.

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C. W. EMMENS and W. L. CARR

Summary.

Groups of twenty female QS-strain mice were injected with a single dose of 0, 1, 3 or 9 mg of the triarylalkene H-774. Males were introduced 3, 30 or 60 days after injection. Mating was not greatly affected, but very few females mating within the first 23 days after injection became pregnant. At 30 days, fertility varied from 62% (1-mg dose) to 17% (9-mg dose) of that in controls. At 60 days, it was substantially back to normal but the numbers/litter were still lower than in controls. In females receiving the same oral doses, fertility was initially as severely affected, but recovery was more rapid.

Further groups of mice were injected with single doses of 0, 2 or 5 mg of the closely related compound, H-1076, vaginal smears were taken daily from some, and others were killed at varying periods between 3 and 119 days afterwards. Some were allowed to mate, others were not. In unmated mice, initial responses were oestrogenic in the uterus and vagina, and oestrous cycles were lengthened at first but later reverted to normal. In the uterus, the glands started to enlarge by Day 7 and proceeded to maximal distention by Day 63. Later, they deflated and five out of six uteri appeared normal by Day 119. In the ovaries, follicles appeared normal in size and numbers, but corpora lutea were few and appeared degenerate. Mating was followed by pregnancy after the 2-mg injections in much the same pattern as with H-774, despite the uterine abnormalities, but only three out of eighteen females became pregnant after 5-mg injections. Implantation numbers and weights were affected in some mice.

These results suggest a lack of progesterone, with little effect on oestrogen production, mediated through reduced ovulation rates and reduced production of progesterone from such corpora lutea as were formed. It is postulated that these compounds may inhibit LH release and/or production.

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K. W. HUMPHREY and C. W. EMMENS

Summary.

The effects of erythro-MEA (erythro-ethyl-α′-methyl-4,4′dihydroxybibenzyl) on tubal transport and implantation in the mouse were studied. When given on Days 1 to 3 of pregnancy, erythro-MEA causes tube-locking of some ova, reduces the recovery of ova to 60% of that in controls, and has similar effects to oestradiol. Treatment with this compound inhibits the deciduoma reaction and implantation of transferred ova in pseudopregnant and progesterone-treated, ovariectomized mice. When given to mice with delayed blastocysts, erythro-MEA induces implantation in 50% of mice and prevents oestradiol-induced implantation in others. In this system, erythro-MEA has both oestrogenic and antioestrogenic properties, but it is concluded that its anti-fertility actions may, in part, be due to its anti-oestrogenic property.

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C. W. EMMENS and C. A. FINN

Summary.

In the mouse, a variety of oestrogens and anti-oestrogens given by a single injection on the 4th day of pregnancy inhibit implantation. Local administration to a segment of one horn of the uterus caused inhibition with lower dosage levels than were required by subcutaneous injection, but this was never confined to the segment or horn so treated.

In the rat, similar phenomena were seen with dimethylstilboestrol and oestradiol, but the locally effective dose of the former equalled the parenteral dose.

No dose-response relationship was found for progesterone or ethyl19-nortestosterone by either route used.

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I. C. A. MARTIN and C. W. EMMENS

Summary.

Four treatment methods for the preparation of deep-frozen bull semen were tested for fertility in a factorial design involving the artificial insemination of 1728 first-service cows with the following results :

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of non-returns to service at 3 months, with equal treatment groups of 432 cows. The improvement in fertility after equilibration in the presence of fructose was highly significant (P < 0·01), but not in its absence, when fertility was depressed even in equilibrated semen.

There was a higher revival rate of spermatozoa after the longer period of equilibration and the use of fructose in the diluent significantly improved the percentage of motile spermatozoa after thawing.

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C. W. EMMENS, B. G. MILLER and W. H. OWEN

Summary.

U-11555A is oestrogenic in vaginal smear tests in mice with a low slope and a subcutaneous med of not less than 5 mg. Its oestrogenic activity intravaginally was not fully investigated, but is not high. It is weakly anti-oestrogenic in similar tests, with an med against oestradiol of about 200 μg subcutaneously, perhaps a little lower intravaginally. No interactions were seen as they were with U-11100A† (Emmens & Martin, 1965).

U-11555A has an antifertility action in the mouse when injected on Days 1 to 3 or 4 to 6 of pregnancy, with meds of about 100 μg (Days 1 to 3) and 300μg (Days 4 to 6). In rats, U-11555A has a constant subcutaneous or oral med on Days 1 to 3 or 4 to 6 of about 400 μg. In simultaneous tests in rats, U-11100A had meds of about 20 μg (Days 1 to 3) and 60 μg (Days 4 to 6) and was significantly more potent orally than by injection.

From these results, the antifertility action of U-11555A can hardly be attributed to oestrogenic properties, as was that of U-11100A by Emmens & Martin (1965), and its action profile is not very similar to that of the latter. Its antifertility action in mice is in accord with its anti-oestrogenic potency in that species.