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PubMed1982

[Synthetic inhibitors of serine proteinases. Part 26: Inhibition of trypsin, plasmin and thrombin by amides of N alpha-arylsulfonylated 2-amino-4-(4-amidino-phenyl) butyric acid and 2-amino-5-amidinophenyl valeric acids (author's transl)].

Among the derivatives of the N alpha-arylsulfonylated omega-amidinophenyl-alpha-aminoalkyl carboxylic acids, the primary amides of N alpha-arylsulfonylated 2-amino-4-(4-amidinophenyl) butyric acid proved to be compounds with strong antiplasmin and antitrypsin activity, they exert, however, only slight inhibitory effect on thrombin. So far, no benzamidine derivatives with strong inhibitory effects on plasmin but with weak antithrombin activity have been known. The secondary amides of the N alpha-arylsulfonylated 2-amino-4-(4-amidinophenyl)butyric acid possess slight inhibitory effects, the corresponding derivatives of 2-amino-5-amidinophenyl valeric acids, however, are potent inhibitors of thrombin.

Amidines↗
PubMed1978

Antitumor activity of N-trifuloroacetyladriamycin-14-valerate.

The antitumor activity and toxicity of N-trifluoroacetyladriamycin-14-valerate (AD 32) dissolved in 10% Tween 80 in distilled water were compared to those of adriamycin dissolved in distilled water in 10% Tween 80 in distilled water, in mice bearing L1210 leukemia, P388 leukemia, Gross leukemia, and solid Sarcoma 180. Treatments were performed ip or iv according to different schedules. The antitumor-activity of AD 32 was not superior to that of adriamycin. The antitumor activity of adriamycin dissolved in aqueous solution of Tween 80 was higher than that of adriamycin dissolved in distilled water after after iv treatment.

Animals↗
PubMed1978

Comparative antineoplastic activity of adriamycin and N-trifluoroacetyladriamycin-14-valerate.

A comparative investigation of the antineoplastic activity of adriamycin and its derivative, N-trifluoroacetyladriamycin-14-valerate (AD 32), was conducted in murine tumor models employing different treatment schedules and injection routes. In all conditions tested, ie, ascitic and disseminated L1210 leukemia, ascitic LSTRA lymphoma, and advanced Lewis lung carcinoma, AD 32 was significantly more effective in terms of lifespan prolongation and induction of cures than optimal adriamycin treatments. As with adriamycin, AD 32 was ineffective on ic transplanted L1210 leukemia.

Animals↗
PubMed1983

[Biologic availability of diflucortolone-21-valerate in human skin].

The concentration of diflucortolone-21-valerate (DFV) in the different layers of human skin was investigated after topical application of Nerisona (0.1%) as a function of the formulation (fatty ointment, ointment and creme), of the duration of exposition and of the condition of the skin. From all galenic formulations DFV penetrated rapidly into the horny layer. Mean highest concentrations were determined 4 h after application with approx. 300 micrograms/ml (ca. 600 mumol/l) after treatment with fatty ointment and ointment and with approx. 500 micrograms/ml (ca. 1000 mumol/l) after treatment with the cream. The corticoid concentration decreased in the horny layer from distal to proximal by 1.5 to 2 decades. After application to damaged skin - as a model for diseased skin - the local corticoid concentrations in all skin layers were distinctly higher than after application to intact skin at all time points investigated. DFV penetrates selectively into the damaged skin. The systemic load caused by percutaneous absorption through intact skin is neglectable.

Adult↗
PubMed1980

Effect of azathioprine on antibody formation in mice and its modification by delta-(2-amino-6-hydroxy-3,4-dihydro-4-oxo-5-pyrimidinyl)-valeric acid.

The effects of azathioprine, either alone or combined with delta-(2-amino-6-hydroxy-3,4-dihydro-4-oxo-5-pyrimidinyl)-valeric acid (VUFB-9777, Damvar) on serum antibody formation was studied in mice. The immunosuppressive effect of azathioprine depended on the regimen of administration. VUFB-9777 alone produced no immunosuppressive effect but markedly enhanced that of azathioprine.

Animals↗
PubMed1994

[Double-blind method of the effect of menopause symptoms, lipid profile, and endometrial thickness of continuous therapy with estradiol valerate and medroxyprogesterone acetate].

Continuous combined therapy (CCT) using estrogens and progestagens has appeared as an alternative to avoid vaginal bleeding, which is characteristic of sequential hormone therapy, and the main reason for the stopping treatment. Irregular vaginal bleeding can occur at the beginning of treatment, but it has been observed that after a few months patients are in amenorrhea. Fifty postmenopausal women were studied in order to evaluate the clinical outcome. Half of them were treated with a product containing 2 mg estradiol valerate and 2.5 mg medroxiprogesterone acetate, while the other half received a placebo. Menopause symptomatology was recorded as described by Blatt-Kupperman, depression was evaluated with the use of Hamilton's test, lipid profile by enzymatic methods and endometrial thickness by transvaginal ultrasonography. Patients were evaluated at the beginning, third and sixth month of the study, following a double blind methodology. Symptomatology diminished both in patients under CCT and using placebo, although improvement was significantly greater in patient under CCT. Thus in the hormone treated group the Blatt-Kupperman score fell from 12.1 to 6.4 and 3.2 in the third and sixth month respectively, while in the group receiving placebo the score fell from 11.5 to 6.3 in the third month and raised to 7.4 in the sixth month. Hamilton's test showed a significant improvement of depression only in patients under hormone therapy. Nineteen out of twenty five women using CCT had vaginal bleeding, showing no changes in the endometrial thickness during the study. Finally, HDL-cholesterol was raised in 14.5% while LDL-cholesterol was lowered in 18.7% (p < 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)

Double-Blind Method↗
PubMed1979

Comparison of the sensitivities of human, canine, and murine hematopoietic precursor cells to adriamycin and N-trifluoroacetyladriamycin-14-valerate.

The sensitivities of leukocyte-committed stem cells of human, dog, and mouse bone marrow to an 18-hr exposure to Adriamycin (ADR) and N-trifluoroacetyladriamycin-14-valerate (AD32) were compared using the agar diffusion chamber assay. The survival of in situ mouse marrow stem cells following the drugs was also measured. The in vivo doses required to produce 37% survival of hematopoietic precursor cells for human, dog, mouse, and in situ mouse marrow stem cells for ADR were 9.5, 3.5, 8, and 8 mg/kg, respectively, while those for AD32 were 22, 17, 37, and 40 mg/kg. Mouse bone marrow cellularity was reduced to 50% by drug doses producing 3 and 7% stem cell survival. AD32 given i.p. to mice was less effective than i.v. drug in producing marrow stem cell death, reduction of marrow cellularity, or acute lethality. Although more AD32 than ADR was required to kill marrow stem cells from each species and canine marrow stem cells were the most sensitive to either drug, human stem cells were relatively more sensitive to AD32 than were mouse stem cells. The reverse was true for ADR. Granulocytopenia may be an important limiting toxicity in the clinical use of AD32.

Animals↗
PubMed1979

Effects of N-trifluoroacetyladriamycin-14-valerate and related agents on DNA strand damage and thymidine incorporation in CCRF-CEM cells.

N-Trifluoroacetyladriamycin-14-valerate (AD32) and N-trifluoroacetyladriamycin (AD41) have been compared with Adriamycin and daunorubicin in CCRF-CEM human lymphoblastic cells. All four agents produce DNA damage, as measured by alkaline unwinding methods. Thymidine incorporation, a measure of DNA synthesis, is inhibited by AD32 and AD41 and completely blocked by the other drugs. AD32 and AD41 inhibit growth of the cells after exposure for 2 hr but are considerably less potent than is either Adriamycin or daunorubicin. In drug uptake studies, cellular levels after 2-hr incubations are lower for AD32 than for Adriamycin, and both are severalfold lower than are those of daunorubicin. The results indicate that AD32 and AD41 (or their metabolites) have DNA-related effects similar to those of Adriamycin and daunorubicin. These common actions may be the proximal cytotoxic events for the four agents.

Cell Division↗
PubMed1993

Follicular growth rate and lack of influence of oestradiol valerate, testosterone propionate and aminoglutethimide phosphate on ovarian follicular development in the musk shrew, Suncus murinus L.

Growth rate of follicles and effects of administration of oestradiol valerate (EV), testosterone propionate (TP) and aminoglutethemide phosphate (AGP) on the development of ovarian follicles of the adult musk shrew were investigated. The follicular growth rate was estimated by mitotic index before and 2 hr after colchicine treatment to the shrews. Mitotic index of granulosa cells increased linearly with the increase in the follicular diameter. The calculated mean duration of mitosis was 0.48 hr. The mean time taken for follicle to pass from primary follicle stage to preovulatory stage was estimated to be 12 days. Treatment of both the steroids EV and TP, failed to produce any noticeable effect on the atretic follicle of the musk shrew. The results indicate that neither EV or TP, nor the potent steroid inhibitor AGP had any influence on the growth of large follicles in this primitive eutherian mammal.

Aminoglutethimide↗
PubMed1998

[Effect of estradiol valerate on the male reproductive organs and various semen parameters in rats].

The effect of the administration of estradiol valerate on the male reproductive organs, on their histological structure, and several semen parameters of Wistar rats was studied. In experiment A and B 140 micrograms estradiol valerate/kg b.w. were administered once a week for 4 weeks to 14 weeks old rats by s.c. injection. One week after the 4th injection the rats of experiment A were sacrificed, while the rats of experiment B lived 5 weeks without treatment for recovery. In both experiments, suppression of body weight, food consumption, decreases in absolute and relative weights of testes, epididymides, prostate and semen vesicles were observed along with testis, epididymis, seminal vesicle and prostate atrophy. The absolute and relative weights of adrenals and pituitary revealed a tendency for increase in both treated groups. The histopathological examination of the testes revealed degeneration of spermatozytes in experiment A, and degeneration of spermatozytes, spermatides, spermatozoa, Sertoli and Leydig cells in experiment B. In experiment A the motility, and number of sperms was significantly decreased, the sperm abnormalities were significantly increased. In experiment B the motility of sperms was slightly, the number significantly decreased and the abnormalities slightly increased.

Adrenal Glands↗
PubMed1979

Physical model evaluation of topical prodrug delivery-simultaneous transport and bioconversion of vidarabine-5'-valerate I: Physical model development.

A physical model approach to the topical delivery of a vidarabine ester prodrug was investigated. It involved modeling, theoretical simulations, experimental method development for factoring and quantifying parameters, and, finally, employment of the deduced parameters to determine the steady-state species fluxes and concentration profiles in the target tissue. The present report describes the physical modeling and theoretical simulation aspects. The physical model for the simultaneous transport and bioconversion of a topically delivered prodrug was formulated assuming homogeneous enzyme distributions and constant diffusivities in the membrane. The mathematical problem was solved, and the solution yielded concentration profiles and fluxes of all species in the biomembrane. These results provided the prevailing levels of the prodrug, the drug, and the metabolite at the target site and the transport rates of all species into the bloodstream. Computations of concentration profiles and fluxes were carried out for a reasonable range of the parameters. The relative activities of the esterase and the deaminase enzymes, as well as the stratum corneum permeabilities, were important in influencing the concentration profiles and fluxes of all species.

Administration, Topical↗