Selective progesterone receptor modulators (SPRMs) represent a new class of progesterone receptor ligands that exert clinically relevant tissue-selective progesterone agonist, antagonist, partial, or mixed agonist/antagonist effects on various progesterone target tissues in an in vivo situation depending on the biological action studied. The SPRM asoprisnil is being studied in women with symptomatic uterine leiomyomata and endometriosis. Asoprisnil shows a high degree of uterine selectivity as compared to effects on ovulation or ovarian hormone secretion in humans. It induces amenorrhea and decreases leiomyoma volume in a dose-dependent manner in the presence of follicular phase estrogen concentrations. It also has endometrial antiproliferative effects. In pregnant animals, the myometrial, i.e. labor-inducing, effects of asoprisnil are blunted or absent. Studies in non-human primates played a key role during the preclinical development of selective progesterone receptor modulators. These studies provided the first evidence of uterusselective effects of asoprisnil and structurally related compounds, and the rationale for clinical development of asoprisnil.
An herbal preparation prepared by the traditional healers of Mandsaur using cow urine and Gymnema sylvestre R. Br. (Leguminosae) is being used in the treatment of diabetes. In order to scientifically appraise the claim, this preparation was studied for antidiabetic activity and also compared with the herbal preparation prepared using water. Fresh cow urine was also used in the study to identify the synergistic effect. The preparations were tested for antidiabetic activity in alloxan-induced diabetic rats at two dose level, 200 and 400 mg/kg, respectively. The study was done for a period of 21 days. The activity was compared with reference standard, insulin (1 unit/kg, i.p.) and control. The herbal preparations significantly (P< 0.05, P < 0.01) lowered the blood sugar level of hyperglycemic rats in a dose-dependent manner. Comparatively, the cow urine preparation showed better activity than did the preparation prepared using water. Fresh cow urine also exhibited significant antidiabetic effect. This study supports the claim of the local traditional healers.
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