AhR modulator-1 is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. It inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. It also possesses anti-estrogenic properties in rat uterus.
Mabuterol is a selective agonist of β2 adrenoreceptor with no beta 1-stimulation. Mabuterol inhibited the positive inotropic effect of isoprenaline at 10(-7) g ml and decreased the maximum driving frequency at 3 X 10(-6) g ml. Mabuterol was 3 times more p
9-deoxy-9-methylene Prostaglandin E2 (9-deoxy-9-methylene PGE2) is a stable, isosteric analog of PGE2 . 9-deoxy-9-methylene PGE2 retains the biological profile of PGE2 with fewer side effects. In the rat 9-deoxy-9-methylene PGE2 is equipotent to PGE2 in decreasing blood pressure. It also stimulates the gerbil colon and primate uterus at the same potency as PGE2.
5β-Dihydroprogesterone (5β-DHP) is a progesterone receptor agonist and metabolite of progesterone .1,2It is formed from progesterone by 5β-reductase.25β-DHP inhibits spontaneous contractions in isolated rat uterus when used at a concentration of 10 μg ml, an effect that can be blocked by the progesterone receptor antagonist RU486 but not the GABAAreceptor antagonist picrotoxin .1It is a negative modulator of homooligomeric Ρ1 subunit-containing GABAAreceptors, inhibiting GABA-induced currents inX. laevisoocytes expressing these receptors (IC50= 5.02 μM).3Plasma levels of 5β-DHP decrease at the onset of spontaneous human labor.4
TAS-108, also known as SR16234, is a synthetic, antiestrogenic steroidal compound with potential antitumor activity. TAS-108 binds to and inhibits estrogenic receptor alpha (ERa), mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors. Blockage of ERa by TAS-108 prevents the binding and effects of estrogen and may lead to an inhibition of estrogen-dependent cancer cell proliferation. TAS-108 also is a partial agonist of the estrogenic receptor beta (ERb), expressed in many tissues including the central nervous system, urogenital tract, bone and cardiovascular system, thereby exerting a positive effect on these tissues.
17-Phenyl trinor Prostaglandin E2 (17-phenyl trinor PGE2) is a synthetic analog of PGE2, functioning as an agonist at the EP1 and EP3 receptors. It induces contraction of the guinea pig ileum at a 11 µM concentration and displays slightly less potency than PGE2 in stimulating the gerbil colon and rat uterus. Notably, with an ED50 value of 350 µg kg, 17-phenyl trinor PGE2 exhibits 4.4 times greater antifertility efficacy in hamsters compared to PGE2.