antifertility

Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor (Ki: 0.18 μM) that inhibits estrogen biosynthesis, exhibits antifertility effects, and induces impairment of spatial memory.

Fluphenazine decanoate is dopamine D2 receptor blocke,and is a long-acting phenothiazine neuroleptic that used to treat schizophrenia.

Lotrifen (Privaprol), an agent of non-hormonal antifertility, causes the arrest and involution of pregnancy. It acts, after the implantation of the blastocyst, directly on the product of conception, which undergoes a slow and gradual degenerative process and ends with the reabsorption or expulsion of it.

Broparestrol (E)- has antifertility activity and is a potent inhibitor of rodent mammary tumorigenesis.

Grandiflorenic acid can reproduce the uterine responses induced by aqueous extract of zoapatle leaves. It is suggested that grandiflorenic acid may have an antifertility effect.

Diethyl adipate has an effect of antifertility.

Prostaglandin F2β (PGF2β) is the 9β-hydroxy stereoisomer of PGF2α. It is much less active than PGF2α in antifertility and bronchoconstrictor activities. PGF2β exhibits bronchodilating activity in guinea pigs and cats and antagonizes the bronchoconstrictor activity of PGF2α.

L 10503 is an antifertility agent.

J 628 is a synthetic impeded estrogen derivative. It also has some postcoital antifertility activity.

Coccinic acid shows inhibitory effects against colorectal carcinoma HCT-15 and oral epithelial cell line KB-3-1.Mixture of coccinic acid and anwuweizonic acid shows significant inhibitory activity against human decidual cells and rat luteal cells in vitro

Prostaglandin F2α (PGF2α) 1,9-lactone, a lipid-soluble internal ester of PGF2α, demonstrates resistance to hydrolysis by human plasma esterases, maintaining its structure even after 20 hours of incubation under physiological conditions. Unlike PGF2α, this compound exhibits minimal antifertility and vasoactivity.

Azacosterol is a diaza derivative of cholesterol which acts as a hypocholesteremic agent by blocking delta-24-reductase causing accumulation of desmosterol. Azacosterol acts as an inhibitor of 24-dehydrocholesterol reductase (24-DHCR), preventing the formation of cholesterol from desmosterol. Although it primarily acts to inhibit 24-DHCR, the drug also inhibits other steps in cholesterol biosynthesis. The antifertility effects of the drug in birds are mediated by inhibition of steroid hormone production, steroid hormones being synthesized from cholesterol.

Prostaglandin F2α 1,11-lactone (PGF2α 1,11-lactone) is a lipid-soluble prodrug of Prostaglandin F2α and can be used in studies about treating glaucoma. Prostaglandin F2α 1,11-lactone is active as an antifertility agent with greatly reduced vasoactivity.

Lupeol acetate possesses antinociceptive, antifertility, and anti-inflammatory properties, the effect probably involves the opioid system, as indicated by the complete blockade of the opioid antagonist naloxone.

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.

L 11204 is an antifertility in vivo. It is an inhibitor of prostaglandin synthesis.

17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to increase lipid solubility, thereby improving uptake into tissues and further lowering the effective concentration. Ethyl amide groups are then removed by amidases, regenerating the active free acid.

Rohitukine is an anti-cancer agent. It modulates apoptosis pathways through gastrin antagonism and H(+) K (+)-ATPase inhibition. Rohitukine ia an antiadipogenic, antidyslipidemic, gastroprotective, antifertility, and antileishmanial compound.

15(S)-15-methyl Prostaglandin D2 (15(S)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. Unlike PGD2, 15(S)-15-methyl PGD2 induces vasoconstriction, increases systemic blood pressure, and exhibits significantly reduced inhibitory activity on ADP-induced platelet aggregation. It also demonstrates strong antifertility activity in hamsters, being 200-fold more potent than PGD2.

Anwuweizonic acid may have inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice. Mixture of coccinic acid and anwuweizonic acid has antifertility activity, shows significant inhibitory activity against human decidu