Sulprostone is an analogue of

prostaglandin E2 Prostaglandin E2 (PGE2), also known as dinoprostone, is a naturally occurring prostaglandin with oxytocic properties that is used as a medication. Dinoprostone is used in labor induction, bleeding after delivery, termination of pregnancy, and ...

(PGE₂) that has

oxytocic A uterotonic, also known as ecbolic, are pharmacological agents used to induce contraction or greater tonicity of the uterus. Uterotonics are used both to induce labor and to reduce postpartum hemorrhage. Labor induction in the third trimester of ...

activity in assays of rat kidney cells and tissues. There are four known receptors which mediate various but often different cellular and tissue responses to PGE₂:

prostaglandin EP1 receptor Prostaglandin E2 receptor 1 (EP1) is a 42kDa prostaglandin receptor encoded by the PTGER1 gene. EP1 is one of four identified EP receptors, EP1, EP2, EP3, and EP4 which bind with and mediate cellular responses principally to prostaglandin E2) (PG ...

prostaglandin EP2 receptor Prostaglandin E2 receptor 2, also known as EP2, is a prostaglandin receptor for prostaglandin E2 (PGE2) encoded by the human gene PTGER2: it is one of four identified EP receptors, the others being EP1, EP3, and EP4, which bind with and mediate ...

prostaglandin EP3 receptor Prostaglandin EP3 receptor (53kDa), also known as EP3, is a prostaglandin receptor for prostaglandin E2 (PGE2) encoded by the human gene PTGER3; it is one of four identified EP receptors, the others being EP1, EP2, and EP4, all of which bind wi ...

, and

prostaglandin EP4 receptor Prostaglandin E2 receptor 4 (EP4) is a prostaglandin receptor for prostaglandin E2 (PGE2) encoded by the PTGER4 gene in humans; it is one of four identified EP receptors, the others being EP1, EP2, and EP3, all of which bind with and mediate cell ...

. Sulprosotone binds to and activates the

with far greater efficacy than the other PGE₂ receptors and also has the advantage of being relatively resistant, compared with PGE₂, to becoming metabolically degraded. It is listed as a comparatively weak

receptor agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an ...

of the prostaglandin EP1 receptor. In all events, this as well as other potent synthetic EP₃

receptor antagonist A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of rece ...

s have the realized or potential ability to promote the beneficial effects of prostaglandin EP3 receptor activation. Sulprostone (as well as other

prostanoids Prostanoids are active lipid mediators that regulate inflammatory response. Prostanoids are a subclass of eicosanoids consisting of the prostaglandins (mediators of inflammatory and anaphylactic reactions), the thromboxanes (mediators of vasocons ...

receptor agonists) is in use for inducting

medical abortion A medical abortion, also known as medication abortion, occurs when drugs (medication) are used to bring about an abortion. Medical abortions are an alternative to surgical abortions such as vacuum aspiration or dilation and curettage. Medical ...

and ending pregnancy after fetal death, for the treatment of severe atonic

postpartum hemorrhage Postpartum bleeding or postpartum hemorrhage (PPH) is often defined as the loss of more than 500 ml or 1,000 ml of blood following childbirth. Some have added the requirement that there also be signs or symptoms of low blood volume for ...

after vaginal delivery, and for removal of the placenta in patients with retained placenta. Currently, sulprostone along with SC-46275, MB-28767, ONO-AE-248 and other EP₃ receptor agonists are in development as drugs for the possible treatment of stomach ulcers in humans.

References

Eicosanoids Sulfonamides Cyclopentanes {{Genito-urinary-drug-stub