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, a ...
(PGE
2) that has
oxytocic 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 PGE
2:
prostaglandin EP1 receptor,
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 w ...
, 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 cel ...
. Sulprosotone binds to and activates the
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 w ...
with far greater efficacy than the other PGE
2 receptors and also has the advantage of being relatively resistant, compared with PGE
2, to becoming metabolically degraded. It is listed as a comparatively weak
receptor agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ag ...
of the prostaglandin EP1 receptor. In all events, this as well as other potent synthetic EP
3 receptor antagonists 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 vasoconst ...
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. Medic ...
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 fo ...
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 EP
3 receptor agonists are in development as drugs for the possible treatment of stomach ulcers in humans.
References
Eicosanoids
Sulfonamides
Cyclopentanes
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