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Nafarelin acetate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
Exendin-4 (exenatide), a 39-amino acid peptide originally isolated from the salivary glands of the Gila monster (Heloderma suspectum), differs from exendin-3 only in two positions close to the N-terminus. Application of exenatide causes an increase in acinar cAMP without stimulating amylase release. As an incretin mimetic, exenatide acts as agonist of the glucagon-like peptide-1 (GLP-1) receptor. As GLP-1, though with prolonged activity, exenatide augments the postprandial production of insulin and suppresses secretion of glucagon. For this reason, exenatide has found use as a medication of diabetes II.
Bivalirudin, a peptide anticoagulant, is a direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
Glucagon-like peptide-1 (GLP-1) is an incretin derived from the transcription product of the proglucagon gene. The major source of GLP-1 in the body is the intestinal L cell that secretes GLP-2 as a gut hormone.
Carbetocin is a long-acting synthetic agonist analogue of human oxytocin, with antihemorrhagic and uterotonic activities. Upon administration, carbetocin targets, binds to and activates peripheral oxytocin receptors that are present on the smooth musculature of the uterus. This causes uterus contractions and prevents excessive bleeding after childbirth, particularly following Cesarean section, and may be used to decrease blood loss during hysteroscopic myomectomy.
Cetrorelix Acetate is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 1.21 nM). It can suppress production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland which inhibits ovulation, exhibit antiproliferative effects and display efficacy against hormone-sensitive cancers in vivo. It is often used to treat hormone-sensitive cancers of the prostate and breast.
Glucagon (Porcine glucagon) is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon decreases the activity of HNF-4. Glucagon increases HNF4α phosphorylation.