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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.
Goserelin acetate stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner. This causes the disruption of the endogenous hormonal feedback systems, resulting in the down-regulation of testosterone and estrogen production.
Abarelix is a synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It directly and competitively binds and blocks the gonadotropin releasing hormone receptors in the anterior pituitary, which inhibits the secretion and release of the luteinizing hormone (LH) and follicle stimulating hormone (FSH). For men, the inhibition of LH secretion prevents the release of testosterone. Therefore, it can relieve symptoms associated with prostate hypertrophy or prostate cancer.
Deslorelin acetate is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist) also known as an LHRH agonist. It stops the production of sex hormones (testosterone and oestrogen).
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.
Bivalirudin, a peptide anticoagulant, is a direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
Buserelin Acetate is an agonist of gonadotropin-releasing hormone receptor(GnRHR). Buserelin is a synthetic luteinizing hormone–releasing hormone (LHRH) analog.
Terlipressin is a synthetic triglycyllysine derivative of vasopressin with vasoconstrictive, antihemorrhagic, and antidiuretic properties. Upon intravenous administration, terlipressin, an inactive prodrug, is biotransformed to its active moiety, lysine vasopressin (LVP), a nonselective vasopressin analogue with affinity for vasopressin receptors V1 (V1a), V2 and V3 (V1b). As a V1 agonist, terlipressin increases systemic vascular resistance, particularly in the splanchnic area, resulting in a decrease of portal pressure. V1 binding also promotes platelet aggregation and glycogenolysis, while V3 binding induces adrenocorticotropic hormone (ACTH) secretion. Compared to vasopressin, terlipressin has a minimal effect on V2 receptors, which are responsible for promotion of water reabsorption in the collecting ducts of the kidney via stimulation of cyclic AMP production.