More than a century ago, Sir Henry Dale demonstrated that a component of the pituitary causes contractions of the mammalian uterus, hence his coining the term “oxytocic,” derived from the Greek for “quick birth,” for its activity. The discovery that a component of the pituitary causes milk secretion followed within a few years. By 1930, oxytocin was separated from vasopressin into pitocin and pitressin, respectively, at Parke Davis and made available for research. That a single peptide was responsible for these uterine and mammary actions was definitively confirmed upon the sequencing and synthesis of the peptide, 9 amino acids in length. Vincent du Vigneaud was awarded a Nobel Prize for this work. Oxytocin is indicated for the initiation or improvement of uterine contractions, where this is desirable and considered suitable for reasons of fetal or maternal concern, in order to achieve vaginal delivery. Oxytocin is indicated to produce uterine contractions during the third stage of labor and to control postpartum bleeding or hemorrhage. Uterine motility depends on the formation of the contractile protein actomyosin under the influence of the Ca2+- dependent phosphorylating enzyme myosin light-chain kinase. Oxytocin promotes contractions by increasing the intracellular Ca2+. Oxytocin has specific receptors in the myometrium and the receptor concentration increases greatly during pregnancy, reaching a maximum in early labor at term. The Oxytocin receptor is a typical class I G protein-coupled receptor that is primarily coupled via G(q) proteins to phospholipase C-beta. The high-affinity receptor state requires both Mg(2+) and cholesterol, which probably function as allosteric modulators. The agonist-binding region of the receptor has been characterized by mutagenesis and molecular modeling and is different from the antagonist binding site. The function and physiological regulation of the Oxytocin system is strongly steroid dependent.

More than a century ago, Sir Henry Dale demonstrated that a component of the pituitary causes contractions of the mammalian uterus, hence his coining the term “oxytocic,” derived from the Greek for “quick birth,” for its activity. The discovery that a component of the pituitary causes milk secretion followed within a few years. By 1930, oxytocin was separated from vasopressin into pitocin and pitressin, respectively, at Parke Davis and made available for research. That a single peptide was responsible for these uterine and mammary actions was definitively confirmed upon the sequencing and synthesis of the peptide, 9 amino acids in length. Vincent du Vigneaud was awarded a Nobel Prize for this work. Oxytocin is indicated for the initiation or improvement of uterine contractions, where this is desirable and considered suitable for reasons of fetal or maternal concern, in order to achieve vaginal delivery. Oxytocin is indicated to produce uterine contractions during the third stage of labor and to control postpartum bleeding or hemorrhage. Uterine motility depends on the formation of the contractile protein actomyosin under the influence of the Ca2+- dependent phosphorylating enzyme myosin light-chain kinase. Oxytocin promotes contractions by increasing the intracellular Ca2+. Oxytocin has specific receptors in the myometrium and the receptor concentration increases greatly during pregnancy, reaching a maximum in early labor at term. The Oxytocin receptor is a typical class I G protein-coupled receptor that is primarily coupled via G(q) proteins to phospholipase C-beta. The high-affinity receptor state requires both Mg(2+) and cholesterol, which probably function as allosteric modulators. The agonist-binding region of the receptor has been characterized by mutagenesis and molecular modeling and is different from the antagonist binding site. The function and physiological regulation of the Oxytocin system is strongly steroid dependent.

Zinc monocarbonate (Zinc Carbonate) is an inorganic salt. In the United States, Zinc Carbonate may be used as an active ingredient in OTC drug products. When used as an active drug ingredient, the established name is Zinc Carbonate. Zinc monocarbonate is generally recognized as safe by FDA. It is used as skin protectant active ingredient. Zinc carbonate was found to retard the degradation of some poly(lactide-co-glycolide) (PLG) microspheres in vivo and in vitro. Adding Zinc Carbonate is essential during the preparation of PLGA microspheres. It can remarkably improve the stability of drugs in the acid microenvironment inside PLGA microspheres.

Aviptadil, a vasoactive intestinal polypeptide, is a vasodilator and lowers blood pressure if administered intravenously. In 2007, the orphan designation was granted by the European Commission for aviptadil for the treatment of sarcoidosis, a disease of unknown cause that affects many organs and tissues, most commonly the lungs. Sarcoidosis is characterized by specific microscopic lesions called granulomas. Aviptadil is able to influence the immune system that decreases the inflammatory processes seen in sarcoidosis by acting on the white blood cells (lymphocytes and monocytes) involved in the formation of the granulomas. In combination with phentolamine, the drug is used to treat erectile dysfunction. In addition, aviptadil has been studied in phase II clinical trials for patients with respiratory distress syndrome.

Thymoctonan (also known as Thymic humoral factor γ2 ) is an octapeptide thymic hormone patented by Yeda Research and Development Co. Ltd. as an immunoregulatory agent. In preclinical models, Thymoctonan exerts potent anti-tumor activity in mice and significantly increases the specific cytotoxic response of immune spleen cells. In addition, Thymoctonan treatment improved the competence of immune spleen cells in adoptive immunotherapy when performed in combination with chemotherapy by melphalan. Besides that Thymoctonan enhancing the anti-viral potential of murine cytomegalovirus immune spleen cells. In fatal murine cytomegalovirus infection model, daily injections of Thymoctonan- enhanced murine cytomegalovirus immune spleen cells prevented the development of a fatal disease in 93% of the recipient mice.

Tertomotide (also known as GV1001) is a synthetic telomerase-specific peptide vaccine patented by Norsk Hydro Asa for the cancer treatment. The agent was initially developed as a cancer vaccine, for example, against pancreatic and prostate cancer. Telomerase, a reverse transcriptase normally repressed in healthy cells, is overexpressed in most cancer cells and plays a key role in cellular proliferation. Vaccination with Tertomotide may activate the immune system to mount a cytotoxic T-lymphocyte response against telomerase-expressing cells. Subsequently, in vivo studies have demonstrated the efficacy of Tertomotide in alleviating benign prostatic hyperplasia (BPH) symptoms by reducing the size of the prostate gland. The mechanism of action of Tertomotide has been proposed to be through its dual activity as a GnRH inhibitor and 5a-reductase inhibitor. The GnRH antagonist activity has been established by co-immunoprecipitation assay, demonstrating an interaction between Tertomotide and the GnRH receptor, which was abolished by pre-treatment with anti-GnRH receptor antibody.

TAT-NR2B9C is a synthetic peptide fusion of the nine C-terminal residues of the NR2B subunit of the N-methyl-D-aspartate (NMDA) receptor and the cell membrane protein transduction domain of the HIV-1 tat protein. It is a postsynaptic density protein-95 (PSD95) inhibitor with neuroprotective properties. It is under development for the treatment of acute stroke and acute cerebral ischemia.