Relcovaptan is a potent, orally active nonpeptide vasopressin V1a antagonist that was undergoing clinical development with Sanofi-Synthélabo (formerly Sanofi) in France. SR49059 is specifically and selectively antagonizes the effect of vasopressin on the V1a receptor in animals’ and in humans. The drug has been shown to have an excellent safety profile in single and repeated dose toxicological studies in animals. In the human uterus in vitro, SR49059 caused a dose-dependent inhibition of vasopressin V1a receptor-mediated activity of myometrial strips and isolated uterine arteries. In vivo in nonpregnant women, an inhibition of vasopressin-induced uterine activity has been observed.

Ataprost (also known as ONO-41483; OP-41483), an epoprostenol agonist, participated in phase II clinical trials in Japan for the treatment patients with heart failure and myocardial ischemia. However, these trials were discontinued.

Argipressin is a neurohypophysial hormone from the vasopressin hormone family. Its two primary functions are to retain water in the body and to constrict blood vessels. The antidiuretic action of Argipressin is ascribed to increase in reabsorption of water by the renal tubules. Argipressin can cause contraction of smooth muscle of the gastrointestinal tract, gall bladder, urinary bladder and all parts of the vascular bed, especially the capillaries, small arterioles and venules with less effect on the smooth musculature of the large veins. Agripressin for injections is used for use in diabetes insipidus, when this is not of nephrogenic origin and control of bleeding from oesophageal varices. In addition, argipressin is indicated to increase blood pressure in adults with vasodilatory shock (e.g., post-cardiotomy or sepsis) who remain hypotensive despite fluids and catecholamines.

Felypressin is a non-catecholamine vasoconstrictor that is chemically related to vasopressin, the posterior pituitary hormone. Felypressin is added to some local anesthetics such as prilocaine in a concentration of 0.03 IU/ml. Its antidiuretic effects are less than those of vasopressin. Felypressin is used as a vasoconstrictor in local anesthetic injections for dental use and is an ingredient of preparations that have been used for the treatment of pain and inflammation of the mouth.