Vasopressin agonists

Arginine vasopressin Agonist of vasopressin (and V2) receptors Vasoconstriction Vasodilatory shock... 

Thibonnier, M. (199CQ Vasopressin agonists and antagonists. Harm. J2es..34.124-128. Laszto, F.A. etal. (1991) Pharmacolocy and clinical perspectives of vasopressin antagonists. Pharmacol. Rev.. 43.7J -108. 

Trade names Glypressin (IS Pharma) Haemopressin Lucassin Terlipressin (Ferring) (Bissendorf Peptide) Variquel Indications Esophageal variceal hemorrhage Category Vasopressin agonist Half-life 50-70 minutes... 

Ogawa, H., Kondo, K., Shinohara, T., Kan, K., Tanada, Y., Kurimura, M., Morita, S. and Uchida, M. (1997) WO-09722591. Benzazepine derivatives with vasopressin agonistic activity. Otsuka Pharmaceutical Co Ltd. 

Failli, A.A., Shumsky, J.S. and Trybulski, E.J. (2000) WO-00046224. Tricyclic pyridine N-oxides vasopressin agonists. Wyeth. 

M. Kagan, M. Chlenov, S. Melnikov, O. McConnell, A. C. Bach, G. Carter, A. Failli, T. J. Caggiano, J. S. Shumsky, D. Lubda, Normal-phase automated mass-directed HPLC purification of a pyrrolohenzodiazepine library with vasopressin agonist activity. J. Comb. Chem. 2009,11, 704-719. 

Kagan, M., Chlenov, M., Melnikov, S., McConnell, O., Bach, A.C., Carter, G., Failli, A., Caggiano, T.J., Shumsky, J. S. and Lubda, D. Normal-phase automated mass-directed HPLC purification of a pyrrolobenzodiazepine library with vasopressin agonist activity. Journal of Combinatorial Chemistry 11(4) 704—719, 2009. 

Table 20. Vasopressin and Oxytocin and Receptor Agonists and Antagonists...

The release of NO from the endothelium is induced by various chemical substances, including acetylcholine polypeptides such as substance P, bradykinin, and arginine vasopressin histamine ATP/ADP a2-adrenoceptor agonists thrombin and Ca2+ iono-phores. NO formed in response to mechanical stimuli like shear stress or transmural pressure plays an important role in maintaining basal blood flow. Endothelial NO causes vasodilatation, decreased... 

In some cases, receptor inactivation, e.g., of the V2 vasopressin receptor, is mediated by agonist-induced enzymatic cleavage of the GPCR. This nonendocytic proteolysis is promoted by a plasma membrane-associated metalloprotease. Proteinase-activated receptors (PARs) such as the thrombin receptor also follow a distinctly different pathway. PARs require the enzymatic cleavage of their N terminus, and the newly generated N terminus activates the receptor. Once... 

A substantial review of the molecular pharmacology of human vasopressin receptors (including oxytocin) and peptidic agonists and antagonists has appeared [135]. 

Vasopressin causes vasoconstrictive effects that, unlike adrenergic receptor agonists, are preserved during hypoxia and severe acidosis. It also causes vasodilation in the pulmonary, coronary, and selected renal vascular beds that may reduce pulmonary artery pressure and preserve cardiac and renal function. However, based on available evidence, vasopressin is not recommended as a replacement for norepinephrine or dopamine in patients with septic shock but may be considered in patients who are refractory to catecholamine vasopressors despite adequate fluid resuscitation. If used, the dose should not exceed 0.01 to 0.04 units/min. 

Ferris, C. F., and Delville, Y. 1994. Vasopressin and serotonin interactions in the control of agonistic behavior. Psychoneuroendocrinology 19 593-602. 

The residues required for internalization, like those implicated in desensitization motifs, do not always meet the requirements for putative sites of kinase-mediated phosphorylation. Among the numerous motifs that have been implicated, an NPXXY motif (154,173) may be required for agonist-induced activation and inter-nahzation of the p -adrenergic receptor, and a dileucine motif in the carboxyl tail of many GPCRs (154) may be involved in internalization of receptors such as the Pj-adrenergic (174) and the vasopressin Via receptors (175). 

Glucagon Vasopressin a-Adrenergic agonists /1-Adrenergic antagonists ... 

Abelson JL, Le Melledo JM, Bichet DG (2001) Dose response of arginine vasopressin to the CCK-B agonist pentagastrin. Neuropsychopharmacology 24 161-169 Antoni FA (1993) Vasopressinergic control of pituitary adrenocortico tropin secretion comes of age. Front Neuroendocrinol 14 76-122... 

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