antidiuretic hormone receptor antagonists


Summary: Endogenous compounds and drugs that inhibit or block the activity of ANTIDUIRETIC HORMONE RECEPTORS.

Top Publications

  1. Kinugawa K, Imamura T, Komuro I. Experience of a vasopressin receptor antagonist, tolvaptan, under the unique indication in Japanese heart failure patients. Clin Pharmacol Ther. 2013;94:449-51 pubmed publisher
  2. Tominaga N, Kida K, Matsumoto N, Akashi Y, Miyake F, Kimura K, et al. Safety of add-on tolvaptan in patients with furosemide-resistant congestive heart failure complicated by advanced chronic kidney disease: a sub-analysis of a pharmacokinetics/ pharmacodynamics study. Clin Nephrol. 2015;84:29-38 pubmed publisher
    ..In this short-term pilot study, coadministration of tolvaptan and furosemide appears to be safe in patients with heart failure and CKD. ..
  3. Adler S, Martinez J, Williams D, Verbalis J. Positive association between blood brain barrier disruption and osmotically-induced demyelination. Mult Scler. 2000;6:24-31 pubmed
  4. Wu M, Chen T, Chen Y, Tarng D, Wu Y, Lin H, et al. Effects and safety of oral tolvaptan in patients with congestive heart failure: A systematic review and network meta-analysis. PLoS ONE. 2017;12:e0184380 pubmed publisher
    ..However, tolvaptan is not beneficial for reducing all-cause mortality in CHF patients. ..
  5. Adachi S, Miura S, Shiga Y, Arimura T, Morii J, Kuwano T, et al. Effects of Tolvaptan With or Without the Pre-Administration of Renin-Angiotensin System Blockers in Hospitalized Patients With Acute Decompensated Heart Failure. Int Heart J. 2017;58:385-392 pubmed publisher
    ..In conclusion, tolvaptan alone might induce an increase in UV in decompensated HF patients without ARB/ ACE-I, although the treatment of HF with ARB/ACE-I is the first choice strategy. ..
  6. Tabata H, Yoneda T, Oshitari T, Takahashi H, Natsugari H. Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form. J Med Chem. 2017;60:4503-4509 pubmed publisher
  7. Takasu K, Miyazaki T, Negoro K, Yatsu S, Shimizu M, Murata A, et al. Successful Treatment of Congestive Heart Failure Due to Severe Aortic Valve Stenosis With Low Dose Tolvaptan in Elderly Patients. Int Heart J. 2017;58:378-384 pubmed publisher
    ..In elderly patients with severe AS, TLV treatment improved CHF without hemodynamic instability. Further prospective studies are needed to assess the safety and efficacy of TLV in decompensated heart failure due to severe AS. ..
  8. Hou L, Zhu L, Zhang M, Zhang X, Zhang G, Liu Z, et al. Participation of Antidiuretic Hormone (ADH) in Asthma Exacerbations Induced by Psychological Stress via PKA/PKC Signal Pathway in Airway-Related Vagal Preganglionic Neurons (AVPNs). Cell Physiol Biochem. 2017;41:2230-2241 pubmed publisher
    ..Our results strongly suggested that ADH participated in psychological stress-induced asthma exacerbations via PKA/PKC signal pathway in AVPNs. ..
  9. Vishram Nielsen J, Gustafsson F. Vasopressin and Vasopressin Antagonists in Heart Failure. Handb Exp Pharmacol. 2017;243:307-328 pubmed publisher
    ..This chapter reviews the role of AVP and copeptin in HF, and the treatment potential of VRAs in HF. ..

More Information


  1. Braun M, Mahowald M. Electrolytes: Sodium Disorders. FP Essent. 2017;459:11-20 pubmed
    ..Hypernatremia most often occurs because of water loss or inadequate water intake. Depending on severity, management involves oral or intravenous hypotonic fluids and addressing the underlying cause. ..
  2. Berl T. Vasopressin antagonists. N Engl J Med. 2015;372:2207-16 pubmed publisher
  3. Mantovani E, Pirrone M, Spanu P, Albicini M, Gandola A, Ottolina D, et al. Hypo-osmolar fluid absorption in endoscopic resection: a new pharmacological approach. Minerva Anestesiol. 2015;81:591-2 pubmed
  4. Kajimoto K, Abe T. Blood urea nitrogen as a marker of the acute response to addition of tolvaptan to standard therapy in patients hospitalized for acute heart failure syndromes. Int J Cardiol. 2014;177:589-91 pubmed publisher
  5. Mahnensmith R. Novel treatments of autosomal dominant polycystic kidney disease. Clin J Am Soc Nephrol. 2014;9:831-6 pubmed publisher
  6. Lee J, Kilonzo K, Nistico A, Yeates K. Management of hyponatremia. CMAJ. 2014;186:E281-6 pubmed publisher
  7. Goldsmith S. Hyponatremia and outcomes in patients with heart failure. Heart. 2012;98:1761-2 pubmed publisher
  8. Clark W, Devuyst O, Roussel R. The vasopressin system: new insights for patients with kidney diseases: Epidemiological evidence and therapeutic perspectives. J Intern Med. 2017;282:310-321 pubmed publisher
  9. Zeynalov E, Jones S, Elliott J. Therapeutic time window for conivaptan treatment against stroke-evoked brain edema and blood-brain barrier disruption in mice. PLoS ONE. 2017;12:e0183985 pubmed publisher
    ..Our experimental data open new possibilities to repurpose conivaptan, and make an important "bench-to-bedside translation" of the results into clinical practice. ..
  10. Janovick J, Spicer T, Bannister T, Scampavia L, Conn P. Pharmacoperone rescue of vasopressin 2 receptor mutants reveals unexpected constitutive activity and coupling bias. PLoS ONE. 2017;12:e0181830 pubmed publisher
    ..These results suggest that particular rescued receptor mutants show functional characteristics that differ from the WT receptor; a finding that may be important to consider as pharmacoperones are developed as therapeutic agents. ..
  11. Nomoto H, Satoh Y, Kamiyama M, Yabe K, Masumura M, Sakakibara A, et al. Mechanisms of Diuresis for Acute Decompensated Heart Failure by Tolvaptan. Int Heart J. 2017;58:593-600 pubmed publisher
    ..002-5.668 × ?ECW/ICW, r2 = 0.306, P = 0.002).Our findings suggest that WRF is caused by a reduction in intravascular volume and that tolvaptan treatment can decrease the excess volume while maintaining intravascular volume. ..
  12. Martínez Archundia M, Colín Astudillo B, Moreno Vargas L, Ramírez Galicia G, Garduño Juárez R, Deeb O, et al. Ligand recognition properties of the vasopressin V2 receptor studied under QSAR and molecular modeling strategies. Chem Biol Drug Des. 2017;90:840-853 pubmed publisher
    ..The results suggest that the proposed QSAR models can reliably predict the reproductive toxicity potential of diverse chemicals, and they can be useful tools for screening new chemicals for safety assessment. ..
  13. Gralla R, Ahmad F, Blais J, Chiodo J, Zhou W, Glaser L, et al. Tolvaptan use in cancer patients with hyponatremia due to the syndrome of inappropriate antidiuretic hormone: a post hoc analysis of the SALT-1 and SALT-2 trials. Cancer Med. 2017;6:723-729 pubmed publisher
    ..In this post hoc study of the SALT trial population, oral tolvaptan was an effective and safe therapy for the treatment of hyponatremia in subjects with SIADH and cancer. ..
  14. Rehberg S, Grundling M, Ertmer C. VANISH: a challenge for current sepsis guidelines!. Crit Care. 2016;20:348 pubmed
  15. Harbeck B, Lindner U, Haas C. Low-dose tolvaptan for the treatment of hyponatremia in the syndrome of inappropriate ADH secretion (SIADH). Endocrine. 2016;53:872-3 pubmed publisher
  16. Ramamohan V, Mladsi D, Ronquest N, Kamat S, Boklage S. An economic analysis of tolvaptan compared with fluid restriction among hospitalized patients with hyponatremia. Hosp Pract (1995). 2017;45:111-117 pubmed publisher
  17. Katz D, Locke C, Greco N, Liu W, Tracy K. Hypothalamic-pituitary-adrenal axis and depression symptom effects of an arginine vasopressin type 1B receptor antagonist in a one-week randomized Phase 1b trial. Brain Behav. 2017;7:e00628 pubmed publisher
    ..47-1.86, p < 0.01) but not on HAM-D-17. The results support further clinical study of the antidepressant potential of ABT-436. ..
  18. Tanaka A, Nakamura T, Sato E, Node K. Aquaporin-2 is a potential biomarker for tolvaptan efficacy in decompensated heart failure complicated by diabetic nephrotic syndrome. Int J Cardiol. 2016;210:1-3 pubmed publisher