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Citations to this article

Potent aquaretic agent. A novel nonpeptide selective vasopressin 2 antagonist (OPC-31260) in men.
A Ohnishi, … , Y Yabuuchi, T Tanaka
A Ohnishi, … , Y Yabuuchi, T Tanaka
Published December 1, 1993
Citation Information: J Clin Invest. 1993;92(6):2653-2659. https://doi.org/10.1172/JCI116881.
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Research Article

Potent aquaretic agent. A novel nonpeptide selective vasopressin 2 antagonist (OPC-31260) in men.

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Abstract

Solute-free water diuretics (aquaretics) by antagonizing hydrosmotic vasopressin receptors (V2) may be useful in treating water-retaining diseases. The effects of intravenous administration of a newly developed nonpeptide, selective V2 antagonist, OPC-31260, at doses ranging from 0.017 to 1.0 mg/kg to groups of healthy, normally hydrated men were compared with those of 0.33 mg/kg furosemide and placebo. OPC-31260 increased the hypotonic urine volume dose dependently for the first 4 h, while furosemide induced sodium diuresis for 2 h. The absolute increase in the cumulative response in the urine to the highest doses of OPC-31260 was not significantly different from that to furosemide. The higher doses of OPC-31260 rapidly lowered urine osmolality for 2 h, particularly between minutes 15 and 45 (e.g., 1.0-mg/kg dose: 63 +/- 2 mOsm/kg in urine collected between minutes 30 and 45). In a marked hypotonic diuresis, mean free water clearance of the 4-h urine increased dose proportionally into the positive range, reaching 1.80 +/- 0.21 ml/min at 1.0 mg/kg. Whereas furosemide induced marked Na and K diuresis, OPC-31260 increased urinary Na excretion only slightly. At 4 h, 0.75 and 1.0 mg/kg of OPC-31260 almost doubled the plasma arginine vasopressin; and the higher doses increased plasma osmolality and plasma Na slightly, but did not alter plasma K, blood pressure, or heart rate. OPC-31260 thus safely induced a potent aquaretic effect in men.

Authors

A Ohnishi, Y Orita, R Okahara, H Fujihara, T Inoue, Y Yamamura, Y Yabuuchi, T Tanaka

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Total citations by year

Year: 2023 2022 2021 2019 2018 2017 2016 2015 2014 2013 2012 2011 2010 2009 2008 2007 2006 2005 2004 2003 2002 2001 2000 1999 1998 1997 1996 1995 1994 1983 Total
Citations: 2 3 1 1 1 3 3 5 2 6 5 3 4 4 5 2 7 2 1 6 4 2 9 4 7 4 6 3 1 1 107
Citation information
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Citations to this article in year 2011 (3)

Title and authors Publication Year
Vaptans for the treatment of hyponatremia
GL Robertson
Nature Reviews Endocrinology 2011
Annual Reports in Medicinal Chemistry
JJ Liu, TW Lee
Annual Reports in Medicinal Chemistry Volume 46 2011
Efficacy and safety of oral tolvaptan therapy in patients with the syndrome of inappropriate antidiuretic hormone secretion
JG Verbalis, S Adler, RW Schrier, T Berl, Q Zhao, FS Czerwiec
European Journal of Endocrinology 2011

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