Acute aquaresis by the nonpeptide arginine vasopressin (AVP) antagonist OPC-31260 improves hyponatremia in patients with syndrome of inappropriate secretion of antidiuretic hormone (SIADH).

@article{Saito1997AcuteAB,
  title={Acute aquaresis by the nonpeptide arginine vasopressin (AVP) antagonist OPC-31260 improves hyponatremia in patients with syndrome of inappropriate secretion of antidiuretic hormone (SIADH).},
  author={T. Saito and San‐e Ishikawa and Katsushige Abe and Kyuzi Kamoi and K. Yamada and Kurakazu Shimizu and Takao Saruta and S Yoshida},
  journal={The Journal of clinical endocrinology and metabolism},
  year={1997},
  volume={82 4},
  pages={
          1054-7
        }
}
The present study was undertaken to determine whether the non-peptide V2 arginine vasopressin (AVP) antagonist 5-dimethylamino- 1[4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepi ne hydrochloride (OPC-31260) produces water diuresis and improves hyponatremia in patients with the syndrome of inappropriate secretion of antidiuretic hormone (SIADH). Eleven patients (9 males and 2 females, 64 +/- 3.5 yr) with SIADH were included in the present protocol, which was comprised of 3… 
Effects of an oral vasopressin receptor antagonist (OPC-31260) in a dog with syndrome of inappropriate secretion of antidiuretic hormone.
TLDR
Treatment of a dog with naturally occurring syndrome of inappropriate secretion of antidiuretic hormone with OPC-31260 at 3 mg/kg body weight orally every 12 h resulted in marked aquaresis and significant palliation of clinical signs with no discernible side-effects detected over a 3-year follow-up period.
BSC1 inhibition complements effects of vasopressin V2 receptor antagonist on hyponatremia in SIADH rats.
TLDR
AVP-induced alterations of rBSC1 expression, as well as those of AQP2, are involved in the pathogenesis of SIADH, which limits its therapeutic efficacy by discontinuing the vasopressin escape.
Successful long-term treatment of hyponatremia in syndrome of inappropriate antidiuretic hormone secretion with satavaptan (SR121463B), an orally active nonpeptide vasopressin V2-receptor antagonist.
TLDR
The new oral vasopressin V(2)-receptor antagonist satavaptan adequately corrects mild or moderate hyponatremia in patients with SIADH and has a good safety profile.
Lithium effectively complements vasopressin V2 receptor antagonist in the treatment of hyponatraemia of SIADH rats.
  • I. Kazama, Tomohiro Arata, M. Matsubara
  • Medicine, Biology
    Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association
  • 2007
TLDR
Although the single effect of therapeutic dose of lithium was weak, it effectively and safely compensated for the therapeutic limitations of a low dose of AVP V(2) receptor antagonist for SIADH by reducing AQP2 expression.
A novel vasopressin dual V1A/V2 receptor antagonist, conivaptan hydrochloride, improves hyponatremia in rats with syndrome of inappropriate secretion of antidiuretic hormone (SIADH).
TLDR
Results show that conivaptan improves hyponatremia in rats with SIADH, supporting the therapeutic potential of convaptan in treatment of patients with hypon atremia associated withSIADH.
Tolvaptan, a selective oral vasopressin V2-receptor antagonist, for hyponatremia.
TLDR
In patients with euvolemic or hypervolemic hyponatremia, tolvaptan, an oral vasopressin V2-receptor antagonist, was effective in increasing serum sodium concentrations at day 4 and day 30.
Therapeutic effects of tolvaptan, a potent, selective nonpeptide vasopressin V2 receptor antagonist, in rats with acute and chronic severe hyponatremia.
TLDR
In animal models, analogous to the hyponatremia forms seen in humans, tolvaptan presents exciting therapeutic implications in the management of patients with severe hypon atremia.
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TLDR
It is indicated that there is dilutional hyponatremia in rats receiving dDAVP and 40 ml/day liquid diets, and that OPC-31260 is an effective therapeutic for hypon atremia associated with d DAVP-induced SIADH.
In vivo diuretic effect of a new non-peptide arginine vasopressin antagonist, OPC-31260, in conscious rats.
TLDR
Results indicate that OPC-31260 is an orally effective non-peptide AVP antagonist to the antidiuretic action of AVP in the conscious rat.
Potent aquaretic agent. A novel nonpeptide selective vasopressin 2 antagonist (OPC-31260) in men.
TLDR
OPC-31260 safely induced a potent aquaretic effect in men and increased plasma osmolality and plasma Na slightly, but did not alter plasma K, blood pressure, or heart rate.
Aquaretic effects of the nonpeptide V2 antagonist OPC-31260 in hydropenic humans.
  • K. Shimizu
  • Medicine, Biology
    Kidney international
  • 1995
TLDR
OPC-31260 is demonstrated to be the first V2 antagonist which exhibits water diuresis (aquaresis) in hydropenic humans with endogenous AVP secretion and maximally concentrated urine and will be useful as an aquaretic in the treatment of some types of hyponatremia where there is excess AVP and water retention.
Therapeutic efficacy of the non-peptide AVP antagonist OPC-31260 in cirrhotic rats.
TLDR
A non-peptide arginine vasopressin (AVP) antagonist (OPC-31260) improves the impaired water excretion in rats with experimental liver cirrhosis and urinary osmolality in cirrhotic rats.
Involvement of arginine vasopressin and renal sodium handling in pathogenesis of hyponatremia in elderly patients.
TLDR
Results indicate that AVP is involved in the mechanism for hyponatremia in the elderly patients with SIADH and central salt-wasting syndrome and should be considered to indicate fludrocortisone acetate therapy.
Aquaretic effect of a potent, orally active, nonpeptide V2 antagonist in men.
TLDR
An orally active, nonpeptide, selective V2 antagonist (OPC-31260) was administered in six dose steps to six healthy, normally hydrated men to investigate the aquaretic effects in comparison with 12 placebo-treated control subjects without serious clinical side effects.
Role of water channel AQP-CD in water retention in SIADH and cirrhotic rats.
TLDR
Water channel AQP-CD plays an important role in water retention in pathological states of SIADH and liver cirrhosis, and the blockade of AVP action by OPC-31260 significantly diminished its expression.
The syndrome of inappropriate antidiuretic hormone secretion (SIADH): pathophysiologic mechanisms in solute and volume regulation.
TLDR
It is shown that cumulative sodium balance and aldosterone secretion rates in patients with SIADH are negatively correlated with water intake, and that intracellular osmotically active solute is either lost or "inactivated" in some manner as intrACEllular potassium is replenished.
Effect of vasopressin antagonist on water excretion in inferior vena cava constriction.
TLDR
Two AVP antagonists were used in the IVC rats at the proximal portion of the hepatic vein under the diaphragm and in sham-operated (control) rats to determine a role for AVP in the impaired water excretion in rats with the inferior vena cava constriction.
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