Practical Synthesis of Both Enantiomers of Vasopressin V2 Receptor Antagonist OPC-41061 Using the Catalytic Asymmetric Hydrogenation

Heterocycles ◽  
2002 ◽  
Vol 56 (1-2) ◽  
pp. 123 ◽  
Author(s):  
Hiroshi Yamashita ◽  
Tadaaki Ohtani ◽  
Seiji Morita ◽  
Kenji Otsubo ◽  
Keizo Kan ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Asymmetric Hydrogenation ◽  
Vasopressin V2 Receptor ◽  
V2 Receptor ◽  
Vasopressin V2 Receptor Antagonist ◽  
Practical Synthesis ◽  
Catalytic Asymmetric ◽  
Catalytic Asymmetric Hydrogenation ◽  
V2 Receptor Antagonist

Effect of SR121463, a Selective Non-Peptide Vasopressin V2 Receptor Antagonist, in a Rabbit Model of Ocular Hypertension

2000 ◽  
Vol 16 (3) ◽  
pp. 203-216 ◽  
Author(s):  
FREDERIC LACHERETZ ◽  
ALAIN BARBIER ◽  
CLAUDINE SERRADEIL-LE GAL ◽  
PIERRE-PAUL ELENA ◽  
JEAN-PIERRE MAFFRAND ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ocular Hypertension ◽  
Rabbit Model ◽  
Vasopressin V2 Receptor ◽  
V2 Receptor ◽  
Vasopressin V2 Receptor Antagonist ◽  
V2 Receptor Antagonist

scholarly journals OPC-31260, a nonpeptide vasopressin V2 receptor antagonist is a novel aquaretic agent

1992 ◽  
Vol 58 ◽  
pp. 195
Author(s):  
Shigeki Nakamura ◽  
Yoshitaka Yamamura ◽  
Hidenori Ogawa ◽  
Tomihiko Chihara ◽  
Toshiyuki Onogawa ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Vasopressin V2 Receptor ◽  
V2 Receptor ◽  
Vasopressin V2 Receptor Antagonist ◽  
V2 Receptor Antagonist

scholarly journals FP051DETERMINANTS OF URINE VOLUME IN ADPKD-PATIENTS USING THE VASOPRESSIN V2 RECEPTOR ANTAGONIST TOLVAPTAN

2018 ◽  
Vol 33 (suppl_1) ◽  
pp. i64-i65
Author(s):  
Bart Kramers ◽  
Judith Heida ◽  
Wendy Boertien ◽  
Maatje van Gastel ◽  
Esther Meijer ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Urine Volume ◽  
Vasopressin V2 Receptor ◽  
V2 Receptor ◽  
Vasopressin V2 Receptor Antagonist ◽  
V2 Receptor Antagonist

Vasopressin V2 Receptor Antagonist Inhibits Cardiac Remodeling with Old Myocardial Infarction in Rats

2011 ◽  
Vol 17 (9) ◽  
pp. S149-S150
Author(s):  
Takanori Yamazaki ◽  
Yasuhiro Nakamura ◽  
Yasukatsu Izumi ◽  
Akihisa Hanatani ◽  
Takashi Muro ◽  
...  
Keyword(s):  
Myocardial Infarction ◽  
Receptor Antagonist ◽  
Cardiac Remodeling ◽  
Vasopressin V2 Receptor ◽  
Old Myocardial Infarction ◽  
V2 Receptor ◽  
Vasopressin V2 Receptor Antagonist ◽  
V2 Receptor Antagonist

scholarly journals Therapeutic Effects of Tolvaptan, a Potent, Selective Nonpeptide Vasopressin V2 Receptor Antagonist, in Rats with Acute and Chronic Severe Hyponatremia

Endocrinology ◽  
2005 ◽  
Vol 146 (7) ◽  
pp. 3037-3043 ◽  
Author(s):  
Toshiki Miyazaki ◽  
Yoshitaka Yamamura ◽  
Toshiyuki Onogawa ◽  
Shigeki Nakamura ◽  
Shizuo Kinoshita ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Water Content ◽  
Animal Behavior ◽  
Neurological Symptoms ◽  
Plasma Sodium ◽  
Severe Hyponatremia ◽  
Vasopressin V2 Receptor ◽  
V2 Receptor ◽  
Vasopressin V2 Receptor Antagonist ◽  
V2 Receptor Antagonist

Abstract The therapeutic efficacy of tolvaptan (OPC-41061), a potent, selective nonpeptide vasopressin V2 receptor antagonist, on acute and chronic severe hyponatremia was assessed in rats. Experiments were designed to demonstrate the efficacy of tolvaptan reducing mortality in an acute model, and controlling the extent of serum sodium elevation without causing abnormal animal behavior suggesting neurological symptoms in a chronic model. In the acute model, rats developed rapidly progressive, severe hyponatremia by continuous sc infusion of [deamino-Cys1, d-Arg8]-vasopressin (10 ng/h) and forced water-loading (additional 10% initial body weight per day). By d 6, untreated rats had a 47% mortality rate. However, rats treated with repeated oral administrations of tolvaptan (1, 3, and 10 mg/kg) produced dose-dependent aquaresis (i.e. urine volume increased and urine osmolality decreased) that resulted in a gradual increase in plasma sodium concentration. Consequently, tolvaptan treatment reduced mortality and, at higher doses, resulted in no observed deaths. In the gradual model, rats receiving a continuous sc infusion of [deamino-Cys1, d-Arg8]-vasopressin (1 ng/h) combined with a liquid diet were induced to stable, severe hyponatremia (∼110 mEq/liter), which lead to increased organ weight and water content. Rats receiving dose titrations of tolvaptan (0.25, 0.5, 1, 2, 4, and 8 mg/kg) increased plasma sodium to healthy levels without causing abnormal animal behavior suggesting neurological symptoms or death, improved hyponatremia-driven increases in wet weight and water content in the organs. Thus, in animal models, analogous to the hyponatremia forms seen in humans, tolvaptan presents exciting therapeutic implications in the management of patients with severe hyponatremia.

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