scholarly journals A Novel Vasopressin Dual V1A/V2 Receptor Antagonist, Conivaptan Hydrochloride, Improves Hyponatremia in Rats with Syndrome of Inappropriate Secretion of Antidiuretic Hormone (SIADH)

2007 ◽  
Vol 30 (1) ◽  
pp. 91-95 ◽  
Author(s):  
Koh-ichi Wada ◽  
Utane Matsukawa ◽  
Akira Fujimori ◽  
Yukinori Arai ◽  
Katsumi Sudoh ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Antidiuretic Hormone ◽  
Inappropriate Secretion ◽  
V2 Receptor ◽  
V2 Receptor Antagonist

scholarly journals A new selective, and sensitive method for the determination of lixivaptan, a vasopressin 2 (V2)-receptor antagonist, in mouse plasma and its application in a pharmacokinetic study

2018 ◽  
Vol 16 (1) ◽  
pp. 614-620
Author(s):  
Haitham Alrabiah ◽  
Mohammed Abunassif ◽  
Sabry Attia ◽  
Gamal Abdel-Hafiz Mostafa
Keyword(s):  
Receptor Antagonist ◽  
Pharmacokinetic Study ◽  
Limit Of Detection ◽  
Internal Standard ◽  
Hplc Method ◽  
Maximum Plasma ◽  
Mouse Plasma ◽  
V2 Receptor ◽  
V2 Receptor Antagonist

AbstractA new, selective and sensitive HPLC method for the determination of lixivaptan, an oral selective vasopressin 2 (V2)-receptor antagonist, was investigated and validated. A Waters symmetry C18 column was used as a stationary phase in isocratic elution mode using a mobile phase composed of KH2PO4 (100 mM)-acetonitrile (40: 60, v/v) at a flow rate of 1.5 mL min-1. Diclofenac was used as the internal standard (IS). Lixivaptan and the IS were extracted from plasma by protein precipitation and were detected at 260 nm. Lixivaptan and diclofenac were eluted at 3.6 and 6.2 min, respectively. The developed method showed good linearity over the calibration range of 50 -1000 ng mL-1 with a lower limit of detection of 16.5 ng mL-1. The extraction percentage of lixivaptan in the mouse plasma was in the range of 88.88 - 114.43%, which indicates acceptable extraction. The aforementioned method was validated according to guidelines of the International Council on Harmonization (ICH). The intra- and inter-day coefficients of variation did not exceed 5.5%. This method was presented to be simple, sensitive, and accurate and was successfully adapted in a pharmacokinetic study of the profile of lixivaptan in mouse plasma. A mean maximum plasma concentration of lixivaptan of 113.82 ng mL-1 was achieved in 0.5 h after oral administration of a 10 mg kg-1 dose in mouse as determined using the developed method.

Arginine vasopressin produces renal vasodilation via V2 receptors in conscious dogs

1993 ◽  
Vol 265 (4) ◽  
pp. R934-R942 ◽  
Author(s):  
M. Naitoh ◽  
H. Suzuki ◽  
M. Murakami ◽  
A. Matsumoto ◽  
A. Ichihara ◽  
...  
Keyword(s):  
Cardiac Output ◽  
Receptor Antagonist ◽  
Arginine Vasopressin ◽  
Statistical Significance ◽  
Conscious Dogs ◽  
Receptor Blockade ◽  
Vasodilatory Response ◽  
V2 Receptor ◽  
Plasma Arginine ◽  
V2 Receptor Antagonist

In conscious dogs, 36-h water deprivation induced a significant increase in renal blood flow (RBF) with elevation of the plasma arginine vasopressin (AVP) concentration to 9.6 +/- 1.8 pg/ml. To simulate such a condition, a mild elevation of plasma AVP was produced by infusing AVP intravenously at a dose of 0.1 ng.kg-1.min-1 for 20 min. The plasma AVP concentration then increased to 6.8 +/- 0.7 pg/ml. This dose of AVP increased the RBF by 21.7 +/- 2.6% and decreased the renal vascular resistance by 18.1 +/- 2.3% without significant changes in mean arterial pressure, cardiac output, or heart rate. The mechanism of this renal vasodilatory action was examined using newly developed, orally effective, selective AVP antagonists OPC-21268 (a V1-receptor antagonist) and OPC-31260 (a V2-receptor antagonist). In 36-h water-deprived dogs, V2-receptor blockade with OPC-31260 significantly decreased the RBF by 20.5 +/- 2.6% without significant changes in cardiac output. The exogenous AVP-induced renal vasodilatory response tended to be augmented when V1 receptors were blocked by pretreatment with OPC-21268, but the change did not achieve statistical significance. On the other hand, V2-receptor blockade by either pretreatment with OPC-31260 or simultaneous infusion of OPC-31260 inhibited this vasodilatory response. Furthermore, intravenous infusion of 1-desamino-8-D-arginine vasopressin (DDAVP) at a dose of 0.3 ng.kg-1 x min-1 for 20 min significantly increased the RBF by 36.5 +/- 1.7%, and this DDAVP-induced renal vasodilation was inhibited by simultaneous infusion of V2-receptor antagonist.(ABSTRACT TRUNCATED AT 250 WORDS)

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 V2 Receptor Antagonist; Tolvaptan

2011 ◽  
Vol 9 (2) ◽  
pp. 50 ◽  
Author(s):  
Joo-Hark Yi ◽  
Hyun-Jong Shin ◽  
Ho-Jung Kim
Keyword(s):  
Receptor Antagonist ◽  
V2 Receptor ◽  
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
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