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Title: Effects of an orally active vasopressin V1 receptor antagonist.
Austin Authors: Burrell, Louise M ;Phillips, P A;Stephenson, J;Risvanis, John;Hutchins, A M;Johnston, Colin I
Affiliation: Medicine (University of Melbourne)
Issue Date: 1-May-1993
Publication information: Clinical and Experimental Pharmacology & Physiology; 20(5): 388-91
Abstract: 1. This paper reports on the in vitro and in vivo characteristics of a non-peptide vasopressin V1 receptor antagonist 1-(1-[4-(3-acetylaminopropoxy)benzoyl]-4-piperidyl)-3,4-dihydro-2( 1H)- quinolinone (OPC-21268). 2. OPC-21268 caused a concentration-dependent displacement of the selective V1 receptor antagonist radioligand, [125I]-[d(CH2)5, sarcosine7]AVP from vasopressin V1 receptors in rat liver and kidney membranes, inhibitory concentration of 50% (IC50) 4 x 10(-8), 0.3 mol/L liver and 1.5 x 10(-8), 0.2 mol/L kidney. OPC-21268 had little effect on the selective V2 antagonist radioligand [3H]desGly-NH2(9)-d(CH2)5[D-Ileu2, Ileu4]AVP binding to V2 receptors in renal membranes (IC50 > 10(-4) mol/L). 3. After oral administration to rats, OPC-21268 was an effective V1 antagonist to both liver and kidney V1 receptors, in a dose-dependent manner. 4. These studies confirm that OPC-21268 is a potent non-peptide, orally effective V1 vasopressin receptor antagonist.
Journal: Clinical and Experimental Pharmacology & Physiology
Type: Journal Article
Subjects: Administration, Oral
Antidiuretic Hormone Receptor Antagonists
Arginine Vasopressin.analogs & derivatives.metabolism
Binding Sites
Dose-Response Relationship, Drug
In Vitro Techniques
Kidney.drug effects.metabolism
Liver.drug effects.metabolism
Piperidines.administration & dosage.pharmacology
Quinolones.administration & dosage.pharmacology
Rats, Sprague-Dawley
Receptors, Vasopressin.metabolism
Appears in Collections:Journal articles

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