[Effects of analogues and drugs on arginine vasopressin receptor binding in rat renal tubular basolateral membrane].
The methods of basolateral membrane isolation from rat kidney and 3H-AVP receptor assay using this basolateral membrane preparation were established. Then, the effects of analogues and drugs on AVP-receptor binding were studied. Specific 3H-AVP binding was inhibited by LVP, dDAVP and oxytocin in that order. Among the various agonistic or antagonistic drugs to AVP (fluoride, cyclophosphamide, mechlorethamine, chlorpropamide), only chlorpropamide inhibited 3H-AVP binding to the membrane. The Kd value calculated by Scatchard analysis was 1.30 +/- 0.28 nM (n = 4, M +/- SD), and it was increased to 2.69 +/- 0.32 nM (n = 5, M +/- SD) by adding 1 mM of chlorpropamide, while Bmax was unchanged. Our data show that 1 mM chlorpropamide decreases receptor affinity for AVP, and alters AVP-receptor binding in a competitive manner.
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Second Department of Internal Medicine, School of Medicine, University of Occupational and Environmental Health, Kitakyushu, Japan.
D000818:Animals; D001127:Arginine Vasopressin / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000378:metabolism*; D001485:Basement Membrane / Q000187:drug effects / Q000378:metabolism; D001667:Binding, Competitive; D002747:Chlorpropamide / Q000494:pharmacology*; D007684:Kidney Tubules / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D011485:Protein Binding / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011945:Receptors, Angiotensin / Q000187:drug effects* / Q000378:metabolism; D017483:Receptors, Vasopressin
D011945:Receptors, Angiotensin; D017483:Receptors, Vasopressin; D001127:Arginine Vasopressin; D002747:Chlorpropamide