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Mechanism of action and structural requirements of vasopressin analog inhibition of transepithelial water flux in toad urinary bladder

WA Mann, F Stassen, W Huffman and LB Kinter

Vasopressin, vasopressin analogs, forskolin and 8-bromo-cyclic AMP (8Br- cAMP) were studied for their effects on transepithelial water flux in toad urinary bladder. Arginine vasopressin, arginine vasotocin, oxytocin, desamino-8-D arginine vasopressin, forskolin and 8Br-cAMP stimulated hydro-osmotic water flux in a dose-dependent fashion. The rank order of potency was arginine vasotocin greater than arginine vasopressin greater than oxytocin greater than desamino-8-D-arginine vasopressin greater than forskolin greater than 8Br-cAMP. The vasopressin analogs [1-(beta-mercapto-beta,beta-cyclopentamethylene propionic acid),2-(O-methyl)tyrosine,8-arginine]vasopressin (SK&F 100273), [1-(beta-mercapto-beta,beta-cyclopentamethylene propionic acid),2-(O-methyl)tyrosine,4-valine,8-arginine]vasopressin (SK&F 100501), [1-(beta-mercapto-beta,beta-cyclopentamethylene propionic acid),2-D-tyrosine,4-valine,8-arginine]vasopressin (SK&F 100885), [1- (beta-mercapto-beta,beta-cyclopentamethylene propionic acid),2-(O- ethyl)tyrosine,4-valine,8-arginine]vasopressin (SK&F 100398), [1-(beta- mercapto-beta,beta-cyclopentamethylene propionic acid),2-D-isoleucine,4- valine,8-arginine]vasopressin (SK&F 101485), [1-(beta-mercapto- beta,beta-cyclopentamethylene propionic acid),2-(O-ethyl)-tyrosine,4- valine,8-arginine]vasopressin (SK&F 101498), [1-(beta-mercapto- beta,beta-cyclopentamethylene propionic acid),2-(O-ethyl)D-tyrosine,4- valine,8-arginine,9-desglycine]vasop ressin (SK&F 101926) and [1-(beta- mercapto-beta-beta-cyclopentamethylene propionic acid),2-D- phenylalanine,4-valine,8-arginine] vasopressin (SK&F 101071) antagonized arginine vasopressin-stimulated water flux and displaced the agonist dose-response relationship to the right in a parallel fashion. The most potent antagonists were those having the (O-ethyl)-D- tyrosine substitution at position 2. None of the antagonists tested had any effect on 8Br-cAMP-stimulated water flux at concentrations up to 10(-6)M.(ABSTRACT TRUNCATED AT 250 WORDS)

Volume 238, Issue 2, pp. 401-406, 08/01/1986
Copyright © 1986 by American Society for Pharmacology and Experimental Therapeutics






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Copyright © 1986 by the American Society for Pharmacology and Experimental Therapeutics.