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We studied the effect of an arginine vasopressin (AVP) analogue, (1-[beta-mercapto-beta, beta-cyclopentamethylenepropionic acid],2-O-ethyltyrosine, 4-valine)AVP(d[CH2]5Tyr[Et]VAVP), on the stimulation of adenylate cyclase by various hormones in the isolated nephron segments and 3H-AVP binding to renal papillary membranes from the rat. The net water flux across the renal cortical collecting tubules of the rabbit was also examined. We found that d(CH2)5Tyr(Et)VAVP significantly inhibited adenylate cyclase activation by AVP in cortical, medullary, and papillary collecting tubules and in the medullary thick ascending limb. In contrast, the AVP analogue did not alter the stimulation of adenylate cyclase by parathyroid hormone in the cortical thick ascending limb, by glucagon in the medullary thick ascending limb, and by calcitonin in cortical collecting tubules. In addition, d(CH2)5Tyr(Et)VAVP blocked [3H]AVP binding to renal papillary membranes. The enhanced net water transport induced by AVP in isolated, perfused rabbit cortical collecting tubules also was completely blocked by this AVP analogue. These results indicate that d(CH2)5Tyr(Et)VAVP specifically antagonizes the cellular action of AVP on the medullary thick ascending limb and on the cortical, medullary, and papillary collecting tubules. Evidence is also presented for competitive antagonism as the cellular mechanism of action.
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
July 1983,
Nihon Jinzo Gakkai shi,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
October 1979,
Biochimica et biophysica acta,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
January 1975,
Molecular and cellular endocrinology,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
August 1984,
Neuroendocrinology,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
October 1982,
The Journal of pharmacology and experimental therapeutics,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
January 1986,
The American journal of physiology,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
June 1985,
Bollettino della Societa italiana di biologia sperimentale,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
September 1982,
Molecular pharmacology,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
November 1978,
Molecular pharmacology,
J K Kim, and
M A Dillingham, and
S N Summer, and
S Ishikawa, and
R J Anderson, and
R W Schrier
January 1980,
Biochemical pharmacology,
