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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
1980-9-26
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pubmed:abstractText |
The synthesis of N-acetyl-[2-(O-methyl)tyrosine]arginine-vasopressin [Ac-Tyr(Me)AVP] was undertaken utilizing a combination of the stepwise active ester and fragment condensation methods. Ac-Tyr(Me)AVP is an antagonist of the vasopressor response to vasopressin (pA2 = 7.18 +/- 0.08), devoid of vasopressor agonist activity, and has an antidiuretic potency of 0.026 +/- 0.002 unit/mg, a 15 000-fold decrease over the antidiuretic activity of [2-(O-methyl)tyrosine]arginine-vasopressin. The analogue is also an antagonist of the in vitro uterotonic activity of oxytocin with pA2 values of 7.29 +/- 0.08 in the absence of Mg2+ and 6.73 +/- 0.14 in 0.5 mM Mg2+. This result of Nalpha-acetylation of Tyr(Me)AVP parallels similar results in the oxytocin series and suggests that this substitution should be considered in the design of potential antagonists of the antidiuretic response to vasopressin.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
23
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
696-8
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:7392038-Animals,
pubmed-meshheading:7392038-Arginine Vasopressin,
pubmed-meshheading:7392038-Blood Pressure,
pubmed-meshheading:7392038-Diuresis,
pubmed-meshheading:7392038-Female,
pubmed-meshheading:7392038-Rats,
pubmed-meshheading:7392038-Uterine Contraction,
pubmed-meshheading:7392038-Vasopressins
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pubmed:year |
1980
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pubmed:articleTitle |
N-Acetyl-[2-(O-methyl)tyrosine]arginine-vasopressin, an interesting antagonist of the vasopressor response to vasopressin.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, U.S. Gov't, P.H.S.
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