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rdf:type | |
lifeskim:mentions | |
pubmed:dateCreated |
1979-12-27
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pubmed:abstractText |
As part of a program to prepare bradykinin (H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH) labelled at high specific radioactivities, we have synthesized three analogs for dehalogenation in tritium gas: [4-Br-Phe5]-bradykinin (BK), [4-Br-Phe8]-BK and [4-Br-Phe5,8]-BK. The analogs were synthesized by the Merrifield solid-phase method and were purified by molecular sieve and partition chromatography. The analogs themselves possess biological activity (as assayed for effects on mean arterial blood pressure and isolated rat uterus). [4-Br-Phe8]-BK was 1.5 to 3 times as active as bradykinin. [4-Br-Phe5,8]-BK was approx. 22% as active as BK and [4-Br-Phe5]-BK was approx. 18% as active. [4-Br-Phe5]-BK was submitted to catalytic dehalogenation with 10% Pd/C and 5% Rh/CaCO3 in H2O and DMF (1:1) plus 10 Ci of 3H2. [4-3H-Phe5]-BK was obtained at 6.7 Ci/mmole in an overall yield of 15%. [4-3H-Phe8]-BK was prepared similarly to yield an intrinsically-labelled peptide with a specific radioactivity of 21 Ci/mmole.
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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:issn |
0065-2598
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
120A
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
39-50
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:495324-Animals,
pubmed-meshheading:495324-Biological Assay,
pubmed-meshheading:495324-Blood Pressure,
pubmed-meshheading:495324-Bradykinin,
pubmed-meshheading:495324-Female,
pubmed-meshheading:495324-Kinins,
pubmed-meshheading:495324-Muscle Contraction,
pubmed-meshheading:495324-Rats,
pubmed-meshheading:495324-Structure-Activity Relationship,
pubmed-meshheading:495324-Tritium,
pubmed-meshheading:495324-Uterus
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pubmed:year |
1979
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pubmed:articleTitle |
Preparation of intrinsically-labelled kinins.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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