ISSN:
0018-019X
Keywords:
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
The synthesis and biological testing of analogues of Met-enkephalin, a recently discovered opioid peptide from mammalian brain, are described. Testing involved determination of affinity constants for an opiate receptor site and of analgesic potency in the tail-flick test in mouse. The effects on opioid activity of modifying various parts of the enkephalin molecule are discussed. Tyr-D-Ala-Gly-MePheMet (O)-olThe ending -ol added to the symbol of an amino acid designates the aminoalcohol obtained by reduction of the α-carboxyl group of the amino acid. (FK 33-824), which was highly active in these tests, was subsequently selected for clinical testing.The use of two complementary models - in vitro binding studies and in vivo test for analgesia - for the assessment of biological activity in the evaluation of analogues is explained.
Additional Material:
2 Tab.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/hlca.19790620206
Permalink
