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The 2-nitro-4-azidophenyl(NAP)-D-Ala2-Leu5-Enkephalin derivatives: Try-D-Ala-Gly-Phe-Leu CONCH2CH2NH-NAP (E-NAP-EDA) and Try-D-Ala-Gly-Phe-Leu CONCH2CH2NH-COCH2CH2NHNAP(E-NAP- -Ala-EDA) were synthesized by conventional peptide methods. Their structure was determined by amino acid analysis, ultra violet, visible and infra red spectroscopy. Both peptides were shown a) to bind with high affinity to the opiate receptors of rat brain membranes and b) to inhibit strongly the contractions of electrically stimulated vas deferens and the adenyl cyclase of the NG 108-15 cell membranes. These effects were reversed by the antagonist naloxone. Photoloysis of the rat brain membranes-(E-NAP- -Ala-EDA) complex caused a 20-30% inactivation of the opiate receptors. Inactivation was prevented when the complex was irradiated in the presence of naloxone. The radio-labeled derivatives of these enkephalin analogs may prove useful photochemical labels of the opiate receptor.
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
January 1982,
Peptides,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
January 1977,
Naunyn-Schmiedeberg's archives of pharmacology,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
June 1989,
Clinical and experimental pharmacology & physiology,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
January 1983,
Farmakologiia i toksikologiia,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
January 1981,
Pharmacology & therapeutics,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
February 1978,
Federation proceedings,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
January 1978,
Arzneimittel-Forschung,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
January 1978,
Advances in biochemical psychopharmacology,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
January 1988,
Proceedings of the Chinese Academy of Medical Sciences and the Peking Union Medical College = Chung-kuo i hsueh k'o hsueh yuan, Chung-kuo hsieh ho i k'o ta hsueh hsueh pao,
C Zioudrou, and
D Varoucha, and
S Loukas, and
R A Streaty, and
W A Klee
April 1983,
Science (New York, N.Y.),
