β-ENDORPHIN: SYNTHESIS AND MORPHINE-LIKE ACTIVITY OF ANALOGS WITH D-AMINO ACID RESIDUES IN POSITIONS 1, 2, 4 AND 5
Donald Yamashiro
Hormone Research Laboratory, University of California, San Francisco, California, U.S.A.
Search for more papers by this authorLiang-Fu Tseng
Department of Pharmacology, University of California, San Francisco, California, U.S.A.
Search for more papers by this authorByron A. Doneen
Hormone Research Laboratory, University of California, San Francisco, California, U.S.A.
Search for more papers by this authorHorace H. Loh
Department of Pharmacology, University of California, San Francisco, California, U.S.A.
Search for more papers by this authorCorresponding Author
Dr. Choh Hao Li
Hormone Research Laboratory, University of California, San Francisco, California, U.S.A.
Hormone Research Laboratory University of California San Francisco, California 94143 U.S.A.Search for more papers by this authorDonald Yamashiro
Hormone Research Laboratory, University of California, San Francisco, California, U.S.A.
Search for more papers by this authorLiang-Fu Tseng
Department of Pharmacology, University of California, San Francisco, California, U.S.A.
Search for more papers by this authorByron A. Doneen
Hormone Research Laboratory, University of California, San Francisco, California, U.S.A.
Search for more papers by this authorHorace H. Loh
Department of Pharmacology, University of California, San Francisco, California, U.S.A.
Search for more papers by this authorCorresponding Author
Dr. Choh Hao Li
Hormone Research Laboratory, University of California, San Francisco, California, U.S.A.
Hormone Research Laboratory University of California San Francisco, California 94143 U.S.A.Search for more papers by this authorAbstract
The solid-phase syntheses of [D-Tyr1]-, [D-Ala2]-, [D-Phe4]-, and [D-Met5]-βc-endorphins are described. A comparison of certain methods of purification and criteria of homogeneity is made with the use of these compounds. Bioassay of these synthetic analogs both in vitro and in vivo show that [D-Ala2]-βc-endorphin possesses significant opiate activity whereas the other analogs have minimal activity.
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