The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 18, 1982

Filed:

Mar. 02, 1978
Applicant:
Inventor:

Choh H Li, Berkeley, CA (US);

Assignee:

Hoffmann-La Roche Inc., Nutley, NJ (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07C / ;
U.S. Cl.
CPC ...
2601 / ;
Abstract

The solid-phase syntheses of [Ala.sup.2 ]-, [D-Leu.sup.2 ]-, [D-Lys.sup.2 ], [Leu.sup.5 ]- and [D-Ala.sup.2, D-Leu.sup.5 ] .beta.-endorphins are described. The synthetic peptides were purified by chromatography on carboxymethylcellulose and partition chromatography on Sephadex G-50. They were characterized by partition chromatography on agarose, thin-layer chromatography, paper electrophoresis, and amino acid analyses of acid and enzymic hydrolysates. Bioassay of the synthetic analogs for analgesic activity by the tail-flick-method showed the D-Leu.sup.2 analog to be 48% as potent as .beta..sub.h -endorphin while the Ala.sup.2, D-Lys.sup.2, Leu.sup.5, and [D-Ala.sup.2, D-Leu.sup.5 ] analogs were 8 to 17% as active.


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