A Synthetic Method Suitable for the Rapid Preparation of 13N-Labeled Dermorphin Analogue, H-Try-D-Met(O)-Phe-Gly-NH2 (SD-62)

Yoshiaki KISO; Satoshi IINUMA; Tsutomu MIMOTO; Hideo SAJI; Akira YOKOYAMA; Kenichi AKAJI

doi:10.1248/cpb.39.2734

A Synthetic Method Suitable for the Rapid Preparation of ¹³N-Labeled Dermorphin Analogue, H-Try-D-Met(O)-Phe-Gly-NH₂ (SD-62)

Yoshiaki KISO, Satoshi IINUMA, Tsutomu MIMOTO, Hideo SAJI, Akira YOKOYAMA, Kenichi AKAJI

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Keywords: positron emission tomography, dermorphin analogue, peptide synthesis, ^<13>N ammonia, active ester ammonolysis, brain uptake, analgestic activity

JOURNAL FREE ACCESS

1991 Volume 39 Issue 10 Pages 2734-2736

DOI https://doi.org/10.1248/cpb.39.2734

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Abstract

A synthetic method suitable for the preparation of ¹³N-labeled dermorphin analogue, H-Tyr-D-Met(O)-Phe-Gly-NH₂ (SD-62), was established; i.e., SD-62 was synthesized by a 5 min treatment of the active ester precursor with ammonia. When the ¹³N-labeled SD-62, prepared by this method with [¹³]ammonia, was administered into mice, the time profile of the radioactivity accumulation in the brain paralleled well that of the analgesic activity.

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