A synthetic method suitable for the rapid preparation of 13N-labeled dermorphin analogue, H-Tyr-D-Met(O)-Phe-Gly-NH2 (SD-62)

A synthetic method suitable for the rapid preparation of 13N-labeled dermorphin analogue, H-Tyr-D-Met(O)-Phe-Gly-NH2 (SD-62)

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 [13N]ammonia,...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 1991, Vol.39 (10), p.2734-2736
Hauptverfasser: KISO, Y, IINUMA, S, MIMOTO, T, SAJI, H, YOKOYAMA, A, AKAJI, K
Format: Artikel
Sprache:eng
Schlagworte:
Analgesics, Opioid - chemical synthesis
Analgesics, Opioid - metabolism
Brain - metabolism
Chemistry
Exact sciences and technology
Hydrolysis
Nitrogen Radioisotopes
Oligopeptides - chemical synthesis
Oligopeptides - metabolism
Opioid Peptides
Organic chemistry
Peptides
Preparations and properties
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Zusammenfassung: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 [13N]ammonia, was administered into mice, the time profile of the radioactivity accumulation in the brain paralleled well that of the analgesic activity.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.39.2734