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, was administered into mice, the time profile of the radioactivity accumulation in the brain paralleled well that of the analgesic activity.
Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Japan.
Y
Y
Kiso
S
S
Iinuma
T
T
Mimoto
H
H
Saji
A
A
Yokoyama
K
K
Akaji
D000701:Analgesics, Opioid / Q000138:chemical synthesis* / Q000378:metabolism; D001921:Brain / Q000378:metabolism; D006868:Hydrolysis; D009590:Nitrogen Radioisotopes; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000378:metabolism; D018847:Opioid Peptides
D000701:Analgesics, Opioid; D009590:Nitrogen Radioisotopes; D009842:Oligopeptides; D018847:Opioid Peptides; C030058:dermorphin; C074009:tyrosyl-methionyl-phenylalanyl-glycinamide