Solid phase synthesis and opioid receptor binding activities of [D-Ala2, D-Leu5]enkephalin analogs containing a fluorinated aromatic amino acid.
Five [D-Ala2, D-Leu55]enkephalin (DADLE) analogs containing fluorinated Tyr1 or Phe4 residue, that is, [Phe(2F)4] (I), [Phe(3F)4] (II), [Phe(4F)4] (III), [Tyr(3F)1] (IV) and [Tyr(2F)1] (V), were synthesized by the solid phase method and their opioid receptor affinities were examined. Affinity profiles of five derivatives for the mu- and delta-receptor were similar to those of DADLE, and the affinity for kappa-receptor was zero or negligible.
Sasaki
Y
Y
Tohoku College of Pharmacy, Sendai, Japan.
Kohno
H
H
Ohkubo
Y
Y
Suzuki
K
K
D016308:Enkephalin, Leucine-2-Alanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D005461:Fluorine; D011957:Receptors, Opioid / Q000378:metabolism*
D011957:Receptors, Opioid; D005461:Fluorine; D016308:Enkephalin, Leucine-2-Alanine