Amino Acids and Peptides. XXIII. Leu-Enkephalin Analogs Containing a Fluorinated Amino Acid at Position 2, 4 or 5

Fluorinated analogs of Leu-enkephalin were synthesized by the solution method and the solid-phase method. The synthetic peptides were examined for opioid activities on mouse vas deferens and guinea pig ileum. Among the synthetic peptides, [D-Ala2, Leu(F3)(2R, 4S)5]enkephalin and [D-Ala2, Leu(F3)(2S,...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1994/08/15, Vol.42(8), pp.1658-1662
Hauptverfasser:	MAEDA, Mitsuko, KAWASAKI, Koichi, TAGUCHI, Takeo, KOBAYASHI, Yoshiro, YAMAMOTO, Yoshihiro, SHIMOKAWA, Kazuhiro, TAKAHASHI, Masakatsu, NAKAO, Kaoru, KANETO, Hiroshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Amino Acids - analysis Animals Biological and medical sciences enkephalin Enkephalin, Leucine - chemical synthesis Enkephalin, Leucine - chemistry Enkephalin, Leucine - pharmacology fluorinated amino acid Fluorine - chemistry guinea pig ileum Guinea Pigs Magnetic Resonance Spectroscopy Male Medical sciences Mice Molecular Sequence Data mouse vas deferens Muscle, Smooth - drug effects Myenteric Plexus - drug effects Neuropharmacology Neurotransmitters. Neurotransmission. Receptors opioid peptide opioid receptor Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Structure-Activity Relationship Vas Deferens - drug effects
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Zusammenfassung:	Fluorinated analogs of Leu-enkephalin were synthesized by the solution method and the solid-phase method. The synthetic peptides were examined for opioid activities on mouse vas deferens and guinea pig ileum. Among the synthetic peptides, [D-Ala2, Leu(F3)(2R, 4S)5]enkephalin and [D-Ala2, Leu(F3)(2S, 4R)5]enkephalin exhibited potent opioid activity, and [Leu(F3)(2S, 4R)5]enkephalin exhibited high δ-receptor selectivity.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.42.1658