Amino Acids and Peptides. XXII. Preparation and Antinociceptive Effect of [D-Ala2] Leu-Enkephalin-Poly (Ethylene Glycol) Hybrid

The hybrid of poly (ethylene glycol) and [D-Ala2] Leu-enkephalin was prepared by the solution method and its antinociceptive effect and inhibitory effect on the electrically induced contractions of mouse vas deferens were examined. The hybrid was synthesized by the coupling of Boc-Tyr-D-Ala-Gly-Phe-...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Biological & pharmaceutical bulletin 1994/06/15, Vol.17(6), pp.823-825
Hauptverfasser:	MAEDA, Mitsuko, KAWASAKI, Koichi, MAYUMI, Tadanori, TAKAHASHI, Masakatsu, KANETO, Hiroshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Analgesics - chemical synthesis Analgesics - pharmacology Animals antinociceptive effect Biological and medical sciences Chromatography, High Pressure Liquid Dose-Response Relationship, Drug Drug Carriers Electric Stimulation enkephalin hybrid Enkephalin, Leucine-2-Alanine - analogs & derivatives Enkephalin, Leucine-2-Alanine - chemical synthesis Enkephalin, Leucine-2-Alanine - chemistry Enkephalin, Leucine-2-Alanine - pharmacology General pharmacology Male Medical sciences Mice Molecular Sequence Data mouse vas deferens Muscle Contraction - drug effects Muscle, Smooth - drug effects Organ Culture Techniques Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions Pharmacology. Drug treatments poly (ethylene glycol) hybrid Polyethylene Glycols - chemical synthesis Polyethylene Glycols - chemistry Polyethylene Glycols - pharmacology Vas Deferens - drug effects
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The hybrid of poly (ethylene glycol) and [D-Ala2] Leu-enkephalin was prepared by the solution method and its antinociceptive effect and inhibitory effect on the electrically induced contractions of mouse vas deferens were examined. The hybrid was synthesized by the coupling of Boc-Tyr-D-Ala-Gly-Phe-Leu-OH and amino-poly (ethylene glycol), followed by trifluoroacetic acid treatment. The hybrid showed more potent antinociceptive activity in mice and 120 times higher inhibitory activity in mouse vas deferens preparation than intact [D-Ala2] Leu-enkephalin.
ISSN:	0918-6158 1347-5215
DOI:	10.1248/bpb.17.823