Potent analgesic activity of the enkephalin-like tetrapeptide H-Tyr-D-Ala-Gly-Phe-NH2

Antinociceptive effect of [Met5]enkephalin semicarbazide is not affected by dipeptidyl carboxypeptidase‐I

“…Furthermore, the amide and semicarbazide derivatives seemed to exert more prolonged analgesia compared with ME, as their analgesia remained near the cutoff time for about 45 min after their intrathecal injection. Similar potentiated and prolonged analgesia have been previously reported for the [D-Ala 2 ]enkephalin amide [14].…”

Hybrid peptidomimetics for the use in neuropathicpain

“…Nine new hybrid peptidomimetics containing two ligands: an enkephalin analogue (opioid agonist) [6] and SHU 9119 (an MC4 receptor antagonist) [4] linked by various spacers have been designed. Spacers in designed peptidomimetics can be classified as short (residues of D-Ala, β -Ala), flexible (residue of 6-aminohexanoic acid (Ahx)), rigid (residues of 4-aminomethylbenzoic acid (4AMB), 4-aminophenylacetic acid (4APhAc) and semi-rigid (dipeptidyl fragment of Pro-Gly [7]).…”

Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors

“…Starting materials, buffer components, GDP, GTPgS were purchased from Sigma-Aldrich Kft. (Budapest, Hungary), fatty acid free bovine serum albumin (BSA) was from Serva (Heidelberg, Germany), DAMGO was obtained from Bachem AG (Bubendorf, Switzerland), Ile 5,6 -deltorphin-2 was prepared in the Laboratory of Chemical Biology (BRC, Hungary), naloxone was kindly provided by Endo Laboratories (Wilmington, DE, USA), WIN-55,212e2 was purchased from Tocris Inc. (Bristol, UK), [ 35 Tritium labeling was carried out in a self-designed vacuum manifold [42] and radioactivity was measured with a Packard Tri-Carb 2100 TR liquid scintillation analyser using Insta Gel scintillation cocktail of PerkinElmer. Analytical thin layer chromatography (TLC) was performed on 5 Â 10 cm glass plates precoated with silica gel 60 F 254 (Merck, Darmstadt, Germany), spots were visualized with UV light.…”