Opioid binding profile of morphiceptin, Tyr-MIF-1 and dynorphin-related peptides in rat brain membranes

Sartania, N. , Benyhe, S., Magyar, A., Rónai, A.Z., Medzihradszky, K. and Borsodi, A. (1996) Opioid binding profile of morphiceptin, Tyr-MIF-1 and dynorphin-related peptides in rat brain membranes. Neuropeptides, 30(3), pp. 225-230. (doi: 10.1016/S0143-4179(96)90068-2)

Abstract

Opioid properties of several morphiceptin- (Tyr-Pro-Phe-Pro-NH2), Tyr-MIF-1 (Tyr-Pro-Leu-Gly-NH2) and dynorphin-derivatives were characterized in rat brain in vitro receptor binding assay and in electrically stimulated longitudinal muscle strip preparation of guinea pig ileum. In the case of morphiceptin-related peptides, an excellent correlation was found between the [3H]-naloxone binding displacement data and the agonist potencies determined in the bioassay. The ‘turning point’ was the C-terminal amidation in the tri- and tetrapeptide pairs in both series. Tyr-MIF-1 derivatives showed weak affinity in the opioid receptor binding assay and none of them had any remarkable effect in the bioassay either as agonist or antagonist. The dynorphin A(1–10)-peptides modified at positions 5 and 8 retained their affinity with Pro5-, Pro8-, and Ala8- substituents, whereas some loss of affinity was observed in the case of Gly8-Dyn A(1–10).

• Item Type: Articles
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Sartania, Professor Nana
• Authors: Sartania, N., Benyhe, S., Magyar, A., Rónai, A.Z., Medzihradszky, K., and Borsodi, A.
• College/School: College of Medical Veterinary and Life Sciences > School of Medicine, Dentistry & Nursing
• Journal Name: Neuropeptides
• ISSN: 0143-4179