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Cyclic analogues of Tyr-W-MIF-1 with prolonged analgesic activity and potency comparable to DAMGO and morphine
Authors:J E Zadina  A J Kastin  L Hackler and S L Chang
Institution:

a VA Medical Center and Tulane University School of Medicine, New Orleans, LA 70146, USA

b Seton Hall University, South Orange, NJ 07079, USA

Abstract:Two cyclic analogues of the brain peptide Tyr-W-MIF-1 (Tyr-Pro-Trp-Gly-NH2) were synthesized and tested for analgesic activity in the rat tail flick test after intracerebroventricular (ICV) injection. The analogues were about 200-fold more potent than the parent peptide. Analgesia was dose dependent, and at 1 μg the two analogues, the mu-selective enkephalin analogue DAMGO (), and morphine, all produced analgesia lasting between 40 and 60 min. Analgesia of longer duration was evident at higher doses of the analogues and lasted more than 6 h after 100 μg, the highest dose tested. The results show that peptide analogues based on the structure of the endogenously occurring Tyr-W-MIF-1 can produce potent and long-lasting effects on nociception.
Keywords:Opiate  Analogues  Tyr-W-MIF-1  Tyr-MIF-1  Analgesia
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