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  • Title: Dimeric dermorphin peptides: central administration suppresses gastric acid secretion through interaction with mu-type opioid receptor.
    Author: Guglietta A, Irons BJ, Lazarus LH, de Castiglione R, Melchiorri P.
    Journal: Methods Find Exp Clin Pharmacol; 1989 Nov; 11(11):663-70. PubMed ID: 2560103.
    Abstract:
    The effect of centrally administered dermorphin and a series of dimeric dermorphin analogs on gastric acid secretion was studied in pylorusligated rats. Dimeric dermorphin analogs consist of identical peptide chains either directly linked with a dihydride bond or a polyethyleneamine bridge at their carboxy termini. At a dose of 0.5 nmol dermorphin, and the dimeric analogs di-[D-Arg2,Sar4]-tetra-DM2, di-penta-DM0, di-[Sar4]-penta-DM0, di-[D-Arg2,Sar4]-penta-DM0, di-[D-Ala4]-penta-DM0 and di-DM0, and di-DM0, inhibited gastric acid output in a statistically significant manner (P less than 0.05). Furthermore, the binding characteristics of these peptides for the mu-type opioid receptor were analyzed using a brain synaptosomal fraction. Dermorphin and several dimeric dermorphin peptides bound to the mu-receptor: di-penta-DM0, di-[Sar4]-penta-DM0, di-penta-DM2 and di-DM0, had 3-to 5-fold greater affinity for the mu-receptor than the specific mu-agonist DAGO. These data indicate that a correlation exists between the central mediated gastric inhibitory effect of DM and several dimeric analogs and their affinity for the mu-type opioid receptor in rat brain.
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