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Vol. 291, Issue 1, 12-18, October 1999

Endomorphin-1 and Endomorphin-2 Show Differences in Their Activation of µ Opioid Receptor-Regulated G Proteins in Supraspinal Antinociception in Mice1

Pilar Sánchez-Blázquez, Marta Rodríguez-Díaz, Isabel DeAntonio and Javier Garzón

Neurofarmacología, Instituto de Neurobiología Santiago Ramón y Cajal, Consejo Superior de Investigaciones Científicas, Madrid, Spain

Endomorphin-1 and endomorphin-2 are tetrapeptides of the brain whose binding profiles and analgesic activities indicate that they are endogenous ligands at µ opioid receptors. To analyze the classes of G transducer proteins activated by these opioids in the production of supraspinal antinociception, the expression of alpha  subunits of the Gi protein class, Gi1, Gi2, Gi3, Go1, Go2, and Gz, and those of the Gq protein family, Gq and G11, was reduced by administration of antisense oligodeoxynucleotides (ODNs) complementary to sequences in their respective mRNAs. The ODN treatments promoted differences in the analgesic effects displayed by morphine, [D-Ala2,N-MePhe4,Gly-ol5]enkephalin (DAMGO), and the novel opioids endomorphin-1 and endomorphin-2. The impairment of Gi1alpha and Gi3alpha function led to a weaker analgesic response to the endomorphins and to the alpha 2-adrenoceptor agonist clonidine, whereas the effects of morphine and DAMGO were not affected. An antisense probe targeting Gi2alpha blocked the antinociceptive effects of endomorphin-2, morphine, DAMGO, and clonidine but was without effect on the activity of endomorphin-1. Mice receiving the ODN to Gzalpha subunits showed impaired response to all agonists. The knockdown of either Go1alpha , Go2alpha , Gqalpha , or G11alpha had little or no influence on the antinociception induced by any of the opioids in the study. Thus, agonists exhibit differences in activating the variety of GTP-binding proteins regulated by µ opioid receptors.

0022-3565/99/2911-0012$03.00/0
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Copyright © 1999 by The American Society for Pharmacology and Experimental Therapeutics


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