Met-enkephalin attenuates morphine tolerance in rats.
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Biomedical subjects
Publications and source records attributed to L Gráf.
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Among opiatelike peptides, stimulatory as well as inhibitory effects are encountered on adenylate cyclase activity. These actions are dependent not only on the investigated brain region but also on the applied peptide. Met-enkephalin stimulates adenylate cyclase activity in the rat brain stem (D-Met2, Pro5)-enkephalinamide and beta-endorphin inhibited it, whereas all three peptides inhibited the activity of cortex. Naloxone antagonized the effects of the applied peptides in the presence of sodium chloride.
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Highly purified calf brain cathepsin D (EC 3.4.23.5) selectively splits the Leu77-Phe78 and Ala36-Ala37 peptide bonds of human beta-lipotropin. It is suggested that the formation of human "beta-melanotropin" from gamma-lipotropin, and that of gamma-endorphin from beta-endorphin, is due to the action of cathepsin D during isolation procedures.
The opioid activities of peptide and non-peptide narcotics were studied in longitudinal muscle strip of guinea pig ileum (GPI) and in mouse vas deferens (MVD). The comparison of agonist activities of peptides found in GPI and MVD offered the opportunity to predict the presence but not the magnitude of potential analgesic activity. The kinetics of the antagonism between naltrexone and different types of agonists were also determined in these systems. Using C-6 epimers of naltrexone, it was found that the site of opiate receptors recognizing the information provided by the C-6 substituent of naltrexone are different in GPI and MVD.
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