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Biomedical subjects

L Gráf

Publications and source records attributed to L Gráf.

At least 19 recordsLinked to original sources

Effect of Met-enkephalin and (D-Met2,Pro5)-enkephalinamide on the adenylate cyclase activity of rat brain.

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.

Adenylyl Cyclases

Kinetic studies in isolated organs: tools to design analgesic peptides and to analyze their receptor effects.

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.

Analgesics, Opioid