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Year : 1997  |  Volume : 29  |  Issue : 2  |  Page : 92-98

Pharmacological activities of some synthetic peptides related to dermorphin

Correspondence Address:
K M Sivanandaiah

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Source of Support: None, Conflict of Interest: None

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Objectives: To investigate the relationship between the structure of dermorphins (DM) and their pharmacological properties, six analogues of [Hyp6] DM and [Pro6] DM were synthesised and their biological activities were studied. Methods: The peptides were synthesised by the solid phase method using 9-fluorenylmethoxycarbonyl amino acid trichlorophenyl esters as coupling agents and Merrifield resin as solid support. The opioid agonist activity was studied using co-axially, electrically stimulated contraction of isolated guinea pig ileum (GPI, in vitro). Their analgesic activity was assessed in mice using Eddy's hot plate method and tail-flick method. The antidiarrhoeal activity was determined by the charcoal meal test in mice. Results: In the GPI assay, the synthetic analogues possess agonistic activity that are less pronounced than morphine. Peptides I and II (substitution of ser at position 7 and Gly at position 4 in [Hyp6] DM series respectively) possessed considerable analgesic activity but are almost inactive in the GPI assay. Peptide Ill ( [ Pro6, Sar7] DM) possess only analgesic activity. In GPI assay, peptide IV was inactive. Peptide V and VI had equipotent analgesic and antidiarrhoeal activity. Conclusion: Peptides with various structures can possess specificities that may prove useful in biolo ical applications. Among them [Sar4, Hyp6, Tyr7] DM, [Hyp6. Pro7] DM, [Pro6, Sar ] DM and [Phg3,Pro4 ] DM exhibited a high degree of selectivity in their activities.


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