Opioid activities of D-Arg2-substituted tetrapeptides.

doi:10.1016/s0022-3565(25)39132-9

Paper

Opioid activities of D-Arg2-substituted tetrapeptides.

Published Aug 1, 1987 · T. Sato, S. Sakurada, T. Sakurada

The Journal of pharmacology and experimental therapeutics

Q2 SJR score

42

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0

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Abstract

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In Vitro Study

Study Snapshot

D-Arg2-substituted tetrapeptides show potent and long-lasting opioid activities due to their high opioid receptor affinity and inhibitory effects on enkephalin-degrading enzymes.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Opioid activities of D-Arg2-substituted tetrapeptides.

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References

Citations

Cyclizing Painkillers: Development of Backbone-Cyclic TAPS Analogs

TAPS c(2-6) shows potential as a metabolically stable, peripheral painkiller with potential as a full opioid receptor functional agonist.

Identification of Dmt-D-Lys-Phe-Phe-OH as a highly antinociceptive tetrapeptide metabolite of the opioid-neurotensin hybrid peptide PK20

Dmt-D-Lys-Phe-Phe-OH (PK20M) is a highly effective analgesic tetrapeptide metabolite of the opioid-neurotensin hybrid peptide PK20, with high potency and opioid subtype receptor selectivity.

Preparation and evaluation at the delta opioid receptor of a series of linear leu-enkephalin analogues obtained by systematic replacement of the amides.

Systematic replacement of amide bonds with ester or N-methyl amide bonds can efficiently design and synthesize novel peptide analogues with enhanced stability, without significantly decreasing their biological activity on the delta opioid receptor.

Synthesis, biological activity and resistance to proteolytic digestion of new cyclic dermorphin/deltorphin analogues.

New cyclic dermorphin/deltorphin analogues show strong antinociceptive effects and resistance to proteolytic digestion, making them potential lead molecules for further evaluation.

Dermorphin tetrapeptide analogs as potent and long-lasting analgesics with pharmacological profiles distinct from morphine

Dermorphin N-terminal tetrapeptide analogs containing d-Arg 2 show potent analgesic activity and distinct pharmacological profiles from morphine, potentially reducing side effects.