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Usenko, A.B.; Emel'yanova, T. G.; Myasoedov, N. F.

doi:10.1023/a:1014359000606

Cited by 6 publications

(2 citation statements)

References 62 publications

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“…Dermorphins and deltorphins (Table 7) are the family of antinociceptive peptides that have been found in the skin of South American frogs [25]. Dermorphins are the most potent and selective MOR agonists, whereas deltorphins are peptides with high affinity and selectivity for DOR [102,103]. The antinociceptive peptide was also extracted from the brain of the frog Odorrana graham.…”

Section: Peptides Of Amphibian Originmentioning

confidence: 99%

Analgesic Peptides: From Natural Diversity to Rational Design

Gach-Janczak,

Biernat,

Kuczer

et al. 2024

Molecules

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Pain affects one-third of the global population and is a significant public health issue. The use of opioid drugs, which are the strongest painkillers, is associated with several side effects, such as tolerance, addiction, overdose, and even death. An increasing demand for novel, safer analgesic agents is a driving force for exploring natural sources of bioactive peptides with antinociceptive activity. Since the G protein-coupled receptors (GPCRs) play a crucial role in pain modulation, the discovery of new peptide ligands for GPCRs is a significant challenge for novel drug development. The aim of this review is to present peptides of human and animal origin with antinociceptive potential and to show the possibilities of their modification, as well as the design of novel structures. The study presents the current knowledge on structure-activity relationship in the design of peptide-based biomimetic compounds, the modification strategies directed at increasing the antinociceptive activity, and improvement of metabolic stability and pharmacodynamic profile. The procedures employed in prolonged drug delivery of emerging compounds are also discussed. The work summarizes the conditions leading to the development of potential morphine replacements.

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Section: Peptides Of Amphibian Originmentioning

confidence: 99%

Analgesic Peptides: From Natural Diversity to Rational Design

Gach-Janczak,

Biernat,

Kuczer

et al. 2024

Molecules

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“…The dermorphins [326,327] (Table 3.17) are potent analgesics in rodents and primates, including humans. Dermorphin (DM) was first isolated from the skin of the frog Phyllomedusa sauvagei.…”

Section: Dermorphinsmentioning

confidence: 99%

Biology of Peptides

Sewald

Jakubke

2009

Peptides: Chemistry and Biology

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Biological evaluation and molecular docking studies of AA3052, a compound containing a μ-selective opioid peptide agonist DALDA and d-Phe-Phe-d-Phe-Leu-Leu-NH2, a substance P analogue

Kowalczyk

Kleczkowska

Rękawek

et al. 2016

European Journal of Pharmaceutical Sciences

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The design of novel drugs for pain relief with improved analgesic properties and diminished side effect induction profile still remains a challenging pursuit. Tolerance is one of the most burdensome phenomena that may hamper ongoing opioid therapy, especially in chronic pain patients. Therefore, a promising strategy of hybridizing two pharmacophores that target distinct binding sites involved in pain modulation and transmission was established. Previous studies have led to the development of opioid agonist/NK1 agonist hybrids that produce sufficient analgesia and also suppress opioid-induced tolerance development. In our present investigation we assessed the antinociceptive potency of a new AA3052 chimera comprised of a potent MOR selective dermorphin derivative (DALDA) and an NK1 agonist, a stabilized substance P analogue. We have shown that AA3052 significantly prolonged responses to both mechanical and noxious thermal stimuli in rats after intracerebroventricular administration. Additionally, AA3052 did not trigger the development of tolerance in a 6-day daily injection paradigm nor did it produce any sedative effects, as assessed in the rotarod performance test. However, the antinociceptive effect of AA3052 was independent of opioid receptor stimulation by the DALDA pharmacophore as shown in the agonist-stimulated G-protein assay. Altogether the current results confirm the antinociceptive effectiveness of a novel opioid/SP hybrid agonist, AA3052, and more importantly its ability to inhibit the development of tolerance.

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Untitled

Cited by 6 publications

References 62 publications

Analgesic Peptides: From Natural Diversity to Rational Design

Analgesic Peptides: From Natural Diversity to Rational Design

Biology of Peptides

Biological evaluation and molecular docking studies of AA3052, a compound containing a μ-selective opioid peptide agonist DALDA and d-Phe-Phe-d-Phe-Leu-Leu-NH2, a substance P analogue

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