ArticlePloS one2012
Lipo-endomorphin-1 derivatives with systemic activity against neuropathic pain without producing constipation.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 31 citations in OpenAlex.
- Rational Design of Putative Dual-Target Opioid-Dopaminergic Casomorphin-Ranatensin Hybrid Peptides: Computational Modeling and Preliminary Antiproliferative Evaluation.Molecules (Basel, Switzerland) · 2026Article
- Peptide-derived ligands for the discovery of safer opioid analgesics.Drug discovery today · 2024Review
- The Somatostatin Receptor-4 Agonist J-2156 Alleviates Mechanical Hypersensitivity in a Rat Model of Breast Cancer Induced Bone Pain.Frontiers in pharmacology · 2018Article
- Optimization andFrontiers in pharmacology · 2017Article
- Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.ACS medicinal chemistry letters · 2015Article
- Novel GPCR paradigms at the μ-opioid receptor.British journal of pharmacology · 2015Review
- Lipid- and sugar-modified endomorphins: novel targets for the treatment of neuropathic pain.Frontiers in pharmacology · 2013Review
- Efficacy and ligand bias at the μ-opioid receptor.British journal of pharmacology · 2013Review
- Chemical methods for peptide and protein production.Molecules (Basel, Switzerland) · 2013Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
To enhance the drug-like properties of the endogenous opioid peptide endomorphin-1 (1 = Tyr-Pro-Trp-Phe-NH(2)), the N-terminus of the peptide was modified with 2-aminodecanoic acid, resulting in compound 3. Tyr in compound 1 was replaced with 2,6-dimethyltyrosine yielding compound 2. Derivative 2 was also substituted with 2-aminodecanoic acid producing compound, 4. Lipoamino acid-modified derivatives showed improved metabolic stability and membrane permeability while maintaining high μ-opioid (MOP) receptor binding affinity and acting as a potent agonist. In vivo studies showed dose-dependent antinociceptive activity following intravenous (i.v.) administration of compounds 3 and 4 in a chronic constriction injury (CCI)-rat model of neuropathic pain with ED(50) values of 1.22 (± 0.93) and 0.99 (± 0.89) µmol/kg, respectively. Pre-treatment of animals with naloxone hydrochloride significantly attenuated the anti-neuropathic effects of compound 3, confirming the key role of opioid receptors in mediating antinociception. In contrast to morphine, no significant constipation was produced following i.v. administration of compound 3 at 16 µmol/kg. Furthermore, following chronic administration of equi-potent doses of compound 3 and morphine to rats, there was less antinociceptive tolerance for compound 3 compared with morphine.
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