ArticleBioorganic & medicinal chemistry letters2015
Modification of amphipathic non-opioid dynorphin A analogues for rat brain bradykinin receptors.
Article in Bioorganic & medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 12 citations in OpenAlex.
- Discovery of Stable Non-opioid Dynorphin A Analogues Interacting at the Bradykinin Receptors for the Treatment of Neuropathic Pain.ACS chemical neuroscience · 2016Article
- Cyclic non-opioid dynorphin A analogues for the bradykinin receptors.Bioorganic & medicinal chemistry letters · 2016Article
- Various modifications of the amphipathic dynorphin A pharmacophore for rat brain bradykinin receptors.Chemical biology & drug design · 2016Article
- Cycloartanes from Oxyanthus pallidus and derivatives with analgesic activities.BMC complementary and alternative medicine · 2016Article
- Dynorphin A analogs for the treatment of chronic neuropathic pain.Future medicinal chemistry · 2016Review
- Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors.Bioorganic & medicinal chemistry letters · 2015Article
- Blockade of non-opioid excitatory effects of spinal dynorphin A at bradykinin receptors.Receptors & clinical investigationArticle
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
It has been shown that under chronic pain or nerve injury conditions, up-regulated dynorphin A (Dyn A) interacts with bradykinin receptors (BRs) to cause hyperalgesia in the spinal cord. Thus BRs antagonist can modulate hyperalgesia by blocking Dyn A's interaction with the BRs in the central nervous system. In our earlier structure-activity relationship (SAR) study, [des-Arg(7)]-Dyn A-(4-11) 13 was discovered as a minimum pharmacophore for rat brain BRs with its antagonist activity (anti-hyperalgesic effect) in in vivo tests using naïve or injured animals. We have pursued further modification on the [des-Arg(7)]-Dyn A analogues and identified a key insight into the pharmacophore of the rat brain BRs: amphipathicity.
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Registered trials
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