ArticleBioorganic & medicinal chemistry letters2012
Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.
Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 24 citations in OpenAlex.
- Natural Products for the Treatment of Pain: Chemistry and Pharmacology of Salvinorin A, Mitragynine, and Collybolide.Biochemistry · 2021Review
- Crosstalk Between Kappa Opioid and Dopamine Systems in Compulsive Behaviors.Frontiers in pharmacology · 2020Review
- A review of salvinorin analogs and their kappa-opioid receptor activity.Bioorganic & medicinal chemistry letters · 2018Review
- Clerodane diterpenes: sources, structures, and biological activities.Natural product reports · 2016Review
- Intrinsic relative activities of κ opioid agonists in activating Gα proteins and internalizing receptor: Differences between human and mouse receptors.European journal of pharmacology · 2015Article
- Salvinorin A, a kappa-opioid receptor agonist hallucinogen: pharmacology and potential template for novel pharmacotherapeutic agents in neuropsychiatric disorders.Frontiers in pharmacology · 2015Review
- Behavioral and cellular pharmacology characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) as a mu opioid receptor selective ligand.European journal of pharmacology · 2014Article
- Salvinorin A analogs and other κ-opioid receptor compounds as treatments for cocaine abuse.Advances in pharmacology (San Diego, Calif.) · 2014Review
- Studies toward bivalent κ opioids derived from salvinorin A: heteromethylation of the furan ring reduces affinity.Beilstein journal of organic chemistry · 2013Article
- The 2-methoxy methyl analogue of salvinorin A attenuates cocaine-induced drug seeking and sucrose reinforcements in rats.European journal of pharmacology · 2013Article
- Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.Bioorganic & medicinal chemistry letters · 2013Article
- Grand opening of structure-guided design for novel opioids.Trends in pharmacological sciences · 2013Review
- Salvinorin B meth-oxy-methyl ether.Acta crystallographica. Section E, Structure reports online · 2012Article
- 6'-Guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment.The Journal of biological chemistry · 2012Article
- Semisynthetic neoclerodanes as kappa opioid receptor probes.Bioorganic & medicinal chemistry · 2012Article
- A Novel Mu-Delta Opioid Agonist Demonstrates Enhanced Efficacy With Reduced Tolerance and Dependence in Mouse Neuropathic Pain Models.The journal of painArticle
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
Abstract
The kappa opioid receptor (KOPR) has been identified as a potential drug target to prevent or alter the course of mood, anxiety and addictive disorders or reduce response to stress. In a search for highly potent and selective KOPR partial agonists as pharmacological tools, we have modified 12-epi-salvinorin A, a compound which we have previously observed to be a KOPR partial agonist. Five analogues of 12-epi-salvinorin A were synthesized and their effects on G protein activation as well as β-arrestin2 recruitment were evaluated. Only 12-epi-salvinorin A (1) partially activated signaling through G proteins, yet acted as a full agonist in the β-arrestin 2 DiscoveRx assay. Other salvinorin analogues tested in these functional assays were full agonists in both assays of KOPR activation. By comparison, the non-selective opioid ligand nalbuphine, known to be a partial agonist for G-protein activation, was also a partial agonist for the β-arrestin mediated signaling pathway activated through KOPR.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.