ArticleJournal of medicinal chemistry2015
3'-functionalized adamantyl cannabinoid receptor probes.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
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Who cites it
11 citing papers in PubMed.
- Covalent cannabinoid receptor ligands - structural insight and selectivity challenges.RSC medicinal chemistry · 2022Review
- Potential Role of Cannabinoid Type 2 Receptors in Neuropsychiatric and Neurodegenerative Disorders.Frontiers in psychiatry · 2022Review
- Functionalized Cannabinoid Subtype 2 Receptor Ligands: Fluorescent, PET, Photochromic and Covalent Molecular Probes.ChemMedChem · 2020Review
- Cannabinoids and Cannabinoid Receptors: The Story so Far.iScience · 2020Review
- Synthesis of Functionalized Cannabilactones.Molecules (Basel, Switzerland) · 2020Article
- Allosteric Modulation of Cannabinoid Receptor 1-Current Challenges and Future Opportunities.International journal of molecular sciences · 2019Review
- Chain Substituted Cannabilactones with Selectivity for the CB2 Cannabinoid Receptor.Molecules (Basel, Switzerland) · 2019Article
- Article
- Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CBJournal of the American Chemical Society · 2018Article
- A covalent antagonist for the human adenosine APurinergic signalling · 2017Article
- Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.Journal of medicinal chemistry · 2016Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
The aliphatic side chain plays a pivotal role in determining the cannabinergic potency of tricyclic classical cannabinoids, and we have previously shown that this chain could be substituted successfully by adamantyl or other polycyclic groups. In an effort to explore the pharmacophoric features of these conformationally fixed groups, we have synthesized a series of analogues in which the C3 position is substituted directly with an adamantyl group bearing functionality at one of the tertiary carbon atoms. These substituents included the electrophilic isothiocyanate and photoactivatable azido groups, both of which are capable of covalent attachment with the target protein. Our results show that substitution at the 3'-adamantyl position can lead to ligands with improved affinities and CB1/CB2 selectivities. Our work has also led to the development of two successful covalent probes with high affinities for both cannabinoid receptors, namely, the electrophilic isothiocyanate AM994 and the photoactivatable aliphatic azido AM993 analogues.
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Registered trials
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.