941583-81-9Relevant academic research and scientific papers
Improved cyclobutyl nabilone analogs as potent CB1 receptor agonists
Papanastasiou, Ioannis P.,Georgiadis, Markos-Orestis,Iliopoulos-Tsoutsouvas, Christos,Paronis, Carol A.,Brust, Christina A.,Tran, Ngan K.,Ji, Lipin,Ma, Xiaoyu,Wood, JodiAnne T.,Zvonok, Nikolai,Tong, Fei,Bohn, Laura M.,Nikas, Spyros P.,Makriyannis, Alexandros
supporting information, (2022/01/20)
In earlier work, we explored the SAR for the C3 side chain pharmacophore in the hexahydrocannabinol template represented by the drug nabilone, which resulted in the development of AM2389. In an effort for further optimization, we have merged features of n
Novel Labelled Cannabinergic Ligands and Related Analogs
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Paragraph 0152; 0153, (2021/10/02)
Novel cannabinoid ligands represented by the general formulas I, II, and III and methods for preparation and use within which one or more of a fluorescent ligand, nitroxide spin label, metal chelate, biotin moiety, or group with enhanced polarity may be incorporated. The compounds can bind to and modulate the cannabinoid CB1 and CB2 receptors and thereby considered specific ligands for these receptors. Some of the disclosed compounds that bind to cannabinoid CB1 and CB2 receptors can exhibit tight or irreversible binding characteristics for these receptors. Due to the presence of the imaging/diagnostic and/or therapeutic functional groups including fluorescent groups, nitroxide spin labels, metal chelates, biotin moieties, and groups with enhanced polarity, the disclosed compounds may be useful as imaging/diagnostic tools and/or therapeutic agents.
Novel Functionalized Cannabinoid Receptor Probes: Development of Exceptionally Potent Agonists
Jiang, Shan,Iliopoulos-Tsoutsouvas, Christos,Tong, Fei,Brust, Christina A.,Keenan, Catherine M.,Raghav, Jimit Girish,Hua, Tian,Wu, Simiao,Ho, Jo-Hao,Wu, Yiran,Grim, Travis W.,Zvonok, Nikolai,Thakur, Ganesh A.,Liu, Zhi-Jie,Sharkey, Keith A.,Bohn, Laura M.,Nikas, Spyros P.,Makriyannis, Alexandros
, p. 3870 - 3884 (2021/05/04)
We report the development of novel cannabinergic probes that can stabilize the cannabinoid receptors (CBRs) through tight binding interactions. Ligand design involves the introduction of select groups at a judiciously chosen position within the classical
2-CYCLOALKYL RESORCINOL CANNABINERGIC LIGANDS
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Paragraph 0179; 0181, (2014/05/07)
The present invention relates to novel 2-cycloalkyl resorcinol compounds; to pharmaceutical compositions comprising the compounds; and to methods of preparing the compounds and uses thereof. The disclosed compounds can bind to and modulate the cannabinoid
Novel 1′,1′-chain substituted hexahydrocannabinols: 9β-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 (CB1) agonist
Nikas, Spyros P.,Alapafuja, Shakiru O.,Papanastasiou, Ioannis,Paronis, Carol A.,Shukla, Vidyanand G.,Papahatjis, Demetris P.,Bowman, Anna L.,Halikhedkar, Aneetha,Han, Xiuwen,Makriyannis, Alexandros
experimental part, p. 6996 - 7010 (2010/12/18)
In pursuit of a more detailed understanding of the structural requirements for the key side chain cannabinoid pharmacophore, we have extended our SAR to cover a variety of conformationally modified side chains within the 9-keto and 9-hydroxyl tricyclic st
