It's all things adamantane in our (@Lambert_Usyd) latest synthetic cannabinoid work, out now in @ACSChemNeurosci!
We synthesised and evaluated a library of adamantane-derived SCRAs, including fluorinated and deuterated analogues 🧪
🧵
https://t.co/yq4EPZPvyZ
🎤 presentation by @AxelleTimmerman @ #TIAFT2024:
"Synthesis and functional evaluation of synthetic cannabinoid receptor agonists related to ADB-HEXINACA"
👉 Fri Sep 6, Session 12
👉 Publ. in May @ACSChemNeurosci: https://t.co/9GY9XbDJLX
👉 🤝 w. @Lambert_Usyd@eric_sparkes
5/11
It's all things adamantane in our (@Lambert_Usyd) latest synthetic cannabinoid work, out now in @ACSChemNeurosci!
We synthesised and evaluated a library of adamantane-derived SCRAs, including fluorinated and deuterated analogues 🧪
🧵
https://t.co/yq4EPZPvyZ
Nice collaborative work (1st paper of @AxelleTimmerman 👏) w. @eric_sparkes & other fantastic @Lambert_Usyd colleagues now out in @ACSChemNeurosci:
Synthesis and Functional Evaluation of Synthetic Cannabinoid Receptor Agonists Related to ADB-HEXINACA
https://t.co/9GY9XbDJLX
🧵 👇
More SCRA work from @Lambert_Usyd out now in @rsc_medchem!
We looked at a series of proteinogenic amino acid-derived SCRAs related to MPP-5F-PICA, MMB-5F-PICA, and MDMB-5F-PICA, investigating the role of chirality in CB1 and CB2 receptor activation.
https://t.co/IpUb6vpCRH
In silico evaluation was used to rationalise some structure-activity relationships observed with Induced fit docking performed by @JackMarkhamPhD and Dai Hibbs
Assessment of βarrestin 2 recruitment was performed by @AxelleTimmerman and @christophestove, with many compounds acting as potent and efficacious agonists at both receptors. Remarkably, many compounds displayed efficacies far above that of CP55,940 at CB1.
Membrane potential assay work was performed by Rochelle Boyd and @EA_Cairns, and revealed most compounds were potent and efficacious agonists of CB1 and CB2.
Latest work from @Lambert_Usyd is online in @ACSChemNeurosci!
In another great collaboration with @christophestove et al., we looked at the recently detected synthetic cannabinoid ADB-HEXINACA and related analogues as emerging NPS🧪🔍
https://t.co/Sra7FCUERl