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Structure-Activity Relationships, Deuteration, and Fluorination of Synthetic Cannabinoid Receptor Agonists Related to AKB48, 5F-AKB-48, and AFUBIATA.
Sparkes, Eric; Maloney, Callan J; Markham, Jack W; Dane, Chianna; Boyd, Rochelle; Gilchrist, Jayson; Moir, Michael; Gordon, Rebecca; Luo, Jia Lin; Pike, Edward; Walker, Katelyn A; Kassiou, Michael; McGregor, Iain S; Kevin, Richard C; Hibbs, David E; Jorgensen, William T; Banister, Samuel D; Cairns, Elizabeth A; Ametovski, Adam.
Afiliação
  • Sparkes E; Lambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney, Sydney, NSW 2050, Australia.
  • Maloney CJ; School of Chemistry, Faculty of Science, The University of Sydney, Sydney, NSW 2006, Australia.
  • Markham JW; Lambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney, Sydney, NSW 2050, Australia.
  • Dane C; School of Chemistry, Faculty of Science, The University of Sydney, Sydney, NSW 2006, Australia.
  • Boyd R; Lambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney, Sydney, NSW 2050, Australia.
  • Gilchrist J; School of Chemistry, Faculty of Science, The University of Sydney, Sydney, NSW 2006, Australia.
  • Moir M; Sydney Pharmacy School, Faculty of Medicine and Health, The University of Sydney, Sydney, NSW 2006, Australia.
  • Gordon R; School of Chemistry, Faculty of Science, The University of Sydney, Sydney, NSW 2006, Australia.
  • Luo JL; Lambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney, Sydney, NSW 2050, Australia.
  • Pike E; Sydney Pharmacy School, Faculty of Medicine and Health, The University of Sydney, Sydney, NSW 2006, Australia.
  • Walker KA; School of Chemistry, Faculty of Science, The University of Sydney, Sydney, NSW 2006, Australia.
  • Kassiou M; National Deuteration Facility, Australian Nuclear Science and Technology Organisation, Sydney, NSW 2234, Australia.
  • McGregor IS; Lambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney, Sydney, NSW 2050, Australia.
  • Kevin RC; Sydney Pharmacy School, Faculty of Medicine and Health, The University of Sydney, Sydney, NSW 2006, Australia.
  • Hibbs DE; Lambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney, Sydney, NSW 2050, Australia.
  • Jorgensen WT; School of Psychology, Faculty of Science, The University of Sydney, Sydney, NSW 2006, Australia.
  • Banister SD; Lambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney, Sydney, NSW 2050, Australia.
  • Cairns EA; School of Chemistry, Faculty of Science, The University of Sydney, Sydney, NSW 2006, Australia.
  • Ametovski A; Department of Chemistry, University of York, York YO10 5DD, U.K.
ACS Chem Neurosci ; 15(11): 2160-2181, 2024 06 05.
Article em En | MEDLINE | ID: mdl-38766866
ABSTRACT
Synthetic cannabinoid receptor agonists (SCRAs) are a growing class of new psychoactive substances (NPS) commonly derived from an N-alkylated indole, indazole, or 7-azaindole scaffold. Diversification of this core (at the 3-position) with amide-linked pendant amino acid groups and modular N-alkylation (of the indole/indazole/7-azaindole core) ensures that novel SCRAs continue to enter the illicit drug market rapidly. In response to the large number of SCRAs that have been detected, pharmacological evaluation of this NPS class has become increasingly common. Adamantane-derived SCRAs have consistently appeared throughout the market since 2011, and as such, a systematic set of these derivatives was synthesized and pharmacologically evaluated. Deuterated and fluorinated adamantane derivatives were prepared to evaluate typical hydrogen bioisosteres, as well as evaluation of the newly detected AFUBIATA.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Halogenação / Agonistas de Receptores de Canabinoides / Indazóis / Indóis Limite: Animals / Humans Idioma: En Revista: ACS Chem Neurosci Ano de publicação: 2024 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Halogenação / Agonistas de Receptores de Canabinoides / Indazóis / Indóis Limite: Animals / Humans Idioma: En Revista: ACS Chem Neurosci Ano de publicação: 2024 Tipo de documento: Article