The Chemistry and Pharmacology of Synthetic Cannabinoid Receptor Agonist New Psychoactive Substances: Evolution

2018 ◽  
pp. 191-226 ◽  
Author(s):  
Samuel D. Banister ◽  
Mark Connor
Keyword(s):  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
New Psychoactive Substances ◽  
Psychoactive Substances ◽  
Synthetic Cannabinoid Receptor Agonist

scholarly journals The chemistry and pharmacology of putative synthetic cannabinoid receptor agonist (SCRA) new psychoactive substances (NPS) 5F-PY-PICA, 5F-PY-PINACA, and their analogues

2018 ◽  
Author(s):  
Samuel D. Banister ◽  
Richard C. Kevin ◽  
Lewis Martin ◽  
Axel Adams ◽  
Christa Macdonald ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Structural Diversity ◽  
Synthetic Cannabinoid ◽  
New Psychoactive Substances ◽  
Resonance Spectroscopy ◽  
Psychoactive Substances ◽  
Flight Mass Spectrometry ◽  
Synthetic Cannabinoid Receptor Agonist

AbstractThe structural diversity of synthetic cannabinoid receptor agonist (SCRA) new psychoactive substances (NPS) has increased since the first examples were reported a decade ago. 5F-PY-PICA and 5F-PY-PINACA were identified in 2015 as putative SCRA NPS, although nothing is known of their pharmacology. 5F-PY-PICA, 5F-PY-PINACA, and analogues intended to explore structure-activity relationships within this class of SCRAs were synthesized and characterized by nuclear magnetic resonance spectroscopy and liquid chromatography–quadrupole time-of-flight–mass spectrometry. Using competitive binding experiments and fluorescence-based plate reader membrane potential assays, the affinities and activities of all analogues at cannabinoid type 1 and type 2 receptors (CB1 and CB2) were evaluated. All ligands showed minimal affinity for CB1 (pKi < 5), although several demonstrated moderate CB2 binding (pKi = 5.45–6.99). At 10 μM none of the compounds produced an effect > 50% of CP55,950 at CB1, while several compounds showed a slightly higher relative efficacy at CB2. Unlike other SCRA NPS, 5F-PYPICA and 5F-PY-PINACA did not produce cannabimimetic effects in mice at doses up to 10 mg/kg.

scholarly journals Synthetic Cannabinoid Receptor Agonist-related Intoxication: Impact and Legislative Success

2020 ◽  
Vol 8 (1) ◽  
pp. 30
Author(s):  
Getaw Worku Hassen ◽  
Andrew Eng ◽  
Ioana Scherbakova ◽  
Aida Eliza Abdul Majid ◽  
Alessandra Renee Piscina ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
Synthetic Cannabinoid Receptor Agonist

Semiquantitative Activity-Based Detection of JWH-018, a Synthetic Cannabinoid Receptor Agonist, in Oral Fluid after Vaping

2020 ◽  
Vol 92 (8) ◽  
pp. 6065-6071 ◽  
Author(s):  
Annelies Cannaert ◽  
Maria del Mar Ramírez Fernández ◽  
Eef L. Theunissen ◽  
Johannes G. Ramaekers ◽  
Sarah M. R. Wille ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Oral Fluid ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
Synthetic Cannabinoid Receptor Agonist

scholarly journals Cumyl‐CBMICA: A new synthetic cannabinoid receptor agonist containing a cyclobutyl methyl side chain

2020 ◽  
Author(s):  
Sebastian Halter ◽  
Benedikt Pulver ◽  
Maurice Wilde ◽  
Belal Haschimi ◽  
Folker Westphal ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
Side Chain ◽  
Synthetic Cannabinoid Receptor Agonist

scholarly journals In vitro and in vivo pharmacological evaluation of the synthetic cannabinoid receptor agonist EG-018

2020 ◽  
Vol 193 ◽  
pp. 172918
Author(s):  
Thomas F. Gamage ◽  
Daniel G. Barrus ◽  
Richard C. Kevin ◽  
David B. Finlay ◽  
Timothy W. Lefever ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
Pharmacological Evaluation ◽  
Synthetic Cannabinoid Receptor Agonist

scholarly journals Analysis and clinical findings of cases positive for the novel synthetic cannabinoid receptor agonist MDMB-CHMICA

2016 ◽  
Vol 54 (8) ◽  
pp. 632-637 ◽  
Author(s):  
Alice Seywright ◽  
Hazel J. Torrance ◽  
Fiona M. Wylie ◽  
Denise A. McKeown ◽  
David J. Lowe ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Clinical Findings ◽  
Synthetic Cannabinoid ◽  
The Novel ◽  
Synthetic Cannabinoid Receptor Agonist

An index of fatal toxicity for new psychoactive substances

2018 ◽  
Vol 32 (7) ◽  
pp. 793-801 ◽  
Author(s):  
Leslie A King ◽  
John M Corkery
Keyword(s):  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
New Psychoactive Substances ◽  
Death Certificates ◽  
Psychoactive Substances ◽  
Receptor Agonists ◽  
A Value ◽  
Other Substances ◽  
Synthetic Cannabinoid Receptor Agonists ◽  
Original Reference

An index of fatal toxicity for new psychoactive substances has been developed based solely on information provided on death certificates. An updated index of fatal toxicity (Tf), as first described in 2010, was calculated based on the ratio of deaths to prevalence and seizures for the original five substances (amphetamine, cannabis, cocaine/crack, heroin and 3,4-methylenedioxymethylamphetamine)*. These correlated well with the 2010 index. Deaths were then examined for cases both where the substance was and was not found in association with other substances. This ratio (sole to all mentions; S/A) was then calculated for deaths in the period 1993 to 2016. This new measure of fatal toxicity, expressed by S/A, was well-correlated with the index Ln (Tf) of the original reference compounds. The calculation of S/A was then extended to a group of new psychoactive substances where insufficient prevalence or seizure data were available to directly determine a value of Tf by interpolation of a graph of Tf versus S/A. Benzodiazepine analogues had particularly low values of S/A and hence Tf. By contrast, γ-hydroxybutyrate/γ-butyrolactone, α-methyltryptamine, synthetic cannabinoid receptor agonists and benzofurans had a higher fatal toxicity.

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