Systematic evaluation of a panel of 30 synthetic cannabinoid receptor agonists structurally related to MMB‐4en‐PICA, MDMB‐4en‐PINACA, ADB‐4en‐PINACA and MMB‐4CN‐BUTINACA using a combination of binding and different CB 1 receptor activation assays PART II: Structure activity relationship assessment via a β‐arrestin recruitment assay

2021 ◽  
Author(s):  
Katharina Elisabeth Grafinger ◽  
Annelies Cannaert ◽  
Adam Ametovski ◽  
Eric Sparkes ◽  
Elizabeth Cairns ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Receptor Activation ◽  
Structure Activity Relationship ◽  
Synthetic Cannabinoid ◽  
Activity Relationship ◽  
Systematic Evaluation ◽  
Receptor Agonists ◽  
Structure Activity ◽  
Synthetic Cannabinoid Receptor Agonists ◽  
Relationship Assessment

Structure-activity relationships of valine-, tert-leucine-, and phenylalanine amino acid-derived synthetic cannabinoid receptor agonists related to ADB-BUTINACA, APP-BUTINACA, and ADB-P7AICA

2021 ◽  
Author(s):  
Eric Sparkes ◽  
Elizabeth Cairns ◽  
Richard Kevin ◽  
Felcia Lai ◽  
Katharina Grafinger ◽  
...  
Keyword(s):  
Amino Acid ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
New Psychoactive Substances ◽  
Psychoactive Substances ◽  
Structure Activity Relationships ◽  
Receptor Agonists ◽  
Structure Activity ◽  
Synthetic Cannabinoid Receptor Agonists

Synthetic cannabinoid receptor agonists (SCRAs) remain one the most prevalent classes of new psychoactive substances (NPS) worldwide, and examples are generally poorly characterised at the time of first detection. We...

scholarly journals Modulation of human T-type calcium channels by synthetic cannabinoid receptor agonists in vitro

2021 ◽  
Vol 187 ◽  
pp. 108478
Author(s):  
Chris Bladen ◽  
Somayeh Mirlohi ◽  
Marina Santiago ◽  
Mitchell Longworth ◽  
Michael Kassiou ◽  
...  
Keyword(s):  
Calcium Channels ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
Receptor Agonists ◽  
Synthetic Cannabinoid Receptor Agonists

scholarly journals Human Toxicity Caused by Indole and Indazole Carboxylate Synthetic Cannabinoid Receptor Agonists: From Horizon Scanning to Notification

2018 ◽  
Vol 64 (2) ◽  
pp. 346-354 ◽  
Author(s):  
Simon L Hill ◽  
Michael Dunn ◽  
Céline Cano ◽  
Suzannah J Harnor ◽  
Ian R Hardcastle ◽  
...  
Keyword(s):  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
Severe Toxicity ◽  
Accurate Identification ◽  
Receptor Agonists ◽  
Horizon Scanning ◽  
Other Substances ◽  
Using Data ◽  
Synthetic Cannabinoid Receptor Agonists ◽  
The Uk

Abstract BACKGROUND The emergence of novel psychoactive substances (NPS), particularly synthetic cannabinoid receptor agonists (SCRA), has involved hundreds of potentially harmful chemicals in a highly dynamic international market challenging users', clinicians', and regulators' understanding of what circulating substances are causing harm. We describe a toxicovigilance system for NPS that predicted the UK emergence and identified the clinical toxicity caused by novel indole and indazole carboxylate SCRA. METHODS To assist early accurate identification, we synthesized 5 examples of commercially unavailable indole and indazole carboxylate SCRA (FUB-NPB-22, 5F-NPB-22, 5F-SDB-005, FUB-PB-22, NM-2201). We analyzed plasma and urine samples from 160 patients presenting to emergency departments with severe toxicity after suspected NPS use during 2015 to 2016 for these and other NPS using data-independent LC-MS/MS. RESULTS We successfully synthesized 5 carboxylate SCRAs using established synthetic and analytical chemistry methodologies. We identified at least 1 SCRA in samples from 49 patients, including an indole or indazole carboxylate SCRA in 17 (35%), specifically 5F-PB-22 (14%), FUB PB-22 (6%), BB-22 (2%), 5F NPB-22 (20%), FUB NPB-22 (2%), and 5F-SDB-005 (4%). In these 17 patients, there was analytical evidence of other substances in 16. Clinical features included agitation and aggression (82%), reduced consciousness (76%), acidosis (47%), hallucinations and paranoid features (41%), tachycardia (35%), hypertension (29%), raised creatine kinase (24%), and seizures (12%). CONCLUSIONS This toxicovigilance system predicted the emergence of misuse of indole and indazole carboxylate SCRA, documented associated clinical harms, and notified relevant agencies. Toxicity appears consistent with other SCRA, including mental state disturbances and reduced consciousness.

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