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“Zombie” Outbreak Caused by the Synthetic Cannabinoid AMB‐FUBINACA in New York
TLDR
The potency of the synthetic cannabinoid identified in these analyses is consistent with strong depressant effects that account for the “zombielike” behavior reported in this mass intoxication in New York City. Expand
Pharmacology of Valinate and tert-Leucinate Synthetic Cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and Their Analogues.
TLDR
In vitro and in vivo data indicate that these SCs act as highly efficacious CB receptor agonists with greater potency than Δ(9)-THC and earlier generations of SCs. Expand
Altered proteostasis in aging and heat shock response in C. elegans revealed by analysis of the global and de novo synthesized proteome
TLDR
Interestingly, although the net rate of protein synthesis is reduced in aged animals, the analyses indicate that the synthesis of certain proteins such as the vitellogenins increases with age. Expand
Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135.
TLDR
In vitro functional activities of SC designer drugs JWH-018, UR-144, PB-22, and APICA, and their respective terminally fluorinated analogues and in vivo in vivo cannabinoid type 1 receptor binding affinity evaluated in rats showed no consistent trend for increased potency of fluorinated SCs over the corresponding des-fluoro SCs in vivo. Expand
Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA, ADB-PINACA, 5F-AB-PINACA, 5F-ADB-PINACA, ADBICA, and 5F-ADBICA.
TLDR
Synthetic cannabinoid designer drugs based on indole and indazole scaffolds and featuring l-valinamide or l-tert-leucinamide side chains and several analogues are synthesized and characterized, indicating that these SCs are cannabimimetic in vivo, consistent with anecdotal reports of psychoactivity in humans. Expand
[18F]DPA-714: Direct Comparison with [11C]PK11195 in a Model of Cerebral Ischemia in Rats
TLDR
The results suggest that, with the longer half-life of [ 18F] which facilitates distribution of the tracer across PET centre, [18F]DPA-714 is a good alternative for TSPO imaging. Expand
Structure of a Signaling Cannabinoid Receptor 1-G Protein Complex
TLDR
The structure of the CB1-Gi signaling complex bound to the highly potent agonist MDMB-Fubinaca (FUB) is presented, which compose the structural framework to explain CB1 activation by different classes of ligands and provide insights into the G protein coupling and selectivity mechanisms adopted by the receptor. Expand
The synthesis and pharmacological evaluation of adamantane-derived indoles: cannabimimetic drugs of abuse.
TLDR
Which structural features of AB-001, AB-002, and their analogues govern the cannabimimetic potency of these chemotypes in vitro and in vivo are elucidated. Expand
Detection of the recently emerged synthetic cannabinoid 5F-MDMB-PICA in 'legal high' products and human urine samples.
TLDR
Exemplary analysis of one urine sample for 5F-MDMB-PICA phase II metabolites showed that two of the main phase I metabolites are subject to extensive glucuronidation prior to renal excretion, and conjugate cleavage is reasonable for enhancing sensitivity. Expand
Comparative Evaluation of Three TSPO PET Radiotracers in a LPS-Induced Model of Mild Neuroinflammation in Rats
TLDR
Second-generation TSPO-PET tracers are able to accurately detect mild-level NI in a rodent model of subtle focal inflammation and show higher core/contralateral ratio and BPND when compared to (R)-[11C]PK11195, while [18F]DPA-714 did not. Expand
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