| Title |
Pharmacological evaluation of new constituents of “Spice”: synthetic cannabinoids based on indole, indazole, benzimidazole and carbazole scaffolds
|
|---|---|
| Published in |
Forensic Toxicology, April 2018
|
| DOI | 10.1007/s11419-018-0415-z |
| Pubmed ID | |
| Authors |
Clara T. Schoeder, Cornelius Hess, Burkhard Madea, Jens Meiler, Christa E. Müller |
| Abstract |
In the present study we characterized a series of synthetic cannabinoids containing various heterocyclic scaffolds that had been identified as constituents of "Spice", a preparation sold on the illicit drug market. All compounds were further investigated as potential ligands of the orphan receptors GPR18 and GPR55 that interact with some cannabinoids. The compounds were studied in radioligand binding assays to determine their affinity for human cannabinoid CB1 and CB2 receptors expressed in CHO cells, and in cAMP accumulation assays to study their functionality. Structure-activity relationships were analyzed. The most potent CB1 receptor agonist of the present series MDMB-FUBINACA (12) (Ki = 98.5 pM) was docked into the human CB1 receptor structure, and a plausible binding mode was identified showing high similarity with that of the co-crystallized THC derivatives. MDMB-CHMCZCA (41) displayed a unique profile acting as a full agonist at the CB1 receptor subtype, but blocking the CB2 receptor completely. Only a few weakly potent antagonists of GPR18 and GPR55 were identified, and thus all compounds showed high CB receptor selectivity, mostly interacting with both subtypes, CB1 and CB2. These results will be useful to assess the compounds' toxicological risks and to guide legislation. Further studies on 41 are warranted. |
X Demographics
The data shown below were collected from the profiles of 10 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 2 | 20% |
| United Kingdom | 1 | 10% |
| Austria | 1 | 10% |
| Portugal | 1 | 10% |
| Unknown | 5 | 50% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 9 | 90% |
| Scientists | 1 | 10% |
Mendeley readers
The data shown below were compiled from readership statistics for 71 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 71 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 12 | 17% |
| Student > Master | 12 | 17% |
| Student > Bachelor | 10 | 14% |
| Researcher | 7 | 10% |
| Student > Doctoral Student | 5 | 7% |
| Other | 9 | 13% |
| Unknown | 16 | 23% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 17 | 24% |
| Pharmacology, Toxicology and Pharmaceutical Science | 12 | 17% |
| Agricultural and Biological Sciences | 6 | 8% |
| Biochemistry, Genetics and Molecular Biology | 4 | 6% |
| Immunology and Microbiology | 2 | 3% |
| Other | 11 | 15% |
| Unknown | 19 | 27% |
Attention Score in Context
This research output has an Altmetric Attention Score of 7. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 21 November 2018.
All research outputs
#4,807,604
of 23,775,451 outputs
Outputs from Forensic Toxicology
#42
of 390 outputs
Outputs of similar age
#90,302
of 328,102 outputs
Outputs of similar age from Forensic Toxicology
#3
of 18 outputs
Altmetric has tracked 23,775,451 research outputs across all sources so far. Compared to these this one has done well and is in the 79th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 390 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 5.2. This one has done well, scoring higher than 89% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 328,102 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 72% of its contemporaries.
We're also able to compare this research output to 18 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 88% of its contemporaries.