Based on the structure of the superpotent 5-HT(2A) agonist 2-(4-bromo-2,5-dimethoxyphenyl)-N-[(2-methoxyphenyl)methyl]ethanamine, which consists of a ring-substituted phenethylamine skeleton modified with an N-benzyl group, we designed and synthesized a small library of constrained analogues to identify the optimal arrangement of the pharmacophoric elements of the ligand. Structures consisted of diversely substituted tetrahydroisoquinolines, piperidines, and one benzazepine. Based on the structure of (S,S)-9b, which showed the highest affinity of the series, we propose an optimal binding conformation. (S,S)-9b also displayed 124-fold selectivity for the 5-HT(2A) over the 5-HT(2C) receptor, making it the most selective 5-HT(2A) receptor agonist ligand currently known.
Pharmacology, Toxicology and Pharmaceutical Science
7
10%
Biochemistry, Genetics and Molecular Biology
6
8%
Agricultural and Biological Sciences
4
6%
Medicine and Dentistry
4
6%
Other
10
14%
Unknown
20
28%
Attention Score in Context
Attention Score in Context
This research output has an Altmetric Attention Score of 18. 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 26 March 2026.
All research outputs
#2,611,027
of 33,982,974 outputs
Outputs from ACS Chemical Neuroscience
#287
of 3,389 outputs
Outputs of similar age
#14,683
of 212,903 outputs
Outputs of similar age from ACS Chemical Neuroscience
#3
of 24 outputs
Altmetric has tracked 33,982,974 research outputs across all sources so far. Compared to these this one has done particularly well and is in the 92nd percentile: it's in the top 10% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 3,389 research outputs from this source. They typically receive a lot more attention than average, with a mean Attention Score of 11.2. This one has done particularly well, scoring higher than 91% 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 212,903 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 93% of its contemporaries.
We're also able to compare this research output to 24 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 87% of its contemporaries.
