In this section
@article{Shimshoni:2016:10.1007/s00210-016-1297-4,
author = {Shimshoni, JA and Winkler, I and Golan, E and Nutt, D},
doi = {10.1007/s00210-016-1297-4},
journal = {Naunyn-Schmiedeberg's Archives of Pharmacology},
pages = {15--24},
title = {Neurochemical binding profiles of novel indole and benzofuran MDMA analogues.},
url = {http://dx.doi.org/10.1007/s00210-016-1297-4},
volume = {390},
year = {2016}
}
TY - JOUR
AB - 3,4-Methylenedioxy-N-methylamphetamine (MDMA) has been shown to be effective in the treatment of post-traumatic stress disorder (PTSD) in numerous clinical trials. In the present study, we have characterized the neurochemical binding profiles of three MDMA-benzofuran analogues (1-(benzofuran-5-yl)-propan-2-amine, 5-APB; 1-(benzofuran-6-yl)-N-methylpropan-2-amine, 6-MAPB; 1-(benzofuran-5-yl)-N-methylpropan-2-amine, 5-MAPB) and one MDMA-indole analogue (1-(1H-indol-5-yl)-2-methylamino-propan-1-ol, 5-IT). These compounds were screened as potential second-generation anti-PTSD drugs, against a battery of human and non-human receptors, transporters, and enzymes, and their potencies as 5-HT2 receptor agonist and monoamine uptake inhibitors determined. All MDMA analogues displayed high binding affinities for 5-HT2a,b,c and NEα2 receptors, as well as significant 5-HT, DA, and NE uptake inhibition. 5-APB revealed significant agonist activity at the 5-HT2a,b,c receptors, while 6-MAPB, 5-MAPB, and 5-IT exhibited significant agonist activity at the 5-HT2c receptor. There was a lack of correlation between the results of functional uptake and the monoamine transporter binding assay. MDMA analogues emerged as potent and selective monoamine oxidase A inhibitors. Based on 6-MAPB favorable pharmacological profile, it was further subjected to IC50 determination for monoamine transporters. Overall, all MDMA analogues displayed higher monoamine receptor/transporter binding affinities and agonist activity at the 5-HT2a,c receptors as compared to MDMA.
AU - Shimshoni,JA
AU - Winkler,I
AU - Golan,E
AU - Nutt,D
DO - 10.1007/s00210-016-1297-4
EP - 24
PY - 2016///
SN - 0028-1298
SP - 15
TI - Neurochemical binding profiles of novel indole and benzofuran MDMA analogues.
T2 - Naunyn-Schmiedeberg's Archives of Pharmacology
UR - http://dx.doi.org/10.1007/s00210-016-1297-4
UR - http://www.ncbi.nlm.nih.gov/pubmed/27650729
VL - 390
ER -
