25X-NBOMe compounds – chemistry, pharmacology and toxicology. A comprehensive review

Discovery and Structure–Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT2A Receptor Agonists

“…Some of these also exhibit pronounced selectivity for 5-HT 2A R over the two other 5-HT 2 R subtypes, 5-HT 2B R and 5-HT 2C R. 30,31 However, concerns about their safety profiles may hinder the clinical development of compounds from the NBOMe class. 32 Representatives of the NBOMe class have been used as tool compounds to investigate the hypothesis that biased agonists mediating selective activation of specific 5-HT 2A R-coupled downstream pathways may hold therapeutic advantages compared to nonbiased receptor agonists. These investigations have led too the development of biased agonists with promising in vitro profiles, but their clinical potential is yet to be investigated.…”

“…The N -benzyl phenethylamine (NBOMe) class of compounds derived from N-benzylation of the 2C-X’s include some of the most potent 5-HT 2A R agonists reported to date. Some of these also exhibit pronounced selectivity for 5-HT 2A R over the two other 5-HT 2 R subtypes, 5-HT 2B R and 5-HT 2C R. , However, concerns about their safety profiles may hinder the clinical development of compounds from the NBOMe class …”

“…Some of these also exhibit pronounced selectivity for 5-HT 2A R over the two other 5-HT 2 R subtypes, 5-HT 2B R and 5-HT 2C R. 30 , 31 However, concerns about their safety profiles may hinder the clinical development of compounds from the NBOMe class. 32 …”