Metabolic fate of hallucinogenic NBOMes
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Metabolic fate of hallucinogenic NBOMes. / Leth-Petersen, Sebastian; Gabel-Jensen, Charlotte; Gillings, Nic; Lehel, Szabolzs; Hansen, Hanne D; Knudsen, Gitte M; Kristensen, Jesper L.
I: Chemical Research in Toxicology, Bind 29, Nr. 1, 2016, s. 96–100.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Metabolic fate of hallucinogenic NBOMes
AU - Leth-Petersen, Sebastian
AU - Gabel-Jensen, Charlotte
AU - Gillings, Nic
AU - Lehel, Szabolzs
AU - Hansen, Hanne D
AU - Knudsen, Gitte M
AU - Kristensen, Jesper L
PY - 2016
Y1 - 2016
N2 - 2,5-dimethoxy-N-benzylphenethylamines (NBOMes) are very potent 5-HT2AR agonists. Illicit use of these psychedelic compounds has emerged in recent years, and several fatalities have been linked to their recreational use. In its [11C]-labelled form, one NBOMe (25B-NBOMe) was recently developed as a PET-ligand for clinical investigations of the 5HT2AR ([11C]Cimbi-36). Herein, we have identified the phase I and phase II metabolites of 25B-NBOMe in pigs as well as in humans. We find that the primary route of metabolism is 5'-demethylation, followed by conjugation to glucuronic acid. [11C]-labelling of 25B-NBOMe in three different positions followed by in vivo evaluation in pigs and in humans corroborated these findings.
AB - 2,5-dimethoxy-N-benzylphenethylamines (NBOMes) are very potent 5-HT2AR agonists. Illicit use of these psychedelic compounds has emerged in recent years, and several fatalities have been linked to their recreational use. In its [11C]-labelled form, one NBOMe (25B-NBOMe) was recently developed as a PET-ligand for clinical investigations of the 5HT2AR ([11C]Cimbi-36). Herein, we have identified the phase I and phase II metabolites of 25B-NBOMe in pigs as well as in humans. We find that the primary route of metabolism is 5'-demethylation, followed by conjugation to glucuronic acid. [11C]-labelling of 25B-NBOMe in three different positions followed by in vivo evaluation in pigs and in humans corroborated these findings.
U2 - 10.1021/acs.chemrestox.5b00450
DO - 10.1021/acs.chemrestox.5b00450
M3 - Journal article
C2 - 26669514
VL - 29
SP - 96
EP - 100
JO - Chemical Research in Toxicology
JF - Chemical Research in Toxicology
SN - 0893-228X
IS - 1
ER -
ID: 151839371