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Pharmacol."],"abstract":"<jats:p><jats:bold>Introduction:<\/jats:bold><jats:italic>N<\/jats:italic>-2-methoxy-benzylated (\u201cNBOMe\u201d) analogues of phenethylamine are a group of new psychoactive substances (NPS) with reported strong psychedelic effects in sub-milligram doses linked to a number of severe intoxications, including fatal ones. In our present work, we provide a detailed investigation of pharmacokinetics and acute behavioural effects of 2C-B-Fly-NBOMe (2-(8-bromo-2,3,6,7-tetrahydrobenzo [1,2-b:4,5-b\u2032]difuran-4-yl)-<jats:italic>N-<\/jats:italic>[(2-methoxybenzyl]ethan-1-amine), an analogue of popular psychedelic entactogen 2C-B (4-Bromo-2,5-dimethoxyphenethylamine).<\/jats:p><jats:p><jats:bold>Methods:<\/jats:bold> All experiments were conducted on adult male Wistar rats. Pharmacokinetic parameters of 2C-B-Fly-NBOMe (1\u00a0mg\/kg subcutaneously; s. c.) in blood serum and brain tissue were analysed over 24\u00a0h using liquid chromatography-mass spectrometry (LC\/MS). For examination of behavioural parameters in open field test (OFT) and prepulse inhibition (PPI) of acoustic startle reaction (ASR), 2C-B-Fly-NBOMe (0.2, 1 and 5\u00a0mg\/kg s. c.) was administered in two temporal onsets: 15 and 60\u00a0min after administration. Thermoregulatory changes were evaluated in individually and group-housed animals over 8\u00a0h following the highest dose used in behavioural experiments (5\u00a0mg\/kg s. c.).<\/jats:p><jats:p><jats:bold>Results:<\/jats:bold> Peak drug concentrations were detected 30 and 60\u00a0min after the drug application in serum (28\u00a0ng\/ml) and brain tissue (171\u00a0ng\/g), respectively. The parental compound was still present in the brain 8\u00a0h after administration. Locomotor activity was dose-dependently reduced by the drug in both temporal testing onsets. ASR was also strongly disrupted in both temporal onsets, drug\u2019s effect on PPI was weaker. 2C-B-Fly-NBOMe did not cause any significant thermoregulatory changes.<\/jats:p><jats:p><jats:bold>Discussion:<\/jats:bold> Our results suggest that 2C-B-Fly-NBOMe penetrates animal brain tissue in a relatively slow manner, induces significant inhibitory effects on motor performance, and attenuates sensorimotor gating. Its overall profile is similar to closely related analogue 2C-B and other NBOMe substances.<\/jats:p>","DOI":"10.3389\/fphar.2023.1120419","type":"journal-article","created":{"date-parts":[[2023,3,9]],"date-time":"2023-03-09T05:05:39Z","timestamp":1678338339000},"update-policy":"https:\/\/doi.org\/10.3389\/crossmark-policy","source":"Crossref","is-referenced-by-count":5,"title":["Acute pharmacological profile of 2C-B-Fly-NBOMe in male Wistar rats\u2014pharmacokinetics, effects on behaviour and thermoregulation"],"prefix":"10.3389","volume":"14","author":[{"given":"Kate\u0159ina","family":"Syrov\u00e1","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kl\u00e1ra","family":"\u0160\u00edchov\u00e1","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hynek","family":"Danda","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Eva","family":"Lhotkov\u00e1","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Pascal","family":"Jorratt","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nikola","family":"Pinterov\u00e1-Leca","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"\u010cestm\u00edr","family":"Vejmola","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lucie","family":"Olejn\u00edkov\u00e1-Ladislavov\u00e1","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kate\u0159ina","family":"H\u00e1jkov\u00e1","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Martin","family":"Kucha\u0159","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ji\u0159\u00ed","family":"Hor\u00e1\u010dek","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tom\u00e1\u0161","family":"P\u00e1len\u00ed\u010dek","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1965","published-online":{"date-parts":[[2023,3,9]]},"reference":[{"key":"B1","doi-asserted-by":"publisher","first-page":"179","DOI":"10.1007\/BF00431945","article-title":"LSD-induced alterations of locomotor patterns and exploration in rats","volume":"77","author":"Adams","year":"1982","journal-title":"Psychopharmacol. 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