Disposition of 4-bromo-2,5-dimethoxyphenethylamine (2C-B) and its metabolite 4-bromo-2-hydroxy-5-methoxyphenethylamine in rats after subcutaneous administration.
Miroslava Rohanová, Tomáš Páleníček, Marie Balíková
Toxicology letters April 21, 2008 DOI: 10.1016/j.toxlet.2008.01.017 via PubMed
Summary
AI-generated from the abstractThe psychedelic compound 2C-B, involved in human drug abuse and overdose cases, was studied in rats to determine its distribution and kinetics after subcutaneous injection. The drug had an estimated half-life of 1.1 hours and a volume of distribution of 16 L/kg. 2C-B entered the brain without significant delay, and its brain-to-serum ratio peaked at 13.9, remaining above 6.5 for six hours. The lungs showed a tendency to retain the drug and release it gradually over time, similar to the brain. The major metabolite 2H5M-BPEA was found in lung, brain, and liver tissues but distributed less efficiently into the brain than the parent compound. These findings help assess the drug's psychotropic and toxic effects.
Study at a glance
| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Rats |
| Intervention | 2C-B |
| Duration | 6 hours after the dose |
| Keywords | 2c-b Psychedelic compound Original compound Pharmacokinetics Drug distribution |
| Citations | 33 |
| Key finding | 2C-B rapidly enters the brain after subcutaneous administration in rats, with a half-life of 1.1 hours and a brain-to-serum ratio that peaks at 13.9 and remains elevated for at least six hours. |
Abstract
The psychedelic compound 4-bromo-2,5-dimethoxyphenethylamine (2C-B) has appeared as an agent in drug abuse or overdose cases in humans. The human pharmacokinetics of this drug is unknown and only partial information is available on its metabolites. Our experimental study was focused on the disposition and kinetic profile of 2C-B in rats after subcutaneous administration using a GC-MS validated method. One of the major metabolites 4-bromo-2-hydroxy-5-methoxyphenethylamine (2H5M-BPEA) was confirmed in rat tissues of lung, brain, liver and was quantitatively evaluated as well. The disposition of 2C-B was characterized by its estimated half-life 1.1h and estimated volume of distribution 16L/kg. The lung susceptibility for drug retention and gradual temporal release parallel to the brain were ascertained. The drug penetrating the blood/brain barrier was without significant delay. 2C-B brain to serum ratio attained a maximum value of 13.9 and remained over the value of 6.5 to the end of our observation (6h after the dose). The distribution of the hydroxylated metabolite 2H5M-BPEA into the lipophilic brain tissue was less efficient in relation to the parent compound. The kinetics of the drug partitioning between blood to brain may be important for the subsequent assessment of its psychotropic or toxic effects.