A preliminary investigation of the psychoactive agent 4-Bromo-2,5-Dimethoxyphenethylamine: A potential drug of abuse
1988; Elsevier BV; Volume: 30; Issue: 3 Linguagem: Inglês
10.1016/0091-3057(88)90071-8
ISSN1873-5177
AutoresRichard A. Glennon, Milt Titeler, Robert A. Lyon,
Tópico(s)Nicotinic Acetylcholine Receptors Study
Resumo—4-Bromo-2,5-dimethoxyphenethylamine (α-desMe DOB) is a psychoactive agent that may possess significant abuse potential. Because of its structural similarity to the established hallucinogen 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane (DOB), and because almost no pharmacological data are available on this agent, we undertook this preliminary investigation. α-DesMe DOB (Ki = 1 nM), like DOB itself (Ki = 0.79 nM), displays a high affinity for [3H]DOB-labeled central 5-HT2 serotonin receptors. However, unlike DOB, the α-desmethyl derivative also binds with significant affinity to 5-HT1A, 5-HT1B and 5-HT1C serotonin receptors and, as such, is selective than DOB. In drug discrimination studies using rats trained to discriminate either DOM (i.e., the 4-methyl analog of DOB) or R(—)DOB from saline, stimulus generalization occurred in both groups of animals. However, stimulus generalization was associated with extensive disruption of behavior, α-DesMe DOB may produce stimulus effects similar, but not identical, to those of DOM and R(—)DOB; in addition, this agent may be capable of producing other, as yet undefined, central effects at comparable doses. These other effects may be reflective of the lack of selectivity of α-desMe DOB for 5-HT2 serotonin receptors. Because other hallucinogenic agents display high affinity for 5-HT2 serotonin receptors and result in stimulus generalization in DOM- and/or DOB-trained animals, it is tentatively concluded that α-desMe DOB is a psychoactive agent with at least some hallucinogenic or DOB-like properties.
Referência(s)