Novel σ receptor ligands attenuate the locomotor stimulatory effects of cocaine
1999; Elsevier BV; Volume: 365; Issue: 1 Linguagem: Inglês
10.1016/s0014-2999(98)00876-0
ISSN1879-0712
AutoresKari A. McCracken, Wayne D. Bowen, Rae R. Matsumoto,
Tópico(s)Nicotinic Acetylcholine Receptors Study
ResumoCocaine interacts with σ receptors, suggesting that these sites are important for many of its behavioral effects. Therefore, two novel σ receptor ligands, BD1008 (N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine) and BD1063 (1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine), were evaluated for their ability to attenuate cocaine-induced locomotor activity. Receptor binding studies showed that BD1008 and BD1063 have nanomolar affinities for σ1 and σ2 sites, but a 250-fold or lower affinity for nine other receptors, making them among the most selective σ receptor ligands identified. In behavioral studies, pretreatment of mice with BD1008 or BD1063 produced a two-fold increase in the ED50 for the locomotor stimulatory effects of cocaine. These results suggest that σ receptors are involved in the behavioral effects of cocaine.
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