Abstract:
:Cocaine interacts with sigma receptors, suggesting that these sites are important for many of its behavioral effects. Therefore, two novel sigma 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 sigma1 and sigma2 sites, but a 250-fold or lower affinity for nine other receptors, making them among the most selective sigma 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 sigma receptors are involved in the behavioral effects of cocaine.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
McCracken KA,Bowen WD,Matsumoto RRdoi
10.1016/s0014-2999(98)00876-0subject
Has Abstractpub_date
1999-01-15 00:00:00pages
35-8issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(98)00876-0journal_volume
365pub_type
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