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- Title
Positive allosteric modulation of the human cannabinoid (CB) receptor by RTI-371, a selective inhibitor of the dopamine transporter.
- Authors
Navarro, Hernán A; Howard, James L; Pollard, Gerald T; Carroll, F Ivy
- Abstract
In our search for an indirect dopamine agonist as therapy for cocaine addiction, several selective inhibitors of the dopamine transporter (DAT), which are 3-phenyltropane analogues, were assayed for their effect on locomotor activity in mice. Interestingly, several of the compounds showed a poor correlation between stimulation of locomotion and DAT inhibition. One of the compounds, 3beta-(4-methylphenyl)-2beta-[3-(4-chlorophenyl)isoxazol-5-yl]tropane (RTI-371), was shown to cross the blood-brain barrier, by binding studies in vivo, and block cocaine-induced locomotor stimulation. As poor pharmacokinetics could not explain the behavioural effects of RTI-371, this compound was screened through our functional assays for activity at other CNS receptors. Initial screening identified RTI-371 as a positive allosteric modulator of the human CB(1) (hCB(1)) receptor.
- Publication
British journal of pharmacology, 2009, Vol 156, Issue 7, p1178
- ISSN
1476-5381
- Publication type
Journal Article
- DOI
10.1111/j.1476-5381.2009.00124.x