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Open Access The psychostimulant d-threo-(R,R)-methylphenidate binds as an agonist to the 5HT1A receptor

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The present study was undertaken to determine whether d-threo-(R,R)-methylphenidate (MPH) was exerting binding activity as an agonist or antagonist of 5-HT1A and 5-HT2B receptors. [35S]guanosine5'[gamma-thio]triphosphate ([35S]GTPγS) binding assay and field-stimulated Guinea pig ileum assay were used to determine 5-HT1A receptor agonism and antagonism activity of d-threo-(R,R)-MPH. The results suggested d-threo-(R,R)-MPH induced 5-HT1A receptor agonist activity at 100 μM. The Guinea pig ileum functional assay showed that d-threo-(R,R)-MPH produced agonist-like reduction of neurogenic twitch with an EC50 5.65 ± 0.36 μM. At 30 μM concentrations, d-threo-(R,R)-MPH produced 171 ± 4.24% of the relaxation relative to that caused by 0.12 μM 8-OH-DPAT. However, d-threo-(R,R)-MPH exhibited no significant pharmacological activity in rat stomach fundus 5-HT2B receptor functional assay. Thus, d-threo-(R,R)-MPH appears to act as a selective 5-HT1A receptor agonist in vitro. It is speculated that the activation of 5-HT1A receptor might play a partial role in d-threo-(R,R)-MPH mediated dopamine (DA) release in the brain.
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Document Type: Research Article

Affiliations: 1: Laboratory of Drug Disposition and Pharmacogenetics, Department of Pharmaceutical and Biomedical Sciences, Charles P. Darby Children’s Research Institute, Medical University of South Carolina, 173 Ashley Avenue, Charleston, South Carolina, SC 29425, USA, Email: [email protected] 2: Department of Psychiatry and Behavioral Sciences, Charles P. Darby Children’s Research Institute, Medical University of South Carolina, Charleston, South Carolina, USA 3: Department of Neurosciences, Charles P. Darby Children’s Research Institute, Medical University of South Carolina, Charleston, South Carolina, USA 4: Laboratory of Drug Disposition and Pharmacogenetics, Department of Pharmaceutical and Biomedical Sciences, Charles P. Darby Children’s Research Institute, Medical University of South Carolina, Charleston, South Carolina, USA

Publication date: 01 February 2009

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