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CP-615,003 is a drug which acts as a subtype-selective partial agonist at GABAA receptors, and was developed by Pfizer as a potential anxiolytic, however poor blood–brain barrier penetration make it primarily useful as a research ligand.
- Shaffer CL, Gunduz M, O'Connell TN, Obach RS, Yee S (November 2005). "Biotransformation of a GABAA receptor partial agonist in sprague-dawley rats and cynomolgus monkeys: identification of two unique N-carbamoyl metabolites". Drug Metabolism and Disposition: the Biological Fate of Chemicals 33 (11): 1688–99. doi:10.1124/dmd.105.004630. PMID 16081672.
- Venkatakrishnan K, Tseng E, Nelson FR, Rollema H, French JL, Kaplan IV, Horner WE, Gibbs MA (August 2007). "Central nervous system pharmacokinetics of the Mdr1 P-glycoprotein substrate CP-615,003: intersite differences and implications for human receptor occupancy projections from cerebrospinal fluid exposures". Drug Metabolism and Disposition: the Biological Fate of Chemicals 35 (8): 1341–9. doi:10.1124/dmd.106.013953. PMID 17470526.