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Demonstration of clomipramine and venlafaxine occupation at serotonin reuptake sites in man in vivo

Cyclotron Unit, MRC CRC, Hammersmith Hospital, London W12 0NN, UK, Psychopharmacology Unit, University of Bristol, Bristol BS8 1TD, UK

J.M. Melichar

Cyclotron Unit, MRC CRC, Hammersmith Hospital, London W12 0NN, UK, Psychopharmacology Unit, University of Bristol, Bristol BS8 1TD, UK

D.J. Brown

Cyclotron Unit, MRC CRC, Hammersmith Hospital, London W12 0NN, UK

R.N. Gunn

Cyclotron Unit, MRC CRC, Hammersmith Hospital, London W12 0NN, UK

A. Reynolds

Wyeth Laboratories, Huntercombe Lane South, Taplow, Maidenhead, Berkshire SL6 0PH, UK

T. Jones

Cyclotron Unit, MRC CRC, Hammersmith Hospital, London W12 0NN, UK

D.J. Nutt

Psychopharmacology Unit, University of Bristol, Bristol BS8 1TD, UK

We describe the use of ¹¹CRTI-55 and the Multiple Objects Coincidences Counter (MOCC) to detect in-vivo binding to peripheral serotonin reuptake sites (left chest comprising platelet and lung serotonin reuptake sites) in man. Displacement and preloading experiments with clomipramine and venlafaxine in two healthy volunteers demonstrated that ¹¹CRTI-55 binding is decreased in a dose-dependent fashion by both these drugs which bind to the serotonin transporter. In addition parallel data from the total head curve (representing ¹¹CRTI-55 binding to central serotonin and dopamine (DA) reuptake sites) suggest that prior blockade of the serotonin transporter may be a useful strategy to maximize radioactive counts in the head when measuring the DA transporter. The MOCC is likely to be useful to determine sequential indices of relative serotonin reuptake blockade in patients on treatment.

Key Words: clomipramine • human • in vivo • PET • pharmacokinetic • RTI-55 • serotonin reuptake site • venlafaxine

Journal of Psychopharmacology, Vol. 11, No. 3, 279-281 (1997)
DOI: 10.1177/026988119701100312


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