Demonstration of clomipramine and venlafaxine occupation at serotonin reuptake sites in man in vivo.
Article Details
- CitationCopy to clipboard
Malizia AL, Melichar JM, Brown DJ, Gunn RN, Reynolds A, Jones T, Nutt DJ
Demonstration of clomipramine and venlafaxine occupation at serotonin reuptake sites in man in vivo.
J Psychopharmacol. 1997;11(3):279-81.
- PubMed ID
- 9305421 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Clomipramine Sodium-dependent serotonin transporter Protein Humans YesInhibitorDetails Venlafaxine Sodium-dependent serotonin transporter Protein Humans YesInhibitorDetails