ABSTRACT
Present knowledge about pineal melatonin regulation in humans is exclusively derived from observations following pharmacological perturbations of the melatonin rhythmicity, which has been observed in patients or healthy volunteers using measurements of plasma and urinary melatonin or 6-sulphatoxymelatonin levels. The clinical pharmacology of melatonin regulation provides strong evidence for the origin of plasma melatonin from the human pineal gland. The majority of clinical pharmacological studies on melatonin regulation have been carried out with drugs affecting processes of noradrenergic neurotransmission. A number of clinical studies have addressed the effects of antidepressant drugs on the regulation of melatonin secretion. Therefore the goal of the majority of clinical pharmacological studies is to prove the significance of neurobiological factors in humans which have been shown to be of primary importance in melatonin regulation in animals. Selective inhibitors of 5HT uptake have been used during the last 16 years as pharmacological tools in preclinical research and for therapeutic purposes.
