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Jalfre M, Ruch-Monachon MA, Haefely W.
“Methods for Assessing the Interaction of Agents with 5-Hydroxytryptamine Neurons and Receptors in the Brain”.
Advances in Psychopharmacology. 1974;10:121-134.
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Abstract
Drugs are the most valuable tools for elucidating the functional role of monoamines tin the central nervous system (CNS). The actual knowledge of central monoamine function would be very poor indeed without the accidental discovery and. the rational development of compounds interacting in some way with these central neurotransmitters. In order to find such drugs, pharmacologists need to have reliable methods for screening, comparing, and analyzing old and new compounds. We present two methods which we consider useful for the study of central 5 - hydroxytryptaminergic mechanisms. A key problem in the study of brain 5 - hydroxytryptamine (5-HT) is how to assess the actual 5-hydroxytryptaminergic tone exerted on a given brain structure. A variety of factors contribute to the 5-hydroxy - tryptaminergic tone: there is the input to the 5-HT neuronsexcitatory and/or inhibitory which determines the activity of the 5-HT neuron, the number and the sequence of action potentials fired; within the neuron itself is the whole biochemical machinery for the synthesis and storage of the transmitter; there is possibly a presynaptic control of the release of 5-HT in response to an action potential arriving at the nerve terminals; the concentration of 5-HT in the synaptic cleft depends on its uptake, diffusion, and metabolism; density and type of receptors atthe target cells determine the immediate effects of 5-HT; few or many intermediary steps may be present before the effect. of 5-HT on its target cells is transduced into a change of brain.activity, which is measurable by electrophysiological or behavioral parameters Two facts considerably complicate the study of central 5-HT mechanisms One is the absence of 5-HT neurons in peripheral
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