Journal ArticleDOI
Discrimination of Multiple [3H]5-Hydroxytryptamine Binding Sites by the Neuroleptic Spiperone in Rat Brain
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Saturation studies of [3H]5‐HT binding assayed in the absence or presence of 1 μM‐spiperone reveal a parallel shift in the Scatchard plot with no change in the dissociation constant of [2‐12 nM], but a significant decrease in the number of specific binding sites.Abstract:
Certain neuroleptic drugs, such as spiperone and (+) butaclamol, can discriminate between two populations of [3H]5-hydroxytryptamine ([3H]5-HT) binding sites in rat brain. The butyrophenone neuroleptic spiperone shows the greatest selectivity for these two binding sites, having at least a 3000-fold difference between its dissociation constants (2-12 nM versus 35,000 nM) for the high- and low-affinity sites, respectively. Inhibition of [3H]5-HT binding by spiperone in rat frontal cortex and corpus striatum yields distinctly biphasic inhibition curves with Hill slopes significantly less than unity. Results from nonlinear regression analysis of these inhibition studies were consistent with a two-site model in each brain region. In the frontal cortex the high-affinity neuroleptic sites comprised about 60% of the total [3/H]5-HT binding sites whereas in the corpus striatum they accounted for only 20% of the sites. Furthermore, saturation studies of [3H]5-HT binding assayed in the absence or presence of 1 μM-spiperone (a concentration that completely blocks the high-affinity site while having minimal activity at the low-affinity site) reveal a parallel shift in the Scatchard plot with no change in the dissociation constant of [3H]5-HT, but a significant decrease (64% in frontal cortex or 28% in corpus striatum) in the number of specific binding sites. These observations are consistent with the existence of at least two populations of [3H]5-HT binding sites having a differential regional distribution in rat brain.read more
Citations
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Journal ArticleDOI
A review of central 5-HT receptors and their function
Nicholas M. Barnes,Trevor Sharp +1 more
TL;DR: A number of 5-HT receptor ligands are currently utilised, or are in clinical development, to reduce the symptoms of CNS dysfunction and the functional responses attributed to each receptor in the brain are reviewed.
Journal ArticleDOI
Quantitative autoradiographic mapping of serotonin receptors in the rat brain. I. Serotonin-1 receptors.
Angel Pazos,José Palacios +1 more
TL;DR: The distribution of serotonin-1 (5-HT1) receptors in the rat brain was studied by light microscopic quantitative autoradiography and the existence of 'selective' areas allowed a detailed pharmacological characterization of these sites to be made in a more precise manner than has been attained in membrane-binding studies.
Journal ArticleDOI
Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine
P.B. Bradley,G. Engel,Wasyl Feniuk,John R. Fozard,Patrick P.A. Humphrey,Derek N. Middlemiss,Ewan J. Mylecharane,B.P. Richardson,Pramod R. Saxena +8 more
TL;DR: This classification of 5-HT receptors into three main groups is based largely, but not exclusively, on data from studies in isolated peripheral tissues where definitive classification is possible, and is believed that this working classification will be relevant to functional responses to 5- HT in the central nervous system.
Book
Brainstem control of wakefulness and sleep
TL;DR: A monograph communicating the current realities and future possibilities of unifying basic studies on anatomy and cellular physiology with investigations of the behavioral and physiological events of waking and sleep.
Journal ArticleDOI
Molecular biology of 5-HT receptors
F.G. Boess,I.L. Martin +1 more
TL;DR: The receptors through which serotonin (5-hydroxytryptamine, 5-HT) produces its effects have been the subject of intense investigation, initially using both in vivo and in vitro pharmacological methods, and later radioligand binding.
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