The Second IUPHAR Satellite Meeting on Serotonin was held under the auspices of the Serotonin Club in Basel, Switzerland in July 1990. The scope was wide, ranging from molecular biology through in vitro and in vivo pharmacology to new drug tools and their clinical signifi cance. There were three invited review lectures, by J. M. Palacios, D. I. Wallis and A. Kaumann, and S. Peroutka gave the first Serotonin Club Irvine H. Page Lecture. The rest of the oral programme was put together by the Scientific Organizing Committee based on volunteered research contributions. The invited review…mehr
The Second IUPHAR Satellite Meeting on Serotonin was held under the auspices of the Serotonin Club in Basel, Switzerland in July 1990. The scope was wide, ranging from molecular biology through in vitro and in vivo pharmacology to new drug tools and their clinical signifi cance. There were three invited review lectures, by J. M. Palacios, D. I. Wallis and A. Kaumann, and S. Peroutka gave the first Serotonin Club Irvine H. Page Lecture. The rest of the oral programme was put together by the Scientific Organizing Committee based on volunteered research contributions. The invited review lecturers, the platform speak ers and selected poster contributors were invited to write up their contributions for inclusion in this volume. Most complied and this book is the result of their efforts. When instructing the authors prior to the meeting, we emphasized that selected new data should be put in the context of the literature findings. In this way we hoped to achieve topicality yet preserve the review perspective which facilitates its appreciation by the non-special ist. It was truly a pleasure to read the interesting papers which resulted and to prepare them for publication. We believe they convey to a remarkable degree the spirit of what was generally felt to be a highly stimulating exchange of information on matters serotonergic which took place in Basel last July.
I: Molecular Pharmacology, Cell Biology, Binding Sites and Receptors.- A tribute to Dr. Irvine H. Page.- Molecular neuroanatomy of 5-HT receptors.- Cloning and expression of a human 5-HT1D receptor.- Developmental and synaptic regulation of 5-HT2 and 5-HT1C serotonin receptors.- Serotonin trophic factors in development, plasticity and aging.- A neurotrophic factor - SNTF - for serotonergic neurons.- Molecular mechanisms of action induced by 5-HT3 receptors in a neuronal cell line and by 5-HT2 receptors in a glial cell line.- Characterization of 5-HT3 receptor mediated electrical responses in nodose ganglion neurones and clonal neuroblastoma cells maintained in culture.- Specific antibodies as new tools for studies of central 5-HT1A receptors.- 5-HT1C 5-HT1D and 5-HT2 receptors in mammalian brain: Multiple affinity states with a different regional distribution.- Second messengers in the definition of 5-HT receptors.- 5-HT1P receptors in the bowel: G protein coupling, localization and function.- Is contraction to serotonin mediated via 5-HT1C receptor activation in rat stomach fundus?.- Further definition of the 5-HT receptor mediating contraction of rat stomach fundus: relation to 5-HT1D recognition sites.- Temperature dependence of agonist and antagonist affinity constants at 5-HT1 -like and 5-HT2 receptors.- Characterization of 5-HT3-like receptors in the rat cortex: Electrophysiological and biochemical studies.- Binding characteristics of a quarternary amine analog of serotonin: 5-HTQ.- 5-HT1-like receptors unrelated to the known binding sites?.- II: Peripheral and Central Pharmacology.- The electrophysiology of 5-HT.- Pharmacological characterization of brain 5-HT4 receptors: Relationship between the effects of indole, benzamide and azabicycloalkylbenzimidazolonederivatives.- Pharmacological properties of the putative 5-HT4 receptor in guinea-pig ileum and rat oesophagus: Role in peristalsis.- 5-HT1D and 5-HT4 receptor agonists stimulate the peristaltic reflex in the isolated guinea pig ileum.- The 5-HT4 receptor mediating tachycardia in the pig.- Contractile 5-HT1D receptors in human brain vessels.- Human, monkey and dog coronary artery responses to serotonin and 5-carboxamidotryptamine.- 5-Carboxamidotryptamine induced renal vasoconstriction in the dog.- The subretrofacial nucleus: A major site of action for the cardiovascular effects of 5-HT1A and 5-HT2 agonist drugs.- Cardiovascular effects of injection of 5-HT, 8-OH-DPAT and flesinoxan into the hypothalamus of the rat.- Pharmacological characterization of the receptor mediating 5-HT evoked motoneuronal depolarization in vitro.- Stimulation of 5-HT3 receptors inhibits release of endogenous noradrenaline from hypothalamus.- Antagonism of serotonin agonist-elicited increases in serum corticosterone concentration in rats.- Influence of 5-HT1A and 5-HT2 receptor agonists on blood glucose and insulin levels.- Novel in vivo models of 5-HT1A receptor-mediated activity: 8-OH-DPAT-induced spontaneous tail-flicks and inhibition of morphine-evoked antinociception.- Evidence that the unilateral activation of 5-HT1D receptors in the substantia nigra of the guinea-pig elicits contralateral rotation.- III: Pathophysiological Roles and Prospects for New Therapies.- 5-Hydroxytryptamine and the human heart.- The effects of BRL 24924 (renzapride) on secretion of gastric acid and pepsin in dogs.- Constipation evoked by 5-HT3 receptor antagonists.- Subchronic D-fenfluramine treatment enhances the immunological competence of old female Fischer 344 rats.- Serotonin as a vascular smooth muscle cell mitogen.- Serotonin, the endothelium and the coronary circulation.- Effects of selective 5-HT, receptor antagonists on some haemodynamic changes produced by experimental pulmonary embolism in rabbits.- The vasoconstrictor action of sumatriptan on human isolated dura mater.- Influence of 5-HT3 receptor antagonists on limbic-cortical circuitry.- Utilization of zacopride and its R- and S-enantiomers in studies of 5-HT3 receptor "subtypes".- CP-93,129: A potent and selective agonist for the serotonin (5-HT1B) receptor and rotationally restricted analog of RU-24,969.- Differentiation of 8-OH-DPAT and ipsapirone in rat models of 5-HT1A receptor function.- Initial studies in man to characterise MDL 73,000EF, a novel 5-HT1A receptor ligand and putative anxiolytic.- 8-OH-DPAT-induced hypothermia in rodents. A specific model of 5-HT1A autoreceptor function?.- Serotonin release is responsible for the locomotor hyperactivity in rats induced by derivatives of amphetamine related to MDMA.
I: Molecular Pharmacology, Cell Biology, Binding Sites and Receptors.- A tribute to Dr. Irvine H. Page.- Molecular neuroanatomy of 5-HT receptors.- Cloning and expression of a human 5-HT1D receptor.- Developmental and synaptic regulation of 5-HT2 and 5-HT1C serotonin receptors.- Serotonin trophic factors in development, plasticity and aging.- A neurotrophic factor - SNTF - for serotonergic neurons.- Molecular mechanisms of action induced by 5-HT3 receptors in a neuronal cell line and by 5-HT2 receptors in a glial cell line.- Characterization of 5-HT3 receptor mediated electrical responses in nodose ganglion neurones and clonal neuroblastoma cells maintained in culture.- Specific antibodies as new tools for studies of central 5-HT1A receptors.- 5-HT1C 5-HT1D and 5-HT2 receptors in mammalian brain: Multiple affinity states with a different regional distribution.- Second messengers in the definition of 5-HT receptors.- 5-HT1P receptors in the bowel: G protein coupling, localization and function.- Is contraction to serotonin mediated via 5-HT1C receptor activation in rat stomach fundus?.- Further definition of the 5-HT receptor mediating contraction of rat stomach fundus: relation to 5-HT1D recognition sites.- Temperature dependence of agonist and antagonist affinity constants at 5-HT1 -like and 5-HT2 receptors.- Characterization of 5-HT3-like receptors in the rat cortex: Electrophysiological and biochemical studies.- Binding characteristics of a quarternary amine analog of serotonin: 5-HTQ.- 5-HT1-like receptors unrelated to the known binding sites?.- II: Peripheral and Central Pharmacology.- The electrophysiology of 5-HT.- Pharmacological characterization of brain 5-HT4 receptors: Relationship between the effects of indole, benzamide and azabicycloalkylbenzimidazolonederivatives.- Pharmacological properties of the putative 5-HT4 receptor in guinea-pig ileum and rat oesophagus: Role in peristalsis.- 5-HT1D and 5-HT4 receptor agonists stimulate the peristaltic reflex in the isolated guinea pig ileum.- The 5-HT4 receptor mediating tachycardia in the pig.- Contractile 5-HT1D receptors in human brain vessels.- Human, monkey and dog coronary artery responses to serotonin and 5-carboxamidotryptamine.- 5-Carboxamidotryptamine induced renal vasoconstriction in the dog.- The subretrofacial nucleus: A major site of action for the cardiovascular effects of 5-HT1A and 5-HT2 agonist drugs.- Cardiovascular effects of injection of 5-HT, 8-OH-DPAT and flesinoxan into the hypothalamus of the rat.- Pharmacological characterization of the receptor mediating 5-HT evoked motoneuronal depolarization in vitro.- Stimulation of 5-HT3 receptors inhibits release of endogenous noradrenaline from hypothalamus.- Antagonism of serotonin agonist-elicited increases in serum corticosterone concentration in rats.- Influence of 5-HT1A and 5-HT2 receptor agonists on blood glucose and insulin levels.- Novel in vivo models of 5-HT1A receptor-mediated activity: 8-OH-DPAT-induced spontaneous tail-flicks and inhibition of morphine-evoked antinociception.- Evidence that the unilateral activation of 5-HT1D receptors in the substantia nigra of the guinea-pig elicits contralateral rotation.- III: Pathophysiological Roles and Prospects for New Therapies.- 5-Hydroxytryptamine and the human heart.- The effects of BRL 24924 (renzapride) on secretion of gastric acid and pepsin in dogs.- Constipation evoked by 5-HT3 receptor antagonists.- Subchronic D-fenfluramine treatment enhances the immunological competence of old female Fischer 344 rats.- Serotonin as a vascular smooth muscle cell mitogen.- Serotonin, the endothelium and the coronary circulation.- Effects of selective 5-HT, receptor antagonists on some haemodynamic changes produced by experimental pulmonary embolism in rabbits.- The vasoconstrictor action of sumatriptan on human isolated dura mater.- Influence of 5-HT3 receptor antagonists on limbic-cortical circuitry.- Utilization of zacopride and its R- and S-enantiomers in studies of 5-HT3 receptor "subtypes".- CP-93,129: A potent and selective agonist for the serotonin (5-HT1B) receptor and rotationally restricted analog of RU-24,969.- Differentiation of 8-OH-DPAT and ipsapirone in rat models of 5-HT1A receptor function.- Initial studies in man to characterise MDL 73,000EF, a novel 5-HT1A receptor ligand and putative anxiolytic.- 8-OH-DPAT-induced hypothermia in rodents. A specific model of 5-HT1A autoreceptor function?.- Serotonin release is responsible for the locomotor hyperactivity in rats induced by derivatives of amphetamine related to MDMA.
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