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Modern 5-HT receptor classification and 5-HT based drugs
Expert Opinion on Investigational Drugs, 1994Based on operational (agonist and antagonist rank order), transductional (second messenger coupling) and structural (gene and amino acid sequence) criteria, the Nomenclature Committee of the Serotonin Club has discerned four distinct 5-HT receptor types, besides two less well characterised categories including some recombinant and the so-called ‘orphan’
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Expression of 5‐HT2A, 5‐HT2B and 5‐HT2C receptors in the mouse embryo
International Journal of Developmental Neuroscience, 2000AbstractExpression patterns of 5‐HT2A, 5‐HT2B and 5‐HT2C receptors during mouse embryogenesis were investigated using highly specific monoclonal antibodies. Differential and overlapping spatio‐temporal patterns of 5‐HT2A, 5‐HT2B and 5‐HT2C receptor immunoreactivity were observed during active phases of morphogenesis of a variety of embryonic tissues ...
J M, Lauder +3 more
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5-HT antagonists and blockade of neuronal (5-HT) receptors on ganglion cells
General Pharmacology: The Vascular System, 1984Potential changes in superior cervical ganglion cells evoked by 5-HT or the nicotinic agonist, dimethyl-phenyl piperazinium (DMPP), were recorded using the sucrose-gap method and a number of putative 5-HT antagonists tested for potency and selectivity. Selective blockade of 5-HT responses was produced by 5-HT itself and, in increasing order of potency,
H L, Nash, D I, Wallis, G, Ash
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Current Opinion in Pharmacology, 2011
Bone formation and bone resorption, the two processes occurring constantly and in a balanced fashion throughout the skeleton, are regulated by signals as various as local and low range growth factors, hormones, and neuronal outputs. Adding to the long list of molecules involved in these regulations, gut-derived and brain-derived serotonin were recently
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Bone formation and bone resorption, the two processes occurring constantly and in a balanced fashion throughout the skeleton, are regulated by signals as various as local and low range growth factors, hormones, and neuronal outputs. Adding to the long list of molecules involved in these regulations, gut-derived and brain-derived serotonin were recently
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1997
Publisher Summary The hypothesis that serotonin dysfunction may play an important role in depression and the fact that tricyclic antidepressants are monoamine uptake inhibitors and have a considerable affinity as antagonists for cholinergic, histaminergic, and adrenergic receptors and, thus, may cause unwanted severe side effects initiated the search
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Publisher Summary The hypothesis that serotonin dysfunction may play an important role in depression and the fact that tricyclic antidepressants are monoamine uptake inhibitors and have a considerable affinity as antagonists for cholinergic, histaminergic, and adrenergic receptors and, thus, may cause unwanted severe side effects initiated the search
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Regulation of 5-HT Release in the CNS by Presynaptic 5-HT Autoreceptors and by 5-HT Heteroreceptors
2000The amount of serotonin (5-hydroxytryptamine; 5-HT) released from the varicosities of the serotoninergic axon terminals in response to invading action potentials at a given frequency is by no means constant. As generally accepted now, exocytotic release of 5-HT can be significantly modified by presynaptic receptors, i.e.
M. Göthert, E. Schlicker
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Discriminating between 5-HT₃A and 5-HT₃AB receptors.
British journal of pharmacology, 2014The 5-HT3B subunit was first cloned in 1999, and co-expression with the 5-HT3A subunit results in heteromeric 5-HT₃AB receptors that are functionally distinct from homomeric 5-HT₃A receptors. The affinities of competitive ligands at the two receptor subtypes are usually similar, but those of non-competitive antagonists that bind in the pore often ...
A J, Thompson, S C R, Lummis
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Characterisation of heteromeric 5-HT₃ receptors: a focus on the 5-HT₃C and 5-HT₃E subunits
20175-HT₃ receptors are ligand-gated cation channels present in both central and peripheral nervous systems. 5-HT₃ receptor antagonists are used clinically for a range of disorders including irritable bowel syndrome, chemotherapy-induced nausea and depression but have varying efficacy. 5-HT₃ receptors potentially contain five different subunits (A, B, C, D
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Desensitization of Terminal 5-HT Autoreceptors by 5-HT Reuptake Blockers
Archives of General Psychiatry, 1991To the Editor.— We commend Goodman et al 1 for their rigorous study on the effectiveness of fluvoxamine in obsessive-compulsive disorder (OCD) and for the comprehensive and scholarly review on the possible mechanisms of action of 5-hydroxytryptamine (5-HT) reuptake blockers in OCD.
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