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Topic: 5-HT receptors



  
 Serotonin and Hallucinogens
We synthesized the quaternary amine derivative of 5-HT, N,N,N-trimethylserotonin, or 5-HTQ, and found it to bind with higher affinity than 5- HT, and to be quite selective for 5-HT3 receptors.
These receptors were named 5- HT2F receptors; that is, they displayed similarity with the other two members of the 5-HT2 family of receptors.
This, at least in part, explained our findings of more than 15 years earlier that there was a significant correlation between hallucinogenic potency and rat fundus 5-HT receptor affinity.
http://www.phc.vcu.edu/rag/serotonin

  
 Serotonin Receptor Subtypes and Ligands
The pharmacological function of 5-HT receptors is currently unknown; it has been speculated that, on the basis of their localization, they may be involved in motor control, feeding, anxiety, depression, learning, memory consolidation, adaptive behavior, and brain development (
5-HT receptors might be involved in mood and learning, as well as in neuroendocrine and vegetative behaviors.
The controversy surrounding the possible existence of 5-HT receptors in rat brain further confounded 5-HT research.
http://www.acnp.org/g4/GN401000039/Ch039.html   (13719 words)

  
 5-HT receptor - Wikipedia, the free encyclopedia
5-HT receptors are located on the cell membrane of nerve cells and other cell types in animals and mediate the effects of serotonin as the endogenous ligand and of a broad range of pharmaceutical and hallucinogenic drugs.
In the field of neurochemistry, 5-HT receptors are receptors for the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine or 5-HT.
Within these general classes of 5-HT receptors, a number of specific types have been characterized:
http://en.wikipedia.org/wiki/5-HT_receptor   (332 words)

  
 Serotonin - Wikipedia, the free encyclopedia
The pharmacology of 5-HT is extremely complex, with its actions being mediated by a large and diverse range of 5-HT receptors.
From here it is free to diffuse over a relatively large region of space (>20µm) and activate 5-HT receptors located on the dendrites, cell bodies and presynaptic terminals of adjacent neurons.
As with all neurotransmitters, the actual effects of 5-HT on the human mood and state of mind, and its role in consciousness, are very difficult to ascertain.
http://en.wikipedia.org/wiki/5-HT   (988 words)

  
 Indoleamines:  The Role of Serotonin in Clinical Disorders
One of the systems involving 5-HT where some of the neurotransmitters and receptors are better understood involves the systems regulating the control of nausea and emesis (83).
The diverse and complex nature of 5-HT involvement in different clinical conditions can be illustrated with 5 clinical examples where the variability in the clinical response to 5-HT based treatments across widely different clinical conditions reflects the complexity of the underlying 5-HT systems.
Figure 5 illustrates the robust positive results from 4 studies of sumatriplin in headache (7).
http://www.acnp.org/G4/GN401000045/CH.html   (988 words)

  
 Expression of Recombinant Homo-oligomeric 5-Hydroxytryptamine(3) Receptors Provides New Insights into Their Maturation and Structure -- Green et al. 270 (11): 6056 -- Journal of Biological Chemistry
Small quantities of the 5-HT receptor have been purified from cell lines by various groups(15, 16, 17), and their analyses of the purified protein seem to indicate that the native receptor is a hetero-oligomer.
Although this is obviously a simplification (otherwise all subunits would readily form homo-oligomeric channels), single subunits forming functional receptors must represent some sort of consensus structure.
One important consequence of this is that it precludes the use of E.
http://www.jbc.org/cgi/content/full/270/11/6056   (5869 words)

  
 Pharmacological Characterization of a Serotonin Receptor (5-HT7) Stimulating cAMP Production in Human Corneal Epithelial Cells -- Crider et al. 44 (11): 4837 -- Investigative Ophthalmology & Visual Science
from the 5-HT and 5-HT receptors by its high-affinity and
Bentley, JC, Bourson, A, Boess, FG, et al (1999) Investigation of stretching behavior induced by selective 5-HT receptor antagonist, Ro-04-6790, in rats Br J Pharmacol 126,1537-1542
39% homology with the 5-HT receptor and 46% with the 5-HT receptor.
http://www.iovs.org/cgi/content/full/44/11/4837   (4460 words)

  
 Effects of ECS on 5-HT-1A Receptor Sensitivity in Hypothalamus: In Vivo Studies
Increased serotonergic transmission mediated by an increase in the sensitivity of post-synaptic 5-HT-1A receptors in the hippocampus has been proposed as a mechanism of action for electroconvulsive shock (ECS) in animals, and by inference for electroconvulsive therapy (ECT) in humans.
We conclude that in contrast to the effects of ECS on 5-HT-1A receptor in the hippocampus in animals, ECT in humans does not induce an increase in sensitivity of post-synaptic 5-HT-1A receptors in the hypothalamus.
Since activation of these receptors reduces firing of serotonergic neurons and 5-HT release, reduction in their sensitivity would be associated with increased 5-HT release and, hence, an increase in serotonergic transmission in the hypothalamus.
http://www.hadassah.org.il/Atarim/biopsych/abstracts/5.html   (364 words)

  
 Dept. of Neuroscience thesis
Mutant 5-HT,B receptors were constructed and the importance of specific amino acid residues in agonist and antagonist binding as well as G protein coupling was investigated by radioligand binding and functional assays on receptors stably expressed in Chinese hamster ovary cells.
The 5-hydroxytryptamine (5-HT, serotonin) B receptor is one of thirteen G protein-coupled 5-HT receptors.
The presynaptic S-HT~B receptor, which is broadly distributed throughout brain of mammals, regulates 5-HT release and may be involved in depression and anxiety disorders.
http://www.neuro.uu.se/spikblad/granas.html   (377 words)

  
 Pharmacological Characterization of an Adenylyl Cyclase-Coupled 5-HT Receptor in Aplysia: Comparison With Mammalian 5-HT Receptors -- Cohen et al. 89 (3): 1440 -- Journal of Neurophysiology
The correlations with the 5-HT and 5-HT receptors
Ap5-HT, had no affect on 5-HT stimulation of AC.
Stimulation of AC activity by 5 µM 5-HT in the presence of antagonist is expressed as percent of 5-HT stimulation in the absence of antagonist.
http://jn.physiology.org/cgi/content/full/89/3/1440   (8978 words)

  
 Physiological and Genomic Consequences of Intermittent Hypoxia: Selected Contribution: Phrenic long-term facilitation requires 5-HT receptor activation during but not following episodic hypoxia -- Fuller et al. 90 (5): 2001 -- Journal of Applied Physiology
5-HT) receptor antagonist (methysergide; Ref. 1) or an antagonist
of 5-HT receptor blockade on XII LTF was not determined in that
Phrenic long-term facilitation requires NMDA receptors in the phrenic motonucleus in rats
http://jap.physiology.org/cgi/content/full/90/5/2001   (3887 words)

  
 Cloning and Functional Expression of an Aplysia 5-HT Receptor Negatively Coupled to Adenylate Cyclase -- Angers et al. 18 (15): 5586 -- Journal of Neuroscience
This view is in agreement with previous phylogenetic studies that suggested that the major subfamilies of 5-HT receptors diverged
Boess FG, Martin IL (1994) Molecular biology of 5-HT receptors.
the divergence of the 5-HT receptor subtypes in vertebrates, and
http://www.jneurosci.org/cgi/content/full/18/15/5586   (5342 words)

  
 5-hydroxytryptamine-moduline, a new endogenous cerebral peptide, controls the serotonergic activity via its specific interaction with 5- hydroxytryptamine1B/1D receptors -- Massot et al. 50 (4): 752 -- Molecular Pharmacology
5-hydroxytryptamine-moduline, a new endogenous cerebral peptide, controls the serotonergic activity via its specific interaction with 5- hydroxytryptamine1B/1D receptors -- Massot et al.
Articles by Massot, O. Articles by Fillion, G. 5-hydroxytryptamine-moduline, a new endogenous cerebral peptide, controls the serotonergic activity via its specific interaction with 5- hydroxytryptamine1B/1D receptors
Pharmacol., March 5, 2003; 138(5): 795 - 800.
http://molpharm.aspetjournals.org/cgi/content/abstract/50/4/752?maxtoshow=&HITS=10&hits=10&RESULTFORMAT=&fulltext="5-ht-moduline"&searchid=1030440595250_477&stored_search=&FIRSTINDEX=&fdate=1/1/1965&tdate=8/31/2002&jc=all   (5342 words)

  
 Drugs With Prominent 5-HT Receptor Activity
This slide lists drugs that interact with 5-HT receptors.
There are seven families of 5-HT receptors (5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7), and at least 15 subpopulations have been cloned.
Giving & Support © 2005 NYU Medical Center
http://www.med.nyu.edu/psych/psychiatrist/depression/slides/sld012.html   (40 words)

  
 Canadian Journal of Psychiatry - In Review (Feb 2001)
 Neuropharmacological research into 5-HT receptors is likely to continue to be of significant interest to general psychiatry and to the evaluation and treatment of sexual disorders.
Perhaps mutations of the 5-HT receptor or subreceptor structures will be found to play a role in a variety of psychiatric disorders (3).
It is also possible that other 5-HT receptor subtypes will be isolated or that further variations in receptor subtypes will be found.
http://www.cpa-apc.org/Publications/Archives/CJP/2001/Feb/Inreview2.asp   (947 words)

  
 Distinct Mechanisms Regulate 5-HT(2) and Thrombin Receptor Desensitization -- Vouret-Craviari et al. 270 (9): 4813 -- Journal of Biological Chemistry
5 A ( left panel), expression of both the full-length and truncated 5-HT receptors can be detected in 293 cells by Western blot analysis following transient transfection.
5 that the same quantity of receptor was present in lysates from control and 5-HT-stimulated cells.
In fact, the sequestration pathway has been proposed to be an important mechanism by which cells re-establish their normal responsiveness to agonists following removal of the stimulus( 4, 5).
http://www.jbc.org/cgi/content/full/270/9/4813   (947 words)

  
 Serotonin 5-HT(6) receptor antagonists and memory
ATIONALE: 5-HT(6) receptors are predominantly located in the brain and may be involved in cognitive processes.
The aim of this study was to assess the effects of two potent and selective 5-HT(6) receptor antagonists, SB-271046-A and SB-357134-A, on learning and memory in the rat.
These data indicate that 5-HT(6) receptor antagonism may be involved in cognitive function.
http://www.nootropic.com/5-ht6   (183 words)

  
 5-HT7 Receptor Research -- Neurotransmitter.net
When LH release was suppressed by 5 microg oestradiol benzoate, SB-269970-A (0.5 and 2 microg) did not elevate levels, indicating it is unlikely that 5-HT7 receptors mediate a tonic inhibition on release but rather are involved in terminating the pre-ovulatory LH surge.
As both 8-OH-DPAT and ritanserin have moderate activity at the 5-HT7 receptor subtype, the possibility that this subtype might mediate their effects in the zona incerta has been investigated.
In rat tissues, three 5-HT7 isoforms, here called 5-HT7(a), 5- HT7(b), and 5-HT7(c), are found.
http://www.neurotransmitter.net/seven.html   (183 words)

  
 Serotonin Receptor Subtypes and Ligands
5-HT receptors might be involved in mood and learning, as well as in neuroendocrine and vegetative behaviors.
The pharmacological function of 5-HT receptors is currently unknown; it has been speculated that, on the basis of their localization, they may be involved in motor control, feeding, anxiety, depression, learning, memory consolidation, adaptive behavior, and brain development (
Although 5-HT receptors represent ion channel receptors, whereas 5-HT receptors represent G-protein coupled receptors, much of the early work in 5-HT research was facilitated by 5-HT ligands; that is, a number of 5-HT ligands were shown to be active at 5-HT receptors.
http://www.acnp.org/G4/GN401000039/Ch039.html   (183 words)

  
 Serotonin Receptor Subtypes and Ligands
Evidence was subsequently provided suggesting that 5-HT receptors exist in a high-affinity state and a low-affinity state; under normal conditions, this equilibrium is heavily in favor of the low-affinity state, and the tritiated antagonist ketanserin binds at both states with comparable affinity.
For example, ketanserin, the most widely used 5-HT antagonist, has been reported to bind with as little as 2-fold to as much as 140-fold selectivity for 5-HT vs. 5-HT receptors.
With the subsequent discovery of 5-HT receptors and the finding that many 5-HT ligands bind nearly equally well at both types of receptors, came the realization that some of the roles attributed to 5-HT receptors may in fact be mediated by 5-HT receptors.
http://www.acnp.org/G4/GN401000039/Ch039.html   (183 words)

  
 Electrophysiology of Serotonin Receptor Subtypes and Signal Transduction Pathways
For example, while 5-HT agonists are directly inhibitory upon serotonergic neurons in the raphe nuclei (possibly at doses insufficient to affect postsynaptic 5-HT receptors), the net effect of this inhibition may be disinhibitory for postsynaptic neurons that express 5-HT receptors and simultaneously disfacilitatory for postsynaptic neurons that express 5-HT, and 5-HT receptors.
With few exceptions (e.g., facial nucleus and the nucleus tractus solitarius), relatively low concentrations of 5-HT receptors or mRNA expression are found in the brainstem.
In brain slices of the nucleus prepositus hypoglossi, focal electrical stimulation evokes inhibitory postsynaptic potentials which have been shown to be mediated by endogenous 5-HT acting on 5-HT receptors to activate a K
http://www.acnp.org/g4/GN401000043/Ch043.html   (183 words)

  
 The Selective Serotonin2A Receptor Antagonist, MDL100,907, Elicits a Specific Interoceptive Cue in Rats
Millan MJ, Peglion J-L, Lavielle G, Perrin-Monneyron S (1997): 5-HT receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists.
Interest in 5-HT receptors has been reinforced by evidence that their blockade may contribute to the distinctive functional profile of the "atypical" antipsychotic, clozapine, and, possibly, other novel agents employed for management of psychotic states (Roth and Meltzer 1995).
1998), and employing the 5-HT antagonist, SB206,553, and the selective 5-HT antagonist, SB242,084, it was shown that 5-HT receptors likewise mediate DS properties of the novel, mixed 5-HT agonist, RO60,0175 ((S)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine; Dekeyne et al.
http://www.nature.com/npp/journal/v26/n4/full/1395832a.html   (2174 words)

  
 5-HT modulates multiple conductances in immature rat rostral ventrolateral medulla neurones in vitro -- Hwang and Dun 517 (1): 217 -- The Journal of Physiology Online
To minimize the potential interference by subtypes of 5-HT receptors coexisting in a single RVLM neurone, experiments were conducted in the presence of the 5-HT receptor antagonist PBD or the 5-HT receptor antagonist ketanserin to isolate the specific response.
To eliminate possible contamination by the activation of undesired 5-HT receptors, the 5-HT receptor antagonist ketanserin or the 5-HT receptor antagonist PBD was included in the perfusing solution so that the conductances underlying I
The following compounds were used: TTX, pindobind-5-HT (PBD) and ketanserin from Research Biochemicals Inc.; 5-HT creatinine sulfate and other chemicals from Sigma.
http://jp.physoc.org/cgi/content/full/517/1/217   (2174 words)

  
 The Selective Serotonin2A Receptor Antagonist, MDL100,907, Elicits a Specific Interoceptive Cue in Rats
1998), and employing the 5-HT antagonist, SB206,553, and the selective 5-HT antagonist, SB242,084, it was shown that 5-HT receptors likewise mediate DS properties of the novel, mixed 5-HT agonist, RO60,0175 ((S)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine; Dekeyne et al.
Further, several 5-HT antagonists failed to generalize to pizotifen, which interacts with many other sites, including histaminergic receptors, which play a major role in its DS properties (Minnema et al.
In distinction, the selective 5-HT antagonist, SB204,741 (0.63 and 10.0 mg/kg), the 5-HT antagonist, SB206,553 (0.16 and 2.5 mg/kg) and the selective 5-HT antagonists, SB242,084 (2.5 and 10.0 mg/kg,) and RS102221 (2.5 and 10.0 mg/kg), did not significantly generalize.
http://www.nature.com/npp/journal/v26/n4/full/1395832a.html   (2174 words)

  
 Serotonin Receptor [Definition]
Note that there is no 5-HT receptor since, after the receptor was cloned and further characterised, it was found to have more in common with the 5-HT family of receptors and was redesignated as the 5-HT receptor.
[click for more], 5-HT receptors are receptors for the neurotransmitter Neurotransmitters are chemicals that are used to relay, amplify and modulate electrical signals between a presynaptic and a postsynaptic neuron.
5-HT receptors are located on the cell membrane A component of every biological cell, the selectively permeable cell membrane (or plasma membrane) is a thin and structured bilayer of phospholipid and protein molecules that envelopes the cell.
http://www.wikimirror.com/Serotonin_receptor   (2174 words)

  
 British Journal of Pharmacology - Abstract of article: The inhibition of cholera toxin-induced 5-HT release by the 5-HT3 receptor antagonist, granisetron, in the rat
Enterochromaffin cells possess numerous receptors that, under basal conditions, modulate 5-HT release.
The simultaneous inhibition of 5-HT release and fluid secretion by granisetron suggests that 5-HT release from enterochromaffin cells is potentiated by endogenous 5-HT receptors.
Net fluid movement was determined by small intestinal perfusion or gravimetry and small intestinal and luminal fluid 5-HT levels were determined by HPLC with fluorimetric detection.
http://www.nature.com/bjp/journal/v130/n5/abs/0703414a.html   (372 words)

  
 Serotonin Receptors
Chronic or repeated administration of antidepressant drugs, such as MAO inhibitors or inhibitors of serotonin uptake, or 5-HT receptor agonists to laboratory rats results in a desensitization of behavioral and electrophysiological responses believed to be mediated by 5-HT receptors.
The 5-HT receptor originally was described in cultured murine collicular neurons as a serotonin receptor coupled to the stimulation of adenylyl cyclase activity, possessing pharmacological characteristics distinct from those of the 5-HT or 5-HT receptors.
The 5-HT receptor in rats and mice and the 5-HT receptor in bovine and human brain are located in high density in the basal ganglia, particularly in the globus pallidus and the substantia nigra (Table 13-2).
http://www.ncbi.nlm.nih.gov/books/bv.fcgi?call=bv.View..ShowSection&rid=bnchm.section.963   (4654 words)

  
 Serotonin-induced muscular activity in Schistosoma mansoni larval stages: importance of 5-HT transport and role in daughter sporocyst production.
Serotonin-induced motility of in vitro-derived sporocysts is not inhibited by antidepressant compounds, e.g., fluoxetine, that block 5-HT transport, suggesting that the receptors responsible for motility responses to 5-HT are surface exposed.
In the present study, we investigated the importance of 5-HT transporter activity in the manifestation of these 5-HT-induced motility changes, and further examined the role of 5-HT in the development of daughter sporocysts in vitro.
Moreover, we demonstrate a strong correlation between endogenous 5-HT levels and basal mother sporocyst muscle activity.
http://counsellingresource.com/medications-research/2005/08/21/serotonin-induced-muscular-activity-in-schistosoma-mansoni-larval-stages-importance-of-5-ht-transport-and-role-in-daughter-sporocyst-production   (4654 words)

  
 Molecular Mechanisms and Therapeutical Implications of Intramembrane Receptor/Receptor Interactions among Heptahelical Receptors with Examples from the Striatopallidal GABA Neurons -- Agnati et al. 55 (3): 509 -- Pharmacological Reviews
5-HT receptor and 5-HT receptor homomers and 5-HT receptor heteromers.
Heteromerization of {delta} and {kappa} Opioid Receptors and of µ and {delta} Opioid Receptors.
Interactions between Adenosine, Dopamine, and Glutamate Metabotropic Receptors in the GABAergic Striatoentopeduncular and Striatonigral Neurons.
http://pharmrev.aspetjournals.org/cgi/content/full/55/3/509   (5247 words)

  
 Serotonergic Inhibition of the T-Type and High Voltage-Activated Ca2+ Currents in the Primary Sensory Neurons of Xenopus Larvae -- Sun and Dale 17 (18): 6839 -- Journal of Neuroscience
The inhibition of HVA Ca currents by 5-HT is dose-dependent and mediated via 5-HT and 5-HT receptors.
In R-B neurons both HVA and T-type currents were inhibited by 5-HT in a voltage-independent manner via the same receptors.
Approximately 70% of the actions of 5-HT on HVA
http://www.jneurosci.org/cgi/content/full/17/18/6839   (5247 words)

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