5-HT receptor - Factbites

5-HT receptor - Factbites
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Topic: 5-HT receptor

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	5-HT receptor - Wikipedia, the free encyclopedia
		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.
		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.
		With the exception of the 5-HT receptor, a ligand gated ion channel, all other 5-HT receptors are G protein coupled seven transmembrane (or heptahelical) receptors that activate an intracellular second messenger cascade.
	en.wikipedia.org /wiki/5-HT_receptor (332 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
		39% homology with the 5-HT receptor and 46% with the 5-HT receptor.
		from the 5-HT and 5-HT receptors by its high-affinity and
		The 5-HT receptor subtypes (5-HT and 5-HT) are negatively coupled to adenylyl cyclase.
	www.iovs.org /cgi/content/full/44/11/4837 (4460 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
		the divergence of the 5-HT receptor subtypes in vertebrates, and
		Boess FG, Martin IL (1994) Molecular biology of 5-HT receptors.
		This view is in agreement with previous phylogenetic studies that suggested that the major subfamilies of 5-HT receptors diverged
	www.jneurosci.org /cgi/content/full/18/15/5586 (5342 words)

	Roles of 5-HT receptors in the release and action of secretin on pancreatic secretion in rats -- Li et al. 280 (4): 595 -- AJP - Gastrointestinal and Liver Physiology
		(a 5-HT receptor antagonist) was purchased from Glaxo-Wellcome.
		antagonist), ketanserin (a 5-HT receptor antagonist), and SDZ-205,557
		Values represent means ± SE from 5 or 6 rats in each group.
	ajpgi.physiology.org /cgi/content/full/280/4/G595 (5259 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.
	en.wikipedia.org /wiki/5-HT (988 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
		Inhibition by methiothepin of the AC-coupled 5-HT receptor in Aplysia SNs
		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.
	jn.physiology.org /cgi/content/full/89/3/1440 (8978 words)

	Effects of ECS on 5-HT-1A Receptor Sensitivity in Hypothalamus: In Vivo Studies
		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.
		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.
		We have used in vivo microdialysis to measure 5-HT levels and 5-HT-1A receptor function in the rat hypothalamus, and neuroendocrine challenge tests to determine the effects of administration of a 5-HT-1A receptor agonist on activity of the hypothalamic-pituitary-adrenal axis in depressed patients and control subjects.
	www.hadassah.org.il /Atarim/biopsych/abstracts/5.html (364 words)

	Serotonin Receptor Subtypes and Ligands
		5-HT is an indolealkylamine that binds to all populations of 5-HT receptors.
		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.
		5-HT receptors might be involved in mood and learning, as well as in neuroendocrine and vegetative behaviors.
	www.acnp.org /g4/GN401000039/Ch039.html (13719 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.
		The receptor was eluted from the resin using 10 bed volumes of the medium salt buffer containing 0.6% CHAPS and 0.1 mM quipazine.
		The overall yield of purified receptor was 100-200 µg of protein from 3 liters of infected Sf9 cells.
	www.jbc.org /cgi/content/full/270/11/6056 (5869 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.
	www.neuro.uu.se /spikblad/granas.html (377 words)

	SUB Göttingen - Dissertationen - Papoucheva, Ekaterina: Die Funktionelle Rolle der Palmitilierung des 5-HT 1A Rezeptor
		In the present study, we verified that the mouse 5-hydroxytryptamine(1A) (5-HT(1A)) receptor is modified by palmitic acid, which is covalently attached to the protein through a thioester-type bond.
		Block of protein synthesis by cycloheximide resulted in a significant reduction of receptor acylation, suggesting that palmitoylation occurs early after synthesis of the 5-HT(1A) receptor.
		To address the functional role of 5-HT(1A) receptor acylation, we have analyzed the ability of acylation-deficient mutants to interact with heterotrimeric G(i) protein and to modulate downstream effectors.
	webdoc.sub.gwdg.de /diss/2005/papoucheva/index.html (378 words)

	Canadian Journal of Psychiatry - In Review (Feb 2001)
		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.
		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.
	www.cpa-apc.org /Publications/Archives/CJP/2001/Feb/Inreview2.asp (947 words)

	Serotonin 5-HT(6) receptor antagonists and memory
		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.
		ATIONALE: 5-HT(6) receptors are predominantly located in the brain and may be involved in cognitive processes.
		These data indicate that 5-HT(6) receptor antagonism may be involved in cognitive function.
	www.nootropic.com /5-ht6 (183 words)

	Effect of a Serotonin Receptor Antagonist on Interleukin-6-Induced Pulmonary Hypertension in Rats -- Miyata et al. 119 (2): 554 -- Chest
		The expression of the 5-HT receptor messenger RNA was observed
		PCR was performed to detect the expression of the 5-HT receptor messenger RNA in the lung specimen.
		on serotonin release and the expression of the 5-HT receptor
	www.chestjournal.org /cgi/content/full/119/2/554 (3861 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
		Spinal serotonin receptor activation is necessary for phrenic long term facilitation following episodic hypoxia.
	jap.physiology.org /cgi/content/full/90/5/2001 (3887 words)

	gpcr.pep
		5-HYDROXYTRYPTAMINE 2A RECEPTOR (5-HT-2A) (SEROTONIN RECEPTOR) (5-HT-2) (5-HT2A).
		5-HYDROXYTRYPTAMINE 1A RECEPTOR (5-HT-1A) (SEROTONIN RECEPTOR) (5- HT1A).
		5-HYDROXYTRYPTAMINE 7 RECEPTOR (5-HT-7) (5-HT-X) (SEROTONIN RECEPTOR) (5HT7) (GPRFO).
	www.research.ibm.com /splash/gpcr/gpcr.pep (905 words)

	Drugs With Prominent 5-HT Receptor Activity
		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.
		This slide lists drugs that interact with 5-HT receptors.
		Giving & Support © 2005 NYU Medical Center
	www.med.nyu.edu /psych/psychiatrist/depression/slides/sld012.html (40 words)

	Abstract: Brain 5-HT(1A) receptor binding in chronic fatigue syndrome measured using positron emission tomography and [(11)C]WAY-100635
		RESULTS: There was a widespread reduction in 5-HT(1A) receptor binding potential in CFS relative to control subjects.
		BACKGROUND: Research from neuroendocrine challenge and other indirect studies has suggested increased central 5-HT function in chronic fatigue syndrome (CFS) and increased 5-HT(1A) receptor sensitivity.
		This may be a primary feature of CFS, related to the underlying pathophysiology, or a finding secondary to other processes, such as previous depression, other biological changes or the behavioral consequences of CFS.
	www.immunesupport.com /library/showarticle.cfm/ID/6261 (308 words)

	Log In Problems
		Medscape requires Netscape or Microsoft browsers in versions 5 or higher.
	www.medscape.com /medline/abstract/11937086 (112 words)

	Serotonin Receptor Subtypes and Ligands
		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.
		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.
		For example, human 5-HT receptors exhibit only 50—55% TM homology with 5-HT receptors, and yet one of the early problems in identifying 5-HT -selective agents was their high affinity for 5-HT receptors.
	www.acnp.org /G4/GN401000039/Ch039.html (112 words)

	Class A Rhodopsin like
		5H1A_MOUSE : HTR1A -- 5-hydroxytryptamine 1A receptor (5-HT-1A) (Serotonin receptor 1A) (5- HT1A).
		5H1A_RAT : HTR1A -- 5-hydroxytryptamine 1A receptor (5-HT-1A) (Serotonin receptor 1A) (5- HT1A).
		CKR5_HUMAN : CCR5 -- C-C chemokine receptor type 5 (C-C CKR-5) (CC-CKR-5) (CCR-5) (CCR5) (HIV-1 fusion coreceptor) (CHEMR13) (CD195 antigen).
	www.gpcr.org /seq/001/001.SEQ.html (112 words)

	The Selective Serotonin2A Receptor Antagonist, MDL100,907, Elicits a Specific Interoceptive Cue in Rats
		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.
		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.
	www.nature.com /npp/journal/v26/n4/full/1395832a.html (2174 words)

	gpcr.pep
		5-HYDROXYTRYPTAMINE 7 RECEPTOR (5-HT-7) (5-HT-X) (SEROTONIN RECEPTOR) (5HT7) (GPRFO).
		5-HYDROXYTRYPTAMINE 2A RECEPTOR (5-HT-2A) (SEROTONIN RECEPTOR) (5-HT-2) (5-HT2A).
		5-HYDROXYTRYPTAMINE 7 RECEPTOR (5-HT-7) (5-HT-X) (SEROTONIN RECEPTOR) (5HT7).
	www.research.ibm.com /splash/gpcr/gpcr.pep (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.
	www.wikimirror.com /Serotonin_receptor (2174 words)

	Texas Medicaid Vendor Drug Program, Serotonin 5-HT1D Receptor Agonists
		Serotonin 5-HT receptor agonists are approved for acute treatment of migraine attacks and may be utilized for extended durations to manage migraine headaches provided that the maximum dosage recommendation is not exceeded in a 24-hour period.
		The use of two or more serotonin 5-HT receptor agonists concurrently is not justified as their vasospastic effects may be additive.
		Adjunctive administration of serotonin 5-HT receptor agonists and MAOIs or administration of serotonin 5-HT receptor agonists within two weeks of discontinuing MAOIs is contraindicated and will be reviewed.
	www.hhsc.state.tx.us /HCF/vdp/Criteria/seroton.html (2174 words)

	Alpha2-adrenergic receptor blockade
		These data demonstrate that alpha2-adrenergic receptors tonically inhibit NAD and DA and phasically inhibit 5-HT release in the FCX and that blockade of alpha2-adrenergic receptors strikingly potentiates the increase in FCX levels of 5-HT, NAD, and DA elicited by reuptake inhibitors.
		The selective alpha2-adrenergic receptor agonist S 18616 (0.16 mg/kg, s.c.) suppressed extracellular levels of NAD, DA, and 5-HT (by 100, 51, and 63%, respectively) in single dialysates of FCX of freely moving rats.
		In contrast, the selective alpha2-adrenergic receptor antagonists atipamezole (0.16 mg/kg, s.c.) and 1-(2-pyrimidinyl)piperazine (1-PP; 2.5 mg/kg, s.c.) increased levels of NAD (by 180 and 185%, respectively) and DA (by 130 and 90%, respectively), without affecting 5-HT levels.
	www.biopsychiatry.com /alp2ant.htm (334 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.
	pharmrev.aspetjournals.org /cgi/content/full/55/3/509 (5247 words)

	Open probability of homomeric murine 5-HT3A serotonin receptors depends on subunit occupancy -- Mott et al. 535 (2): 427 -- The Journal of Physiology Online
		Furthermore, the role of 5-HT receptors in modulating activity in the myenteric plexus suggests that 5-HT receptor antagonists might be useful for treatment of irritable bowel syndrome (Greenshaw and Silverstone, 1997; Farthing, 1999).
		These results, however, do not rule out a block of 5-HT receptors by serotonin acting at a site within the vestibule that is uninfluenced by the direction of net current flow or the transmembrane electric field.
		Serotonin is a biogenic amine that activates a large and heterogeneous family of receptors that are widely distributed throughout the central and peripheral nervous systems (Boess and Martin, 1994; Jackson and Yakel, 1995).
	jp.physoc.org /cgi/content/full/535/2/427 (5247 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.
		Receptors in the GABA Striatopallidal Neuron: Biochemical-Cellular Level.
	pharmrev.aspetjournals.org /cgi/content/full/55/3/509 (5247 words)

	Serotonin 5-HT7 receptors mediate relaxation of porcine pial veins -- Ishine et al. 278 (3): 907 -- AJP - Heart and Circulatory Physiology
		The possibility that 5-HT receptors mediate the 5-HT inhibition of pial venous RC was therefore proposed.
		Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus.
		Serotonin 5-HT7 receptors mediate relaxation of porcine pial veins -- Ishine et al.
	ajpheart.physiology.org /cgi/content/full/278/3/H907 (5247 words)

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In the News (Fri 25 Dec 09)