5-HT receptors - Factbites

5-HT receptors - Factbites
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Topic: 5-HT receptors

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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)

	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)

	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.
		I joined Dr. Gessner shortly after he and Page had synthesized 5-methoxy-N,N,dimethyltryptamine (5-OMe DMT), speculated that it might be a major psychoactive component of certain hallucinogenic crude plant products used by South American Indians, and had demonstrated that it was a potent serotonin agonist.
	www.phc.vcu.edu /rag/serotonin (13719 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.
		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.
	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.
	www.neuro.uu.se /spikblad/granas.html (377 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
		39% homology with the 5-HT receptor and 46% with the 5-HT receptor.
		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
		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
		the divergence of the 5-HT receptor subtypes in vertebrates, and
	www.jneurosci.org /cgi/content/full/18/15/5586 (5342 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)

	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)

	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.
		� Table 5 lists four of the neurotransmitter systems where agonists produce nausea and emesis and antagonists prevent it.
	www.acnp.org /G4/GN401000045/CH.html (40 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.
		P]orthophosphate, treated with thrombin for 10 min, and lysed in 300 µl of Triton X-100 lysis buffer, and immunoprecipitation was performed as described above with 5 µl of anti-VSVG antibody.
	www.jbc.org /cgi/content/full/270/9/4813 (40 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
		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.
		Inhibition by methiothepin of the AC-coupled 5-HT receptor in Aplysia SNs
	jn.physiology.org /cgi/content/full/89/3/1440 (8978 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)

	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.
		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.
	www.jbc.org /cgi/content/full/270/11/6056 (5869 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
		Ganglia were superfused with saline in the following sequence: saline without 5-HT or antagonist, saline with 5 µM 5-HT (4 min), saline with 5 µM 5-HT and 20 µM methiothepin (4 min), and finally saline with 5 µM 5-HT and 100 µM methiothepin (5 min).
		Membranes from 4 desheathed pleural ganglia, each from a separate animal, were assayed with and without 25 µM 5-HT, in the presence and absence of 10 µM methiothepin.
		5 µM 5-HT was applied initially in the absence of antagonist and
	jn.physiology.org /cgi/content/full/89/3/1440 (5869 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.
	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 (5869 words)

	Heterodimerization of Mineralocorticoid and Glucocorticoid Receptors at a Novel Negative Response Element of the 5-HT1A Receptor Gene -- Ou et al. 276 (17): 14299 -- Journal of Biological Chemistry
		DNase I protection analysis of nGRE-like region of the rat 5-HT1A receptor gene was performed.
		COS-7 cells, which lack endogenous GR and MR, were transfected with 8 µg of expression plasmids Flag-GR for GR alone (2 pmol, lanes 2 and 3), 12 µg of GST-MR for MR alone (2 pmol, lanes 4 and 5), or both (1 pmol each of MR and GR plasmids, lanes 6-8).
		Recombinant proteins were preincubated with 0.4 µg of anti-GR antibody ( A, lane 5), anti-MR antibody ( B, lane 5), or anti-NF1 antibody or normal rabbit serum ( lanes 6 and 7).
	www.jbc.org /cgi/content/full/276/17/14299 (5869 words)

	Phospholipase D Activation by Endogenous 5-Hydroxytryptamine 2C Receptors Is Mediated by Galpha 13 and Pertussis Toxin-Insensitive Gbeta gamma Subunits -- McGrew et al. 62 (6): 1339 -- Molecular Pharmacology
		NIH3T3 cells stably expressing the rat INI isoform of the 5-HT receptor were washed three times, incubated with DMEM supplemented with 0.5% fatty-acid free BSA for 16 h, and then incubated as indicated with peptides solubilized in HBSS for 30 min.
		Cells were treated with 10 nM 5-HT for 5 min where indicated.
		5, our data also suggest that activation of PLD involves both G
	molpharm.aspetjournals.org /cgi/content/full/62/6/1339 (5869 words)

	Activation of Serotonin Receptors Modulates Synaptic Transmission in Rat Cerebral Cortex -- Zhou and Hablitz 82 (6): 2989 -- Journal of Neurophysiology
		In both of these 2 neurons, bath application of 100 µM mCPBG, a specific 5-HT agonist, evoked a brief burst of sIPSCs, lasting for ~5 s.
		5 min failed to induce any visible change in sIPSCs,
		Left : monosynaptic eIPSCs recorded under control condition.
	jn.physiology.org /cgi/content/full/82/6/2989 (5869 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.
	www.cpa-apc.org /Publications/Archives/CJP/2001/Feb/Inreview2.asp (947 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
	jap.physiology.org /cgi/content/full/90/5/2001 (3887 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.
	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.
	www.neurotransmitter.net /seven.html (183 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 (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.
	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
	www.acnp.org /g4/GN401000043/Ch043.html (183 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)

	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.
	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.
	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.
	www.wikimirror.com /Serotonin_receptor (2174 words)

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In the News (Sat 26 May 12)