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Topic: H3 receptor

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Histamine

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	BioMed Central \| Full text \| Plasticity of histamine H3receptor expression and binding in the vestibular nuclei after ...
		receptor binding densities occurring in the ipsilateral medial vestibular nuclei 48 h post-lesion.
		receptor was recently cloned from human [17], monkey [18], rat [19], mouse [20], and guinea pig [21].
		Moreover, the receptor was found to have several isoforms [21-26] with differential coupling to second messenger systems and a variation in their distribution in a region-specific manner.
	www.biomedcentral.com /1471-2202/5/32 (5125 words)

	BioMed Central \| Full text \| Increased brain histamine H3receptor expression during hibernation in golden-mantled ...
		receptor mRNA increases in the cortex, caudate nucleus and putamen during hibernation, an increase that is accompanied by elevated receptor binding in the cerebral cortex, globus pallidus and substantia nigra.
		receptor expression in cortical neurons and in striatopallidal and striatonigral GABAergic neurons.
		receptor gene is one of the few with a transcript that increases during hibernation, indicating an important role for the receptor in regulating this state.
	www.biomedcentral.com /1471-2202/4/24 (5678 words)

	INABIS '98 - The Role of Interactions Between Histaminergic and Cholinergic Systems in Learning and Memory
		Consistently, H3 receptors decreased in the cerebral cortex after local infusion of neurotoxins (Cumming et al., 1991; Pollard et al., 1993), and H3 receptor stimulation failed to alter the potassium-evoked release of tritiated ACh from synaptosomes of the entorhinal cortex (Arrang et al., 1995).
		We investigated the capacity of H3 receptor antagonists to influence scopolamine-induced amnesia in rats, measured by object recognition (Ennaceur et al., 1988) and a passive avoidance response (Blandina et al., 1996a).
		H3 receptor antagonists, by increasing the release of endogenous histamine, may facilitate cholinergic activity in brain areas crucial for cognitive functions.
	www.mcmaster.ca /inabis98/huston/blandina0227/two.html (3107 words)

	Weill Cornell Scientists Reveal Action of a Histamine Receptor That May Lead to New Therapies for Heart Attacks, ... (Site not responding. Last check: 2007-11-05)
		He says that while the receptor limits the release of noradrenaline in both normal states and ischemia, the receptor in normal states is “not terribly important.” It is in ischemia that the receptor plays a critical role, which he and Dr. Silver, an Associate Professor of Physiology and Biophysics, have examined in two recent articles.
		The authors observed the results of exposing the lines of neuroblastoma cells to an H3-receptor agonist (a chemical that activates the receptor) and to an H3-receptor antagonist (a chemical that blocks the receptor).
		The presence of the receptor proved to be necessary for the limiting of both noradrenaline release from the cells and calcium intake to the cells.
	www.med.cornell.edu /news/press/2001/dec_20_histamine.html (882 words)

	Histamine h3 receptor antagonists, preparation and therapeutic uses invention
		The histamine H3 receptor is relatively neuron specific and inhibits the release of a number of monamines, including histamine.
		Accordingly, the histamine H3 receptor is an important target for new therapeutics in Alzheimer disease, mood and attention adjustments, cognitive deficiencies, obesity, dizziness, schizophrenia, epilepsy, sleeping disorders, narcolepsy and motion sickness.
		Furthermore, the identification of this new receptor has fundamentally changed histamine biology and must be considered in the development of histamine H3 receptor antagonists.
	www.freshpatents.com /Histamine-h3-receptor-antagonists-preparation-and-therapeutic-uses-dt20060727ptan20060167046.php (1209 words)

	Histamine
		receptor was initially defined in functional assays (e.g., smooth muscle contraction) and by the design of potent antagonists, the so-called "antihistamines" (e.g., mepyramine), most of which have prominent sedative properties.
		Agonist binding was regulated by guanyl nucleotides, implying that the receptor belonged to the superfamily of receptors coupled to G proteins.
		receptor were known to occur in distinct cell lines or brain slices but could have been due to stimulation of isoreceptors.
	www.acnp.org /g4/GN401000037/CH037.html (4444 words)

	[No title]
		Although their activating ligands vary widely in structure and character, the amino acid sequences of the receptors are very similar and are believed to adopt a common structural framework comprising 7 transmembrane (TM) helices [2, 3, 4].
		In the periphery, low levels of H3 have been detected in the human small intestine, testis and prostate but not in a number of other tissues tested, including the heart, lung and spleen [6].
		Binding of histamine to H3 receptors results in inhibition of forskolin-stimulated cAMP accumulation, suggesting coupling to a G-protein of the Gi class [6].
	www.ebi.ac.uk /interpro/DisplayIproEntry?ac=IPR003980&format=curator (415 words)

	Abbott's H3 histamine receptor antagonist, ABT-239, a candidate treatment of cognitive disorders, ADHD, Alzheimer's and ...
		Histamine H3 receptors, which are predominantly expressed in the CNS, act as autoreceptors in presynaptic neurons, and control histamine turnover.
		Histamine H3 antagonists were first investigated as possible modulators of food intake however it is now clear that histamine H3 receptors are involved in arousal disorders (eg attention deficit hyperactivity disorder - ADHD) and conditions associated with reduced cognition (eg Alzheimer's disease).
		The identification of H3 receptor antagonists has received considerable attention in the field of attention and cognitive disorders since first generation antagonists were shown to promote attention and wakefulness and improve short-term and social memory in rodents.
	www.bioportfolio.com /LeadDiscovery/PubMed-120407.html (1803 words)

	Medical Update - Weill Cornell Medical College Advances
		Meanwhile, the mature (cleaved) neurotrophins interact with trk (pronounced “track”) receptors, leading to cell survival, and, when blood vessels are injured, to responses to that injury.
		To fight cancer, a strategy may be to promote the binding of proneurotrophins and p75 receptors in the appropriate tissues—to promote the dying off of cancerous cells.
		The receptor proved to be necessary for the limiting of both noradrenaline release and calcium intake to the cells.
	www.educationupdate.com /archives/2002/jan_02/htmls/med_weillcornell.html (859 words)

	Ciproxifan, a Histamine H3-Receptor Antagonist/Inverse Agonist, Potentiates Neurochemical and Behavioral Effects of ...
		receptors in the regulation of proenkephalin mRNA abundance in the striatum and accumbens of the rat brain.
		Le Moine C, Bloch B (1995) D1 and D2 dopamine receptor gene expression in the rat striatum: sensitive cRNA probes demonstrate prominent segregation of D1 and D2 mRNAs in distinct neuronal populations of the dorsal and ventral striatum.
		receptors in the striatum and substantia nigra after 6-hydroxydopamine-induced denervation of dopaminergic neurons: an autoradiographic study.
	www.jneurosci.org /cgi/content/full/22/16/7272 (5151 words)

	Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype -- ...
		H3 receptors are predominantly expressed in the CNS (9, 10),
		= 3; 228 ± 53.9 cpm in H3 mice and 143 ± 30.9
		Lecklin, A., and Tuomisto, L. The blockade of H1 receptors attenuates the suppression of feeding and diuresis induced by inhibition of histamine catabolism.
	www.jci.org /cgi/content/full/110/12/1791 (5392 words)

	Histaminergic and Catecholaminergic Interactions in the Central Regulation of Vasopressin and Oxytocin Secretion -- ...
		Effect of the H1 receptor antagonist Mep, the H2 receptor antagonist Cim or the H3 receptor agonist Ime on NE-induced release of AVP (A) or OT (B).
		Effect of the H1 receptor antagonist Mep, the H2 receptor antagonist Cim or the H3 receptor agonist Ime on E-induced release of AVP (A) or OT (B).
		H1 receptors are abundant and the density of H3 receptors is
	endo.endojournals.org /cgi/content/full/140/8/3713 (4965 words)

	HPMR - ReceptorHRH3, histamine receptor H3
		Its various actions are mediated by histamine receptors H1, H2, H3 and H4.
		Histamine receptor H3 belongs to the family 1 of G protein-coupled receptors.
		This receptor can also increase voltage-dependent calcium current in smooth muscles and innervates the blood vessels and the heart in cardiovascular system.
	receptome.stanford.edu /hpmr10/SearchDB/getGenePage.asp?Param=6005782&ProtId=1&ProtType=Receptor (149 words)

	British Journal of Pharmacology - Histamine and its receptors (Site not responding. Last check: 2007-11-05)
		Although evidence for histamine receptor heterogeneity had been provided in the 1940s, much of the research activity on histamine at this time was devoted to the study of its storage, release and metabolism.
		receptors had been identified on a range of white cells but, in fact, it was the chemistry of the molecule and, in particular, the thiourea group in the side chain that was the cause of the toxicity.
		Thus, mutant receptors in which these amino acids in the rat receptor are changed to those of the human receptor (119 Ala to Thr, 122 Val to Ala) exhibited changed ligand-binding potencies of the imidazole-containing antagonists, to levels similar to those of the human receptor (Ligneau et al.
	www.nature.com /uidfinder/10.1038/sj.bjp.0706440 (6245 words)

	Weill Cornell Scientists Reveal Action of a Histamine Receptor That May Lead to New Therapies for Heart Attacks - New ...
		He says that while the receptor limits the release of noradrenaline in both normal states and ischemia, the receptor in normal states is not terribly important.
		It is in ischemia that the receptor plays a critical role, which he and Dr. Silver, an Associate Professor of Physiology and Biophysics, have examined in two recent articles.
		The presence of the receptor proved to be necessary for the limiting of both noradrenaline release from the cells and calcium intake to the cells.
	www.nyp.org /news/hospital/355.html (2563 words)

	Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype -- ...
		Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype -- Takahashi et al.
		Histamine h3 receptor antagonists: preclinical promise for treating obesity and cognitive disorders.
		Photoperiodic Regulation of Histamine H3 Receptor and VGF Messenger Ribonucleic Acid in the Arcuate Nucleus of the Siberian Hamster
	www.jci.org /cgi/content/abstract/110/12/1791 (664 words)

	Novel insights into histamine H2 receptor biology -- Del Valle and Gantz 273 (5): 987 -- AJP - Gastrointestinal and ... (Site not responding. Last check: 2007-11-05)
		Histamine receptors in adipose tissue: involvement of cyclic adenosine monophosphate and the H
		receptor: roles of aspartic acid 107, asparagine 198, and threonine 194.
		receptor antagonists on melanogenesis and cellular proliferation in melanoma cells in culture.
	ajpgi.physiology.org /cgi/content/full/273/5/G987 (5297 words)

	Histamine H3 Receptor Antagonists: Preclinical Promise for Treating Obesity and Cognitive Disorders -- Esbenshade et ...
		amine with an acidic or hydrogen-bonding residue in the receptor.
		receptors inhibit serotonin release in substantia nigra pars reticulata.
		receptor ligands GT-2331 and ciproxifan in a repeated acquisition avoidance response in the spontaneously hypertensive rat pup.
	molinterv.aspetjournals.org /cgi/content/full/6/2/77 (5981 words)

	Histamine Receptors (H1R-H4R) Antibodies
		H1 receptor plays roles in smooth muscle contraction, stimulation of nitric oxide formation, endothelial cell contraction, and increasing vascular permeability, all of which have close relationships with allergic conditions.
		H2 receptor agonist, dimaprit, is a relatively selective H2 receptor agonist with minimal H1R receptor agonism.
		Subsequently, the H3 receptor has been shown to be a presynaptic heteroreceptor in nonhistamine-containing neurons in both the central and peripheral nervous systems.
	www.4adi.com /flr/histamineflr.html (699 words)

	Cloning of Rat Histamine H3 Receptor Reveals Distinct Species Pharmacological Profiles -- Lovenberg et al. 293 (3): 771 ...
		receptor is similar to the human in that it inhibits adenylate cyclase in response to histamine and
		Cardell LO and Edvinsson L (1994) Characterization of the histamine receptors in the guinea-pig lung: Evidence for relaxant histamine H3 receptors in the trachea.
		Cherifi Y, Pigeon C, Le Romancer M, Bado A, Reyl-Desmars F and Lewin MJM (1992) Purification of a histamine H3 receptor negatively coupled to phosphoinositide turnover in the human gastric cell line HGT1.
	jpet.aspetjournals.org /cgi/content/full/293/3/771 (4459 words)

	Centre de recherche en neurobiologie - RECHERCHES ET PUBLICATIONS (Site not responding. Last check: 2007-11-05)
		Marchetti and A.G. Zapata (1999) Partial blockade of T-cell differentiation during ontogeny and marked alterations of the thymic microenvironment in transgenic mice with impaired glucocorticoid receptor function.
		Lévesque (2000) Contrasting patterns and cellular specificity of transcriptional regulation of the nuclear receptor nerve growth factor-inducible B by haloperidol and clozapine in the rat forebrain.
		Barden, F. Holsboer and J.M. Reul (2000) Glucocorticoid receptor impairment alters CNS responses to a psychological stressor: an in vivo microdialysis study in transgenic mice.
	www.crn.crchul.ulaval.ca /neurobiologie/publi.html (5561 words)

	APStracts 5:0301A, 1998. (Site not responding. Last check: 2007-11-05)
		In the heart, histamine (H3) receptors may function as inhibitory presynaptic receptors that decrease adrenergic norepinephrine release in conditions of enhanced sympathetic neural activity.
		In a canine model of E. coli sepsis, we found that H3 receptor blockade caused increases in cardiac output (3.6 to 5.3 L/min; p<.05), systemic blood pressure (mean 76 to 96 mmHg, p<.05), and LV contractility compared with pretreatment values.
		We conclude that activation of H3 receptors may contribute to cardiovascular collapse in sepsis.
	www.uth.tmc.edu /apstracts/1998/jap/July/301A.html (185 words)

	Faculty::Physiology and Biophysics::WMC::Cornell University
		There are three areas of research in the lab all of which focus on receptor mediated regulation of plasma membrane transporters.
		The overall objective of this project is to elucidate the renal mechanisms in the intercalated cells of the cortical collecting duct involved in the adaptation to hypovolemia as may occur in such conditions as diarrhea, diuretic use, and congestive heart failure.
		We speculate that this locally produced angiotensin, acts in a paracrine mode, and stimulates AT receptors on the cardiac sympathetic nerves, leading to excessive release of norepinephrine during ischemia.
	physiology.med.cornell.edu /faculty/silver/silver_research.html (566 words)

	International Union of Pharmacology. XIII. Classification of Histamine Receptors -- Hill et al. 49 (3): 253 -- ...
		The classification of histamine receptors has to date been based on rigorous classical pharmacological analysis, and as yet,
		The third histamine receptor was also defined by a functional assay.
		-subclasses of histamine receptor by Ash and Schild (1966)
	pharmrev.aspetjournals.org /cgi/content/full/49/3/253 (4271 words)

	Characterization of the DNA-Binding and Dimerization Properties of the Nuclear Orphan Receptor Germ Cell Nuclear Factor ... (Site not responding. Last check: 2007-11-05)
		The orphan receptor germ cell nuclear factor (GCNF) is a member of the superfamily of nuclear receptors.
		Activation function 2 (AF-2) of retinoic acid receptor and 9-cis retinoic acid receptor: presence of a conserved autonomous constitutive activating domain and influence of the nature of the response element on AF-2 activity.
		Nuclear receptors in Sicily: all in the famiglia.
	mcb.asm.org /cgi/content/full/19/1/690 (8058 words)

	HRH3 - histamine receptor H3
		HRH3 - histamine receptor H3 These observations indicate that the clone is a distinct histamine receptor from HH3R, and thus is named HH4R.
		However, the binding affinities and agonistic activities of H3 agonists to HH4R were weaker than those to HH3R.
		HRH3 is a homologue of Hrh3 (histamine receptor H 3) from Mus musculus.
	www.ihop-net.org /UniPub/iHOP/gg/96255.html (116 words)

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