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Topic: H1 receptor


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In the News (Wed 23 Dec 09)

  
  H1 receptor - Wikipedia, the free encyclopedia
receptor is an important target for clinically important drugs, and is likely one of the most important receptors for modulating mammalian circadian cycles.
receptor are metabotropic G-protein-coupled receptors expressed throughout the body, specifically in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system.
receptors are activated by endogenous histamine, which is released by neurons which have their cell bodies in the tuberomamillary neurons of the hypothalamus.
en.wikipedia.org /wiki/H1_receptor   (316 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)

  
 eMedicine - Toxicity, Antihistamine : Article Excerpt by: David J McCann, MD   (Site not responding. Last check: 2007-11-03)
Pathophysiology: H1, H2, and H3 receptors are the 3 histamine receptors that have been identified.
All H1 histamine antagonists are reversible competitive inhibitors of histamine receptors.
H2-receptor antagonists are considered relatively benign in overdose; as observed with cimetidine, the primary adverse reaction is confusion.
www.emedicine.com /emerg/byname/toxicity-antihistamine.htm   (542 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)

  
 [No title]   (Site not responding. Last check: 2007-11-03)
The H1 receptor is found in both the brain and in the periphery.
The activation of the H1 receptor results in an increase in phosphoinositol hydrolysis, which in turn leads to an increase the intracellular calcium levels (Katzung 1998).
All three subtypes are receptors for histamine, and cause biological reactions as a result of exposure to the compound.
sulcus.berkeley.edu /mcb/165_001/papers/manuscripts/_698.html   (3160 words)

  
 INABIS '98 - Histamine H1 Receptor-Mediated Inhibition of Potassium-evoked Release of 5-Hydroxytryptamine from Mice ...
Brain slices of H1 receptor knockout mice and the wild-type mice were superfused with Ringer bicarbonate solution, and the endogenous release of 5-hydroxytryptamine (5-HT) was measured.
H1 receptor-mediated inhibition of serotonin release in the wild-type mice was also observed in the presence of thioperamide.
Histamine H1 Receptor-Mediated Inhibition of Potassium-evoked Release of 5-Hydroxytryptamine from Mice Brains : A Study of H1 Receptor Knockout Mice.
www.mcmaster.ca /inabis98/huston/yanai0260   (414 words)

  
 Novel Effects of Histamine on Lipoprotein Metabolism: Suppression of Hepatic Low Density Lipoprotein Receptor ...
Livers were obtained for the determination of LDL receptor expression and LDL receptor mRNA levels, and blood was drawn for analyses of plasma total cholesterol and triglycerides and for FPLC analysis of plasma lipoproteins.
Six hours after the injection of H1 agonists, livers and blood were obtained for the determination of LDL receptor expression and plasma lipids as described in Fig.
Chlorpheniramine (CPR; H1 antagonist) or cimetidine (CTD; H2 antagonist) were orally administered at a dose of 0.6 mmol/kg BW 1 h before the injection of C48/80 (2 mg/rat).
endo.endojournals.org /cgi/content/full/138/5/1863   (4703 words)

  
 CLIC4 - chloride intracellular channel 4
Immunoblot analysis established that this reduction of receptor activity was due to a reduction of expression of both ASGR subunit polypeptides H1 and H2.
We considered that the histamine-1 (H1) receptor antagonist hydroxyzine, which also partially inhibits brain mast cells and has anxiolytic properties, may reduce MS symptoms.
Terfenadine potentiation of NMDA receptor response was mimicked by other H1 antagonists, including chlorpheniramine (25 microM), oxatomide (20 microM), and triprolidine (50 microM), was prevented by histamine (1 mM), and did not require RNA synthesis.
www.ihop-net.org /UniPub/iHOP/gg/97280.html   (1460 words)

  
 Novel insights into histamine H2 receptor biology -- Del Valle and Gantz 273 (5): 987 -- AJP - Gastrointestinal and ...
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   (5296 words)

  
 Inflammatory Mediators of Asthma: An Update -- Barnes et al. 50 (4): 515 -- Pharmacological Reviews
The cloning of receptors has made it possible to study the factors regulating their expression.
receptors are coupled to PI turnover, with release of intracellular calcium ions.
increases the discharge of "irritant" receptors in vivo (A
pharmrev.aspetjournals.org /cgi/content/full/50/4/515   (6778 words)

  
 Histamine and Anti-histamine Drugs
receptors and initiates a second messenger response which proceeds by (1.) Increasing adenylyl cyclase activity which (2.) Results in an increase in the second messenger, cyclic AMP which (3.) Causes an increase in intracellular calcium levels.
histamine receptor blockers are drugs of choice to treat allergic rhinitis and urticaria.
receptor antagonists, at higher dosages than for management of peptic or gastric ulcer disease,are used as one component of treatment.
www.pharmacology2000.com /Histamine/histamine.htm   (2576 words)

  
 Erwin Gelfand, MD - Airway Inflammation: New Advances & Approaches in Treatment
Secondly, are histamine effects in asthma mediated through H1 receptors, and I think you all are aware now that there are at least 4 subtypes of histamine receptors, cleverly named 1,2,3 and 4.
In terms of antigen receptor mediated responses, in gene knock out mice an H1 receptors deficient T-cells, their low proliferative responses were a number of signaling lygams, H1 receptor deficient B-cells at low proliferative responses, to B-cell and receptor cross linking and the H1 receptor deficient mice, had very significant decreases in antibody production.
I hope I've been able to convince you that histamine is indeed a mediator of asthma and certainly based on the data illustrated with use of an H1 specific receptor antagonist that we could block many of the histamine mediator effects in asthma that are mediated through these receptors.
www.vioworks.com /clients/acaai/trans/gelfand_11-17.htm   (1629 words)

  
 International Union of Pharmacology. XIII. Classification of Histamine Receptors -- Hill et al. 49 (3): 253 -- ...
Classification of Histamine Receptors -- Hill et al.
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   (4312 words)

  
 Augmentation of Antigen Receptor-mediated Responses by Histamine H1 Receptor Signaling -- Banu and Watanabe 189 (4): ...   (Site not responding. Last check: 2007-11-03)
Histamine is known to be a neurotransmitter (26), an inflammatory mediator, a factor in anaphylaxis, and a regulator of
Expression cloning of cDNA encoding the bovine histamine H1 receptor.
Histamine type 1 (H1) receptor radioligand binding studies on normal T cell subsets, B cells and monocytes.
www.jem.org /cgi/content/full/189/4/673   (5460 words)

  
 Allergy & Asthma Disease Management Center: Ask the Expert: Antihistamine
H1 antihistamines have similar efficacy in the treatment of allergic disorders; however, they differ in terms of their chemical structure, clinical pharmacology, and safety.
The reason for this anti-cholinergic effect was that such early antihistamines were not specific for the H1 histamine receptor, binding to cholinergic and other receptors as well.
In moderate persistent asthma, clinical benefits of H1 antagonists are apparent, but may not be worth the potential risks of the higher-than-usual doses required.
www.aaaai.org /aadmc/ate/antihistamine.html   (9595 words)

  
 Medications   (Site not responding. Last check: 2007-11-03)
Benefit/risk ratio of the antihistamines (H1 receptor antagonists) terfendaine and chlorpheniramine in children.
Histamine and H1 receptor antagonists in allergic disease.
Rafferty P, Jackson L, Smith R, Holgate ST. Terfenadine, a potent histamine H1 receptor antagonist in the treatment of grass pollen sensitive asthma.
www.jcaai.org /param/Rhinitis/Complete/medications.htm   (2833 words)

  
 Welcome to PeerView
The study found that desloratadine was a potent antagonist of muscarinic acetylcholine receptors, especially the M2 subtype, and had significantly higher affinity for muscarinic receptors than its parent compound, loratadine.
receptor is not inevitable in the metabolites of second-generation antihistamines.
receptor is not inevitable in the metabolites of second-generation antihistamines and can influence the side-effect profile.
www.docguide.com /peerview.nsf/release/072001_sec2_fexo_hi.html   (319 words)

  
 eMedicine - Toxicity, Antihistamine : Article by David J McCann, MD   (Site not responding. Last check: 2007-11-03)
H3 receptors are presynaptic regulators of synthesis and release of histamine into the synapse.
Piperidine derivatives (eg, terfenadine, astemizole, loratadine) are peripherally selective H1 antagonists with few GI adverse effects and a low incidence of drowsiness (see Nonsedating antihistamines).
Researchers have suggested a natural anticonvulsant role of histamine because H1 receptors coalesce around epileptogenic foci in brain and inhibit generalization of seizure activity.
www.emedicine.com /emerg/topic38.htm   (5301 words)

  
 A Potent and Selective Histamine H4 Receptor Antagonist with Anti-Inflammatory Properties -- Thurmond et al. 309 (1): ...
A, effects of histamine receptor antagonists on the histamine-mediated calcium increase.
Histamine (fl bars) and the various histamine receptor antagonists (all 10 µM) were added to the cells 10 min prior to the calcium measurements.
B, effects of histamine receptor antagonists on histamine-induced mast cell chemotaxis.
jpet.aspetjournals.org /cgi/content/full/309/1/404   (5466 words)

  
 Binding Characteristics of Cetirizine and Levocetirizine to Human H1 Histamine Receptors: Contribution of Lys191 and ...
receptors with a half-time of 142 min; that of (S)-cetirizine
This mutation decreased the dissociation half-time of levocetirizine
receptor was decreased by a factor of 4 to 6, whereas the affinity
molpharm.aspetjournals.org /cgi/content/full/61/2/391   (4713 words)

  
 Booth Publications
Choksi, N.Y., Nix, William B., Wyrick, S.D., and Booth, R.G. A novel phenylaminotetralin recognizes histamine H1 receptors and stimulates dopamine synthesis in vivo in rat brain.
Choksi, N.Y., Nix, W.B., and Wyrick, S.D., and Booth, R.G. Phenylaminotetralins activate histamine H1 receptors to stimulate dopamine synthesis in vivo in rat brain.
Booth, R.G., Choksi, N.Y., Nix, W.B., and Wyrick, S.D. Histamine H1 receptors mediate stimulation of dopamine synthesis by phenylaminotetralins in vivo.
www.unc.edu /~jcfowler/publications.html   (2043 words)

  
 The H1 histamine receptor regulates allergic lung responses -- Bryce et al. 116 (6): 1624 -- Journal of Clinical ...
The H1 histamine receptor regulates allergic lung responses -- Bryce et al.
Histamine regulates T-cell and antibody responses by differential expression of H1 and H2 receptors.
Kayasuga, R., Sugimoto, Y., Watanabe, T., and Kamei, C. Histamine H1 receptors are involved in mouse nasal allergic responses: a demonstration with H1 receptor-deficient mice.
www.jci.org /cgi/content/full/116/6/1624   (5049 words)

  
 A Novel Phenylaminotetralin Radioligand Reveals a Subpopulation of Histamine H1 Receptors -- Booth et al. 302 (1): 328 ...
receptors also may be expressed as monomers and oligomers.
Maggio R, Barbier P, Colelli A, Salvadori F, Demontis G and Corsini GU (1999) G protein-linked receptors: pharmacological evidence for the formation of heterodimers.
Palacios JM, Garbarg M, Barbin G and Schwartz JC (1978) Pharmacological characterization of histamine receptors mediating the stimulation of cyclic AMP accumulation in slices from guinea pig hippocampus.
jpet.aspetjournals.org /cgi/content/full/302/1/328   (4610 words)

  
 IIA
Vasopressin acts on V1a, V1b and V2 receptors, a sub-family within the large superfamily of G-protein-linked receptors.
Most remaining actions of vasopressin on blood vessel constriction and certain brain functions are mediated via v1a-type receptors that are coupled to a Gq/11 protein.
V1 receptor activation leads to stimulation of phospholipases C, D and A2 and an increase in intracellular calcium.
www.kumc.edu /research/medicine/pharmacology/CAI/iiia.htm   (1899 words)

  
 Antihistamine Summary
An antihistamine is a drug used to counteract the effects of histamine, the chemical released by certain cells in the body during an allergic reaction.
When these are inhaled into the body, antibodies seek out the irritant and combine with it.
A large blood cell known as a basophil, or mast cell, then releases the compound histamine, which attaches itself to receptor cells in mucous membranes.
www.bookrags.com /Antihistamine   (3162 words)

  
 UniProtKB/Swiss-Prot entry P35367 [HRH1_HUMAN] Histamine H1 receptor
: In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Molecular function: histamine receptor activity (traceable author statement from ProtInc).
G-protein coupled receptor; Glycoprotein; Lipoprotein; Membrane; Palmitate; Phosphorylation; Receptor; Transducer; Transmembrane.
www.expasy.org /uniprot/P35367   (447 words)

  
 Role of Protein Kinase Calpha in Signaling from the Histamine H1 Receptor to the Nucleus -- Megson et al. 59 (5): 1012 ...
Role of Protein Kinase Calpha in Signaling from the Histamine H1 Receptor to the Nucleus -- Megson et al.
receptor is a seven-transmembrane spanning receptor that produces its intracellular effects via the activation
Selbie LA and Hill SJ (1998) G-protein-coupled receptor cross-talk: the fine-tuning of multiple receptor-signalling pathways.
molpharm.aspetjournals.org /cgi/content/full/59/5/1012   (5980 words)

  
 Mechanisms of vasoactive intestinal peptide-mediated vasodilation in human skin -- Wilkins et al. 97 (4): 1291 -- ...
Effect of H1- and H2-receptor blockade on the inhibition of immediate cutaneous reactions.
Involvement of H1- and H2-receptors in triple response to histamine in human volunteers.
Involvement of H1 and H2 receptors in histamine-induced skin response in human.
jap.physiology.org /cgi/content/full/97/4/1291   (5479 words)

  
 Alternative Promoter Use and Splice Variation in the Human Histamine H1 Receptor Gene -- Swan et al. 35 (1): 118 -- ...
H1 receptor gene was investigated in cells relevant to the pathogenesis
known to express histamine H1 receptors (placenta and brain).
H1 receptor gene expression, both within and between cell types.
ajrcmb.atsjournals.org /cgi/content/abstract/35/1/118   (318 words)

  
 A Gq/11-coupled Mutant Histamine H1 Receptor F435A Activated Solely by Synthetic Ligands (RASSL) -- Bruysters et al. ...
A Gq/11-coupled Mutant Histamine H1 Receptor F435A Activated Solely by Synthetic Ligands (RASSL) -- Bruysters et al.
receptors F435A, F435V, and F435L, the affinity and potency
To whom correspondence should be addressed: Dept. of Medicinal Chemistry, Vrije Universiteit Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.
www.jbc.org /cgi/content/full/280/41/34741   (2986 words)

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