Chapter 14: Histamine (PDF)
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Neurotransmitter Resource Guide
NEUROTRANSMITTER RESOURCE GUIDE Science + Insight doctorsdata.com Doctor’s Data, Inc. Neurotransmitter RESOURCE GUIDE Table of Contents Sample Report Sample Report ........................................................................................................................................................................... 1 Analyte Considerations Phenylethylamine (B-phenylethylamine or PEA) ................................................................................................. 1 Tyrosine .......................................................................................................................................................................................... 3 Tyramine ........................................................................................................................................................................................4 Dopamine .....................................................................................................................................................................................6 3, 4-Dihydroxyphenylacetic Acid (DOPAC) ............................................................................................................... 7 3-Methoxytyramine (3-MT) ............................................................................................................................................... 9 Norepinephrine ........................................................................................................................................................................ -
TABLE 1 Studies of Antagonist Activity in Constitutively Active
TABLE 1 Studies of antagonist activity in constitutively active receptors systems shown to demonstrate inverse agonism for at least one ligand Targets are natural Gs and constitutively active mutants (CAM) of GPCRs. Of 380 antagonists, 85% of the ligands demonstrate inverse agonism. Receptor Neutral Antagonist Inverse Agonist Reference Human β2-adrenergic Dichloroisoproterenol, pindolol, labetolol, timolol, Chidiac et al., 1996; Azzi et alprenolol, propranolol, ICI 118,551, cyanopindolol al., 2001 Turkey erythrocyte β-adrenergic Propranolol, pindolol Gotze et al., 1994 Human β2-adrenergic (CAM) Propranolol Betaxolol, ICI 118,551, sotalol, timolol Samama et al., 1994; Stevens and Milligan, 1998 Human/guinea pig β1-adrenergic Atenolol, propranolol Mewes et al., 1993 Human β1-adrenergic Carvedilol CGP20712A, metoprolol, bisoprolol Engelhardt et al., 2001 Rat α2D-adrenergic Rauwolscine, yohimbine, WB 4101, idazoxan, Tian et al., 1994 phentolamine, Human α2A-adrenergic Napthazoline, Rauwolscine, idazoxan, altipamezole, levomedetomidine, Jansson et al., 1998; Pauwels MPV-2088 (–)RX811059, RX 831003 et al., 2002 Human α2C-adrenergic RX821002, yohimbine Cayla et al., 1999 Human α2D-adrenergic Prazosin McCune et al., 2000 Rat α2-adrenoceptor MK912 RX821002 Murrin et al., 2000 Porcine α2A adrenoceptor (CAM- Idazoxan Rauwolscine, yohimbine, RX821002, MK912, Wade et al., 2001 T373K) phentolamine Human α2A-adrenoceptor (CAM) Dexefaroxan, (+)RX811059, (–)RX811059, RS15385, yohimbine, Pauwels et al., 2000 atipamezole fluparoxan, WB 4101 Hamster α1B-adrenergic -
The Histamine H4 Receptor: a Novel Target for Safe Anti-Inflammatory
GASTRO ISSN 2377-8369 Open Journal http://dx.doi.org/10.17140/GOJ-1-103 Review The Histamine H4 Receptor: A Novel Target *Corresponding author Maristella Adami, PhD for Safe Anti-inflammatory Drugs? Department of Neuroscience University of Parma Via Volturno 39 43125 Parma Italy * 1 Tel. +39 0521 903943 Maristella Adami and Gabriella Coruzzi Fax: +39 0521 903852 E-mail: [email protected] Department of Neuroscience, University of Parma, Via Volturno 39, 43125 Parma, Italy Volume 1 : Issue 1 1retired Article Ref. #: 1000GOJ1103 Article History Received: May 30th, 2014 ABSTRACT Accepted: June 12th, 2014 th Published: July 16 , 2014 The functional role of histamine H4 receptors (H4Rs) in the Gastrointestinal (GI) tract is reviewed, with particular reference to their involvement in the regulation of gastric mucosal defense and inflammation. 4H Rs have been detected in different cell types of the gut, including Citation immune cells, paracrine cells, endocrine cells and neurons, from different animal species and Adami M, Coruzzi G. The Histamine H4 Receptor: a novel target for safe anti- humans; moreover, H4R expression was reported to be altered in some pathological conditions, inflammatory drugs?. Gastro Open J. such as colitis and cancer. Functional studies have demonstrated protective effects of H4R an- 2014; 1(1): 7-12. doi: 10.17140/GOJ- tagonists in several experimental models of gastric mucosal damage and intestinal inflamma- 1-103 tion, suggesting a potential therapeutic role of drugs targeting this new receptor subtype in GI disorders, such as allergic enteropathy, Inflammatory Bowel Disease (IBD), Irritable Bowel Syndrome (IBS) and cancer. KEYWORDS: Histamine H4 receptor; Stomach; Intestine. -
From Inverse Agonism to 'Paradoxical Pharmacology' Richard A
International Congress Series 1249 (2003) 27-37 From inverse agonism to 'Paradoxical Pharmacology' Richard A. Bond*, Kenda L.J. Evans, Zsirzsanna Callaerts-Vegh Department of Pharmacological and Pharmaceutical Sciences, University of Houston, 521 Science and Research Bldg 2, 4800 Caltioun, Houston, TX 77204-5037, USA Received 16 April 2003; accepted 16 April 2003 Abstract The constitutive or spontaneous activity of G protein-coupled receptors (GPCRs) and compounds acting as inverse agonists is a recent but well-established phenomenon. Dozens of receptor subtypes for numerous neurotransmitters and hormones have been shown to posses this property. However, do to the apparently low percentage of receptors in the spontaneously active state, the physiologic relevance of these findings remains questionable. The possibility that the reciprocal nature of the effects of agonists and inverse agonists may extend to cellular signaling is discussed, and that this may account for the beneficial effects of certain p-adrenoceptor inverse agonists in the treatment of heart failure. © 2003 Elsevier Science B.V. All rights reserved. Keywords. Inverse agonism; GPCR; Paradoxical pharmacology 1. Brief history of inverse agonism at G protein-coupled receptors For approximately three-quarters of a century, ligands that interacted with G protein- coupled receptors (GPCRs) were classified either as agonists or antagonists. Receptors were thought to exist in a single quiescent state that could only induce cellular signaling upon agonist binding to the receptor to produce an activated state of the receptor. In this model, antagonists had no cellular signaling ability on their own, but did bind to the receptor and prevented agonists from being able to bind and activate the receptor. -
(12) Patent Application Publication (10) Pub. No.: US 2010/0221245 A1 Kunin (43) Pub
US 2010O221245A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0221245 A1 Kunin (43) Pub. Date: Sep. 2, 2010 (54) TOPICAL SKIN CARE COMPOSITION Publication Classification (51) Int. Cl. (76) Inventor: Audrey Kunin, Mission Hills, KS A 6LX 39/395 (2006.01) (US) A6II 3L/235 (2006.01) A638/16 (2006.01) Correspondence Address: (52) U.S. Cl. ......................... 424/133.1: 514/533: 514/12 HUSCH BLACKWELL SANDERS LLP (57) ABSTRACT 4801 Main Street, Suite 1000 - KANSAS CITY, MO 64112 (US) The present invention is directed to a topical skin care com position. The composition has the unique ability to treat acne without drying out the user's skin. In particular, the compo (21) Appl. No.: 12/395,251 sition includes a base, an antibacterial agent, at least one anti-inflammatory agent, and at least one antioxidant. The (22) Filed: Feb. 27, 2009 antibacterial agent may be benzoyl peroxide. US 2010/0221 245 A1 Sep. 2, 2010 TOPCAL SKIN CARE COMPOSITION stay of acne treatment since the 1950s. Skin irritation is the most common side effect of benzoyl peroxide and other anti BACKGROUND OF THE INVENTION biotic usage. Some treatments can be severe and can leave the 0001. The present invention generally relates to composi user's skin excessively dry. Excessive use of some acne prod tions and methods for producing topical skin care. Acne Vul ucts may cause redness, dryness of the face, and can actually garis, or acne, is a common skin disease that is prevalent in lead to more acne. Therefore, it would be beneficial to provide teenagers and young adults. -
Pitolisant (Wakix) Reference Number: CP.PMN.221 Effective Date: 03.01.20 Last Review Date: 02.21 Line of Business: Commercial, HIM, Medicaid Revision Log
Clinical Policy: Pitolisant (Wakix) Reference Number: CP.PMN.221 Effective Date: 03.01.20 Last Review Date: 02.21 Line of Business: Commercial, HIM, Medicaid Revision Log See Important Reminder at the end of this policy for important regulatory and legal information. Description ® Wakix (pitolisant) is a selective histamine 3 (H3) receptor antagonist/inverse agonist. FDA Approved Indication(s) Wakix is indicated for the treatment of excessive daytime sleepiness (EDS) or cataplexy in adult patients with narcolepsy. Policy/Criteria Provider must submit documentation (such as office chart notes, lab results or other clinical information) supporting that member has met all approval criteria. It is the policy of health plans affiliated with Centene Corporation® that Wakix is medically necessary when the following criteria are met: I. Initial Approval Criteria A. Narcolepsy with Cataplexy (must meet all): 1. Diagnosis of narcolepsy with cataplexy; 2. Prescribed by or in consultation with a neurologist or sleep medicine specialist; 3. Age ≥ 18 years; 4. Failure of 2 of the following antidepressants, each used for ≥ 1 month, unless member’s age is ≥ 65, clinically significant adverse effects are experienced, or all are contraindicated: venlafaxine, fluoxetine, atomoxetine, clomipramine, protriptyline; 5. Dose does not exceed 35.6 mg (two 17.8 mg tablets) per day. Approval duration: Medicaid/HIM – 12 months Commercial – Length of Benefit B. Narcolepsy with Excessive Daytime Sleepiness (must meet all): 1. Diagnosis of narcolepsy with EDS; 2. Prescribed by or in consultation with a neurologist or sleep medicine specialist; 3. Age ≥ 18 years; 4. Failure of a 1-month trial of one of the following central nervous system (CNS) stimulants at up to maximally indicated doses, unless clinically significant adverse effects are experienced or all are contraindicated: amphetamine immediate-release (IR), amphetamine, dextroamphetamine IR, dextroamphetamine, methylphenidate IR; *Prior authorization may be required for CNS stimulants Page 1 of 6 CLINICAL POLICY Pitolisant 5. -
Mol.116.105981.Full.Pdf
Molecular Pharmacology Fast Forward. Published on September 13, 2016 as DOI: 10.1124/mol.116.105981 This article has not been copyedited and formatted. The final version may differ from this version. MOL #105981 CURRENT KNOWLEDGE AND PERSPECTIVES FOR HISTAMINE H1 AND H2 RECEPTOR PHARMACOLOGY. FUNCTIONAL SELECTIVITY, RECEPTOR CROSSTALK AND REPOSITIONING OF CLASSIC HISTAMINERGIC LIGANDS. Downloaded from Federico Monczor and Natalia Fernandez. Instituto de Investigaciones Farmacológicas, ININFA. Universidad de Buenos Aires—Consejo molpharm.aspetjournals.org Nacional de Investigaciones Científicas y Técnicas, CONICET. Buenos Aires, Argentina. at ASPET Journals on September 28, 2021 1 Molecular Pharmacology Fast Forward. Published on September 13, 2016 as DOI: 10.1124/mol.116.105981 This article has not been copyedited and formatted. The final version may differ from this version. MOL #105981 Running title: Current and perspectives for histamine receptors pharmacology. Corresponding author: Federico Monczor. Laboratorio de Farmacología de Receptores. Instituto de Investigaciones Farmacológicas, ININFA. Universidad de Buenos Aires—Consejo Nacional de Investigaciones Científicas y Técnicas, CONICET. Junin 956 (1113) Buenos Aires, Argentina. Tel:+54-11-5287-4856. e-mail: [email protected]. Total text pages: 41 Downloaded from Tables: 2 Figures: 1 References: 125 molpharm.aspetjournals.org Abstract words: 222 Abbreviations: AML, acute myeloid leukemia; ATP, adenosine triphosphate; GTP, guanosine triphosphate; AC, adenylyl cyclase; IP, inositol -
Histidine Decarboxylase Knockout Mice Production and Signal
Nitric Oxide Mediates T Cell Cytokine Production and Signal Transduction in Histidine Decarboxylase Knockout Mice This information is current as Agnes Koncz, Maria Pasztoi, Mercedesz Mazan, Ferenc of October 1, 2021. Fazakas, Edit Buzas, Andras Falus and Gyorgy Nagy J Immunol 2007; 179:6613-6619; ; doi: 10.4049/jimmunol.179.10.6613 http://www.jimmunol.org/content/179/10/6613 Downloaded from References This article cites 41 articles, 8 of which you can access for free at: http://www.jimmunol.org/content/179/10/6613.full#ref-list-1 http://www.jimmunol.org/ Why The JI? Submit online. • Rapid Reviews! 30 days* from submission to initial decision • No Triage! Every submission reviewed by practicing scientists • Fast Publication! 4 weeks from acceptance to publication *average by guest on October 1, 2021 Subscription Information about subscribing to The Journal of Immunology is online at: http://jimmunol.org/subscription Permissions Submit copyright permission requests at: http://www.aai.org/About/Publications/JI/copyright.html Email Alerts Receive free email-alerts when new articles cite this article. Sign up at: http://jimmunol.org/alerts The Journal of Immunology is published twice each month by The American Association of Immunologists, Inc., 1451 Rockville Pike, Suite 650, Rockville, MD 20852 Copyright © 2007 by The American Association of Immunologists All rights reserved. Print ISSN: 0022-1767 Online ISSN: 1550-6606. The Journal of Immunology Nitric Oxide Mediates T Cell Cytokine Production and Signal Transduction in Histidine Decarboxylase Knockout Mice1 Agnes Koncz,*† Maria Pasztoi,* Mercedesz Mazan,* Ferenc Fazakas,‡ Edit Buzas,* Andras Falus,*§ and Gyorgy Nagy2,3*¶ Histamine is a key regulator of the immune system. -
Stress Impairs 5-HT2A Receptor-Mediated Serotonergic Facilitation of GABA Release in Juvenile Rat Basolateral Amygdala
Neuropsychopharmacology (2009) 34, 410–423 & 2009 Nature Publishing Group All rights reserved 0893-133X/09 $32.00 www.neuropsychopharmacology.org Stress Impairs 5-HT2A Receptor-Mediated Serotonergic Facilitation of GABA Release in Juvenile Rat Basolateral Amygdala 1,2 1 3 4 1 ,1,2 Xiaolong Jiang , Guoqiang Xing , Chunhui Yang , Ajay Verma , Lei Zhang and He Li* 1 Department of Psychiatry, Center for the Study of Traumatic Stress, Uniformed Services University of the Health Sciences, Bethesda, MD, USA; 2 3 Neuroscience Program, Uniformed Services University of the Health Sciences, Bethesda, MD, USA; Section on Neuropathology, Clinical Brain 4 Disorders Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA; Department of Neurology, Uniformed Services University of the Health Sciences, Bethesda, MD, USA The occurrence of stress and anxiety disorders has been closely associated with alterations of the amygdala GABAergic system. In these disorders, dysregulation of the serotonergic system, a very important modulator of the amygdala GABAergic system, is also well recognized. The present study, utilizing a learned helplessness stress rat model, was designed to determine whether stress is capable of altering serotonergic modulation of the amygdala GABAergic system. In control rats, administration of 5-HT or a-methyl-5-HT, a 5-HT2 receptor agonist, to basolateral amygdala (BLA) slices dramatically enhanced frequency and amplitude of spontaneous inhibitory postsynaptic currents (sIPSCs). This effect was blocked by selective 5-HT2A receptor antagonists while a selective 5-HT2B receptor agonist and a selective 5-HT2C receptor agonist were without effect on sIPSCs. Double immunofluorescence labeling demonstrated that the 5-HT2A receptor is primarily localized to parvalbumin-containing BLA interneurons. -
THE USE of MIRTAZAPINE AS a HYPNOTIC O Uso Da Mirtazapina Como Hipnótico Francisca Magalhães Scoralicka, Einstein Francisco Camargosa, Otávio Toledo Nóbregaa
ARTIGO ESPECIAL THE USE OF MIRTAZAPINE AS A HYPNOTIC O uso da mirtazapina como hipnótico Francisca Magalhães Scoralicka, Einstein Francisco Camargosa, Otávio Toledo Nóbregaa Prescription of approved hypnotics for insomnia decreased by more than 50%, whereas of antidepressive agents outstripped that of hypnotics. However, there is little data on their efficacy to treat insomnia, and many of these medications may be associated with known side effects. Antidepressants are associated with various effects on sleep patterns, depending on the intrinsic pharmacological properties of the active agent, such as degree of inhibition of serotonin or noradrenaline reuptake, effects on 5-HT1A and 5-HT2 receptors, action(s) at alpha-adrenoceptors, and/or histamine H1 sites. Mirtazapine is a noradrenergic and specific serotonergic antidepressive agent that acts by antagonizing alpha-2 adrenergic receptors and blocking 5-HT2 and 5-HT3 receptors. It has high affinity for histamine H1 receptors, low affinity for dopaminergic receptors, and lacks anticholinergic activity. In spite of these potential beneficial effects of mirtazapine on sleep, no placebo-controlled randomized clinical trials of ABSTRACT mirtazapine in primary insomniacs have been conducted. Mirtazapine was associated with improvements in sleep on normal sleepers and depressed patients. The most common side effects of mirtazapine, i.e. dry mouth, drowsiness, increased appetite and increased body weight, were mostly mild and transient. Considering its use in elderly people, this paper provides a revision about studies regarding mirtazapine for sleep disorders. KEYWORDS: sleep; antidepressive agents; sleep disorders; treatment� A prescrição de hipnóticos aprovados para insônia diminuiu em mais de 50%, enquanto de antidepressivos ultrapassou a dos primeiros. -
Histamine Receptors
Tocris Scientific Review Series Tocri-lu-2945 Histamine Receptors Iwan de Esch and Rob Leurs Introduction Leiden/Amsterdam Center for Drug Research (LACDR), Division Histamine is one of the aminergic neurotransmitters and plays of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit an important role in the regulation of several (patho)physiological Amsterdam, De Boelelaan 1083, 1081 HV, Amsterdam, The processes. In the mammalian brain histamine is synthesised in Netherlands restricted populations of neurons that are located in the tuberomammillary nucleus of the posterior hypothalamus.1 Dr. Iwan de Esch is an assistant professor and Prof. Rob Leurs is These neurons project diffusely to most cerebral areas and have full professor and head of the Division of Medicinal Chemistry of been implicated in several brain functions (e.g. sleep/ the Leiden/Amsterdam Center of Drug Research (LACDR), VU wakefulness, hormonal secretion, cardiovascular control, University Amsterdam, The Netherlands. Since the seventies, thermoregulation, food intake, and memory formation).2 In histamine receptor research has been one of the traditional peripheral tissues, histamine is stored in mast cells, eosinophils, themes of the division. Molecular understanding of ligand- basophils, enterochromaffin cells and probably also in some receptor interaction is obtained by combining pharmacology specific neurons. Mast cell histamine plays an important role in (signal transduction, proliferation), molecular biology, receptor the pathogenesis of various allergic conditions. After mast cell modelling and the synthesis and identification of new ligands. degranulation, release of histamine leads to various well-known symptoms of allergic conditions in the skin and the airway system. In 1937, Bovet and Staub discovered compounds that antagonise the effect of histamine on these allergic reactions.3 Ever since, there has been intense research devoted towards finding novel ligands with (anti-) histaminergic activity. -
The Roles Played by Highly Truncated Splice Variants of G Protein-Coupled Receptors Helen Wise
Wise Journal of Molecular Signaling 2012, 7:13 http://www.jmolecularsignaling.com/content/7/1/13 REVIEW Open Access The roles played by highly truncated splice variants of G protein-coupled receptors Helen Wise Abstract Alternative splicing of G protein-coupled receptor (GPCR) genes greatly increases the total number of receptor isoforms which may be expressed in a cell-dependent and time-dependent manner. This increased diversity of cell signaling options caused by the generation of splice variants is further enhanced by receptor dimerization. When alternative splicing generates highly truncated GPCRs with less than seven transmembrane (TM) domains, the predominant effect in vitro is that of a dominant-negative mutation associated with the retention of the wild-type receptor in the endoplasmic reticulum (ER). For constitutively active (agonist-independent) GPCRs, their attenuated expression on the cell surface, and consequent decreased basal activity due to the dominant-negative effect of truncated splice variants, has pathological consequences. Truncated splice variants may conversely offer protection from disease when expression of co-receptors for binding of infectious agents to cells is attenuated due to ER retention of the wild-type co-receptor. In this review, we will see that GPCRs retained in the ER can still be functionally active but also that highly truncated GPCRs may also be functionally active. Although rare, some truncated splice variants still bind ligand and activate cell signaling responses. More importantly, by forming heterodimers with full-length GPCRs, some truncated splice variants also provide opportunities to generate receptor complexes with unique pharmacological properties. So, instead of assuming that highly truncated GPCRs are associated with faulty transcription processes, it is time to reassess their potential benefit to the host organism.