H2受容体
WordNet
- the 8th letter of the Roman alphabet (同)h
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- hydrogenの化学記号
- 鉛筆の硬度 / 《俗》heroin
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2017/02/03 21:44:44」(JST)
[Wiki en表示]
HRH2 |
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Identifiers |
Aliases |
HRH2, H2R, histamine receptor H2 |
External IDs |
MGI: 108482 HomoloGene: 40613 GeneCards: HRH2 |
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Targeted by Drug |
amthamine, impromidine, cimetidine, ciproxifan, clobenpropit, conessine, mk-0249, pitolisant, (E)-ranitidine, abt-239[1] |
Gene ontology |
Molecular function |
• G-protein coupled receptor activity
• signal transducer activity
• histamine receptor activity
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Cellular component |
• integral component of membrane
• membrane
• plasma membrane
• integral component of plasma membrane
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Biological process |
• visual learning
• G-protein coupled receptor signaling pathway
• epithelial cell morphogenesis
• gastric acid secretion
• G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
• memory
• toxin transport
• regulation of synaptic plasticity
• gastrin-induced gastric acid secretion
• positive regulation of vasoconstriction
• immune response
• digestive tract development
• signal transduction
• gland development
• histamine-induced gastric acid secretion
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Sources:Amigo / QuickGO |
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RNA expression pattern |
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More reference expression data |
Orthologs |
Species |
Human |
Mouse |
Entrez |
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Ensembl |
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UniProt |
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RefSeq (mRNA) |
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RefSeq (protein) |
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NP_001010973.1
NP_032312.2
NP_001010973
NP_032312
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Location (UCSC) |
Chr 5: 175.66 – 175.71 Mb |
Chr 13: 54.19 – 54.24 Mb |
PubMed search |
[2] |
[3] |
Wikidata |
View/Edit Human |
View/Edit Mouse |
H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of protein kinase A.[4] PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a histamine H2 receptor agonist.
Contents
- 1 Function
- 2 Tissue distribution
- 3 Physiological responses
- 4 See also
- 5 References
- 6 Further reading
- 7 External links
Function
Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons.[4] Its various actions are mediated by histamine receptors H1, H2, H3 and H4. The histamine receptor H2 belongs to the rhodopsin-like family of G protein-coupled receptors. It is an integral membrane protein and stimulates gastric acid secretion. It also regulates gastrointestinal motility and intestinal secretion and is thought to be involved in regulating cell growth and differentiation.[5]
Tissue distribution
It is found here:[4]
- Gastric parietal cells (oxyntic cells)
- Vascular smooth muscle
- Neutrophils
- Central nervous system
- Heart
- Uterus
Physiological responses
Activation of the H2 receptor results in the following physiological responses:
- Stimulation of gastric acid secretion (Target of anti-histaminergics (H2 receptors) for peptic ulcer disease and GERD)
- Smooth muscle relaxation (Experimental histamine H2 receptor agonist used for asthma and COPD)
- Inhibit antibody synthesis, T-cell proliferation and cytokine production
- Vasodilation – PKA activity causes phosphorylation of MLCK, decreasing its activity, resulting in MLC of myosin being dephosphorylated by MLCP and thus inhibiting contraction. The smooth muscle relaxation leads to vasodilation.[6]
See also
References
- ^ "Drugs that physically interact with Histamine receptor H2 view/edit references on wikidata".
- ^ "Human PubMed Reference:".
- ^ "Mouse PubMed Reference:".
- ^ a b c Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (Sep 1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacological Reviews. 49 (3): 253–78. PMID 9311023.
- ^ "Entrez Gene: HRH2 histamine receptor H2".
- ^ Walter F., PhD. Boron (2005). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. Page 479
Further reading
- Del Valle J, Gantz I (Nov 1997). "Novel insights into histamine H2 receptor biology". The American Journal of Physiology. 273 (5 Pt 1): G987–96. PMID 9374694.
- Gantz I, Munzert G, Tashiro T, Schäffer M, Wang L, DelValle J, Yamada T (Aug 1991). "Molecular cloning of the human histamine H2 receptor". Biochemical and Biophysical Research Communications. 178 (3): 1386–92. doi:10.1016/0006-291X(91)91047-G. PMID 1714721.
- Vannier E, Dinarello CA (Apr 1994). "Histamine enhances interleukin (IL)-1-induced IL-6 gene expression and protein synthesis via H2 receptors in peripheral blood mononuclear cells". The Journal of Biological Chemistry. 269 (13): 9952–6. PMID 7511596.
- Smit MJ, Timmerman H, Alewijnse AE, Punin M, van den Nieuwenhof I, Blauw J, van Minnen J, Leurs R (Sep 1995). "Visualization of agonist-induced internalization of histamine H2 receptors". Biochemical and Biophysical Research Communications. 214 (3): 1138–45. doi:10.1006/bbrc.1995.2404. PMID 7575521.
- Nishi T, Koike T, Oka T, Maeda M, Futai M (May 1995). "Identification of the promoter region of the human histamine H2-receptor gene". Biochemical and Biophysical Research Communications. 210 (2): 616–23. doi:10.1006/bbrc.1995.1703. PMID 7755641.
- Traiffort E, Vizuete ML, Tardivel-Lacombe J, Souil E, Schwartz JC, Ruat M (Jun 1995). "The guinea pig histamine H2 receptor: gene cloning, tissue expression and chromosomal localization of its human counterpart". Biochemical and Biophysical Research Communications. 211 (2): 570–7. doi:10.1006/bbrc.1995.1851. PMID 7794271.
- Orange PR, Heath PR, Wright SR, Pearson RC (May 1996). "Allelic variations of the human histamine H2 receptor gene". NeuroReport. 7 (7): 1293–6. doi:10.1097/00001756-199605170-00015. PMID 8817552.
- Elenkov IJ, Webster E, Papanicolaou DA, Fleisher TA, Chrousos GP, Wilder RL (Sep 1998). "Histamine potently suppresses human IL-12 and stimulates IL-10 production via H2 receptors". Journal of Immunology. 161 (5): 2586–93. PMID 9725260.
- Murakami H, Sun-Wada GH, Matsumoto M, Nishi T, Wada Y, Futai M (May 1999). "Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression". FEBS Letters. 451 (3): 327–31. doi:10.1016/S0014-5793(99)00618-3. PMID 10371214.
- Wang LD, Wang M, Todisco A, Grand E, del Valle J (Jun 2000). "The human histamine H(2) receptor regulates c-jun and c-fos in a differential manner". American Journal of Physiology. Cell Physiology. 278 (6): C1246–55. PMID 10837353.
- Suh BC, Lee H, Jun DJ, Chun JS, Lee JH, Kim KT (Aug 2001). "Inhibition of H2 histamine receptor-mediated cation channel opening by protein kinase C in human promyelocytic cells". Journal of Immunology. 167 (3): 1663–71. doi:10.4049/jimmunol.167.3.1663. PMID 11466390.
- Brew OB, Sullivan MH (Sep 2001). "Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto-maternal interface of human pregnancy". Inflammation Research. 50 (9): 449–52. doi:10.1007/PL00000269. PMID 11603849.
- Shayo C, Fernandez N, Legnazzi BL, Monczor F, Mladovan A, Baldi A, Davio C (Nov 2001). "Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases". Molecular Pharmacology. 60 (5): 1049–56. PMID 11641433.
- Tanimoto A, Murata Y, Nomaguchi M, Kimura S, Arima N, Xu H, Hamada T, Sasaguri Y (Nov 2001). "Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells". FEBS Letters. 508 (3): 345–9. doi:10.1016/S0014-5793(01)03073-3. PMID 11728449.
- Gutzmer R, Langer K, Lisewski M, Mommert S, Rieckborn D, Kapp A, Werfel T (Mar 2002). "Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells". The Journal of Allergy and Clinical Immunology. 109 (3): 524–31. doi:10.1067/mai.2002.121944. PMID 11898002.
- Esbenshade TA, Kang CH, Krueger KM, Miller TR, Witte DG, Roch JM, Masters JN, Hancock AA (Feb 2003). "Differential activation of dual signaling responses by human H1 and H2 histamine receptors". Journal of Receptor and Signal Transduction Research. 23 (1): 17–31. doi:10.1081/RRS-120018758. PMID 12680587.
External links
- "Histamine Receptors: H2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- H2 receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
Cell surface receptor: G protein-coupled receptors
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Class B: Secretin like
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Adhesion |
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Orphan |
- GPR (56
- 64
- 97
- 98
- 110
- 111
- 112
- 113
- 114
- 115
- 116
- 123
- 124
- 125
- 126
- 128
- 133
- 143
- 144
- 155
- 157)
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Other |
- Brain-specific angiogenesis inhibitor (1
- 2
- 3)
- Cadherin (1
- 2
- 3)
- Calcitonin
- CALCRL
- CD97
- Corticotropin-releasing hormone (1
- 2)
- EMR (1
- 2
- 3)
- Glucagon (GR
- GIPR
- GLP1R
- GLP2R)
- Growth hormone releasing hormone
- PACAPR1
- GPR
- Latrophilin (1
- 2
- 3
- ELTD1)
- Methuselah-like proteins
- Parathyroid hormone (1
- 2)
- Secretin
- Vasoactive intestinal peptide (1
- 2)
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Class C: Metabotropic glutamate / pheromone
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Taste |
- TAS1R (1
- 2
- 3)
- TAS2R (1
- 3
- 4
- 5
- 7
- 8
- 9
- 10
- 13
- 14
- 16
- 19
- 20
- 30
- 31
- 38
- 39
- 40
- 41
- 42
- 43
- 45
- 46
- 50
- 60
- Vomeronasal receptor)
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Other |
- Calcium-sensing receptor
- GABA B (1
- 2)
- Glutamate receptor (Metabotropic glutamate (1
- 2
- 3
- 4
- 5
- 6
- 7
- 8))
- GPRC6A
- GPR (156
- 158
- 179)
- RAIG (1
- 2
- 3
- 4)
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Class F: Frizzled / Smoothened
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Frizzled |
- Frizzled (1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10)
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Smoothened |
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Histaminergics
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Receptor
(ligands) |
H1 |
- Agonists: 2-Pyridylethylamine
- Betahistine
- Histamine
- HTMT
- UR-AK49
- Antagonists: First-generation: 4-Methyldiphenhydramine
- Alimemazine
- Antazoline
- Azatadine
- Bamipine
- Benzatropine (benztropine)
- Bepotastine
- Bromazine
- Brompheniramine
- Buclizine
- Captodiame
- Carbinoxamine
- Chlorcyclizine
- Chloropyramine
- Chlorothen
- Chlorphenamine
- Chlorphenoxamine
- Cinnarizine
- Clemastine
- Clobenzepam
- Clocinizine
- Cloperastine
- Cyclizine
- Cyproheptadine
- Dacemazine
- Decloxizine
- Deptropine
- Dexbrompheniramine
- Dexchlorpheniramine
- Dimenhydrinate
- Dimetindene
- Diphenhydramine
- Diphenylpyraline
- Doxylamine
- Embramine
- Etodroxizine
- Etybenzatropine (ethylbenztropine)
- Etymemazine
- Fenethazine
- Flunarizine
- Histapyrrodine
- Homochlorcyclizine
- Hydroxyethylpromethazine
- Hydroxyzine
- Isopromethazine
- Isothipendyl
- Meclozine
- Medrylamine
- Mepyramine (pyrilamine)
- Mequitazine
- Methafurylene
- Methapyrilene
- Methdilazine
- Moxastine
- Orphenadrine
- Oxatomide
- Oxomemazine
- Phenindamine
- Pheniramine
- Phenyltoloxamine
- Pimethixene
- Piperoxan
- Pipoxizine
- Promethazine
- Propiomazine
- Pyrrobutamine
- Talastine
- Thenalidine
- Thenyldiamine
- Thiazinamium
- Thonzylamine
- Tolpropamine
- Tripelennamine
- Triprolidine
- Second/third-generation: Acrivastine
- Alinastine
- Astemizole
- Azelastine
- Bamirastine
- Barmastine
- Bepiastine
- Bepotastine
- Bilastine
- Cabastinen
- Carebastine
- Cetirizine
- Clemastine
- Clemizole
- Clobenztropine
- Desloratadine
- Dorastine
- Ebastine
- Efletirizine
- Emedastine
- Epinastine
- Fexofenadine
- Flezelastine
- Ketotifen
- Latrepirdine
- Levocabastine
- Levocetirizine
- Linetastine
- Loratadine
- Mapinastine
- Mebhydrolin
- Mizolastine
- Moxastine
- Noberastine
- Octastine
- Olopatadine
- Perastine
- Pibaxizine
- Piclopastine
- Quifenadine (phencarol)
- Rocastine
- Rupatadine
- Setastine
- Sequifenadine (bicarphen)
- Talastine
- Temelastine
- Terfenadine
- Vapitadine
- Zepastine
- Non-generational: Atypical antipsychotics (e.g., aripiprazole, asenapine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine)
- Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline)
- Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine)
- Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)
- Unknown/unsorted: Belarizine
- Elbanizine
- Flotrenizine
- Napactadine
- Tagorizine
- Trelnarizine
- Trenizine
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H2 |
- Agonists: Amthamine
- Betazole
- Dimaprit
- Histamine
- HTMT
- Impromidine
- UR-AK49
- Antagonists: Bisfentidine
- Burimamide
- Cimetidine
- Dalcotidine
- Donetidine
- Ebrotidine
- Etintidine
- Famotidine
- Isolamtidine
- Lafutidine
- Lamtidine
- Lavoltidine (loxtidine)
- Lupitidine
- Metiamide
- Mifentidine
- Niperotidine
- Nizatidine
- Osutidine
- Oxmetidine
- Pibutidine
- Quisultazine (quisultidine)
- Ramixotidine
- Ranitidine
- Roxatidine
- Sufotidine
- Tiotidine
- Tuvatidine
- Venritidine
- Xaltidine
- Zolantidine
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H3 |
- Agonists: α-Methylhistamine
- Cipralisant
- Histamine
- Imetit
- Immepip
- Immethridine
- Methimepip
- Proxyfan
- Antagonists: A-349,821
- A-423,579
- ABT-239
- ABT-652
- AZD5213
- Betahistine
- Burimamide
- Ciproxifan
- Clobenpropit
- Conessine
- Enerisant
- GSK-189,254
- Impentamine
- Iodophenpropit
- Irdabisant
- JNJ-5207852
- MK-0249
- NNC 38-1049
- PF-03654746
- Pitolisant
- SCH-79687
- Thioperamide
- VUF-5681
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H4 |
- Agonists: 4-Methylhistamine
- α-Methylhistamine
- Histamine
- OUP-16
- VUF-8430
- Antagonists: JNJ-7777120
- Mianserin
- Thioperamide
- Toreforant
- VUF-6002
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Transporter
(inhibitors) |
VMATs |
TAAR1 inactive |
- Amiodarone
- APP
- AZIK
- Bietaserpine
- Deserpidine
- Dihydrotetrabenazine
- Efavirenz
- GBR-12935
- GZ-793A
- Ibogaine
- Ketanserin
- Lobeline
- Methoxytetrabenazine
- Reserpine
- Rose bengal
- SD-809
- Tetrabenazine
- Valbenazine
- Vanoxerine (GBR-12909)
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TAAR1 active |
- Amphetamine
- Methamphetamine
- MDMA
- Phenethylamine
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Enzyme
(inhibitors) |
HDC |
- Catechin
- Meciadanol
- Naringenin
- Tritoqualine
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HNMT |
- Amodiaquine
- Diphenhydramine
- Harmaline
- Metoprine
- Quinacrine
- SKF-91,488
- Tacrine
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DAO |
- Pimagedine (aminoguanidine)
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Others |
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UpToDate Contents
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English Journal
- Molecular basis of in vitro affinity maturation and functional evolution of a neutralizing anti-human GM-CSF antibody.
- Eylenstein R1,2, Weinfurtner D1,2, Härtle S1, Strohner R1, Böttcher J3,4, Augustin M3, Ostendorp R1, Steidl S1.
- mAbs.MAbs.2016 Jan 2;8(1):176-86. doi: 10.1080/19420862.2015.1099774. Epub 2015 Sep 25.
- X-ray structure analysis of 4 antibody Fab fragments, each in complex with human granulocyte macrophage colony stimulating factor (GM-CSF), was performed to investigate the changes at the protein-protein binding interface during the course of in vitro affinity maturation by phage display selection.
- PMID 26406987
- Hydrogen peroxide modulates synaptic transmission in ventral horn neurons of the rat spinal cord.
- Ohashi M1, Hirano T1, Watanabe K1, Katsumi K1, Ohashi N2, Baba H2, Endo N1, Kohno T2.
- The Journal of physiology.J Physiol.2016 Jan 1;594(1):115-134. doi: 10.1113/JP271449. Epub 2015 Dec 7.
- KEY POINTS: Excessive production of reactive oxygen species (ROS) is implicated in many central nervous system disorders; however, the physiological role of ROS in spinal ventral horn (VH) neurons remains poorly understood. We investigated how pathological levels of H2 O2 , an abundant ROS, regulate
- PMID 26510999
- Spinal histamine in attenuation of mechanical hypersensitivity in the spinal nerve ligation-induced model of experimental neuropathy.
- Wei H1, Viisanen H1, You HJ2, Pertovaara A3.
- European journal of pharmacology.Eur J Pharmacol.2015 Dec 23. pii: S0014-2999(15)30433-7. doi: 10.1016/j.ejphar.2015.12.039. [Epub ahead of print]
- Here we studied whether and through which mechanisms spinal administration of histamine dihydrochloride (histamine) attenuates pain behavior in neuropathic animals. Experiments were performed in rats with spinal nerve ligation-induced neuropathy and a chronic intrathecal catheter for spinal drug del
- PMID 26723513
Japanese Journal
- 長期低用量アスピリン服用者における出血性消化管病変 (特集 低用量アスピリンによる消化管粘膜傷害研究の進歩)
- 生体分子の立体構造と分子間相互作用の研究を振り返って
- 石田 寿昌
- YAKUGAKU ZASSHI 132(7), 785-816, 2012
- … (4) conformational feature of histamine H2 receptor antagonists and design of cathepsin B inhibitors; …
- NAID 130001888694
- Roles of Histamine in Exercise-Induced Fatigue: Favouring Endurance and Protecting against Exhaustion
- Niijima-Yaoita Fukie,Tsuchiya Masahiro,Ohtsu Hiroshi [他],Yanai Kazuhiko,Sugawara Shunji,Endo Yasuo,Tadano Takeshi
- Biological and Pharmaceutical Bulletin 35(1), 91-97, 2012
- … Mice given a histamine H1-receptor antagonist [fexofenadine (peripherally acting) or pyrilamine (peripherally and centrally acting)] or an irreversible HDC inhibitor (α-fluoromethylhistidine) displayed less PW endurance than control mice. … Ranitidine (H2-receptor antagonist) tended to reduce endurance. … Other histamine-receptor (H3 and H4) antagonists had no significant effects on endurance. …
- NAID 130001872348
Related Links
- H 2-receptor see histamine receptor. ... About DUEXIS DUEXIS, a proprietary single-tablet combination of the NSAID ibuprofen and the histamine H2-receptor antagonist famotidine, is indicated for the relief of signs and symptoms of ...
- antagonist [an-tag´o-nist] antagonistic muscle. (see illustration.) 1. a substance that tends to nullify the action of another, as a drug that binds to a cellular receptor for a hormone, neurotransmitter, or another drug blocking the action ...
Related Pictures
★リンクテーブル★
[★]
- 英
- H2 receptor
- 同
- ヒスタミンH2受容体 histamine H2 receptor、H2レセプター
- 関
- ヒスタミン、ヒスタミン受容体
[★]
ヒスタミンH2受容体、ヒスタミンH2レセプター
- 関
- H2 receptor
[★]
- 関
- prostaglandin H2-thromboxane A2 receptor、thromboxane A2 receptor
[★]
H2受容体遮断薬、H2受容体拮抗薬
- 関
- H2 blocker、H2 receptor blocker
[★]
H2受容体遮断薬
- 関
- H2 receptor antagonist
[★]
- 関
- Histamine 2
- 同
- histamine-2
[★]