- 関
- specific agents
WordNet
- (biochemistry) a drug that can combine with a receptor on a cell to produce a physiological reaction
- a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist"
- someone involved in a contest or battle (as in an agon)
- amine formed from histidine that stimulates gastric secretions and dilates blood vessels; released by the human immune system during allergic reactions
- 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
- ヒスタミン(子宮収縮・血圧降下の薬)
- =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)』「2016/04/25 20:38:53」(JST)
[Wiki en表示]
A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes.
H2 : Betazole and Impromidine are examples of agonists used in diagnostics to increase histamine.
H3 : Betahistine is a weak Histamine1 agonist and a very strong Histamine3 antagonist (paradoxically histamine increasing).
See also
External links
- Histamine agonist at the US National Library of Medicine Medical Subject Headings (MeSH)
- MeSH list of agents 82017442
Histaminergics
|
|
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
- Rocastine
- Rupatadine
- Setastine
- 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
|
|
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
|
|
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
|
|
H4 |
- Agonists: 4-Methylhistamine
- α-Methylhistamine
- Histamine
- OUP-16
- VUF-8430
- Antagonists: JNJ-7777120
- Mianserin
- Thioperamide
- Toreforant
- VUF-6002
|
|
|
Transporter
(inhibitors) |
VMATs |
TAAR1 inactive |
- Amiodarone
- APP
- AZIK
- Bietaserpine
- Deserpidine
- Dihydrotetrabenazine
- Efavirenz
- GBR-12935
- GZ-793A
- Ibogaine
- Ketanserin
- Lobeline
- Methoxytetrabenazine
- NBI-98854
- Reserpine
- Rose bengal
- SD-809
- Tetrabenazine
- Vanoxerine (GBR-12909)
|
|
TAAR1 active |
- Amphetamine
- Methamphetamine
- MDMA
- Phenethylamine
|
|
|
|
Enzyme
(inhibitors) |
HDC |
- Catechin
- Meciadanol
- Naringenin
- Tritoqualine
|
|
HNMT |
- Amodiaquine
- Diphenhydramine
- Harmaline
- Metoprine
- Quinacrine
- SKF-91,488
- Tacrine
|
|
DAO |
|
|
|
Others |
|
|
Neuromodulation
|
|
Types |
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Partial agonist
- Antagonist
- Inverse agonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- ♦ Transporter [Reuptake]: Enhancer (RE)
- Inhibitor (RI)
- Releaser (RA)
- ♦ Miscellaneous: Precursor
- Cofactor
|
|
Classes |
Enzyme
|
see Enzyme inhibition
|
|
Ion channel
|
- Calcium channel blocker (CCB)
- Potassium channel blocker (PCB)
- Sodium channel blocker (SCB)
- Potassium channel opener (PCO)
|
|
Receptor &
transporter
|
BA/M
|
Adrenergic
|
- Adrenergic receptor agonist (α
- β (1
- 2))
- Adrenergic receptor antagonist (α (1
- 2), β)
- Adrenergic reuptake inhibitor (ARI)
|
|
Dopaminergic
|
- Dopamine receptor agonist
- Dopamine receptor antagonist
- Dopamine reuptake inhibitor (DRI)
|
|
Histaminergic
|
- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
|
|
Serotonergic
|
- Serotonin receptor agonist
- Serotonin Receptor Antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
|
|
|
AA
|
GABAergic
|
- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
|
|
Glutamatergic
|
- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
- Glutamate reuptake inhibitor
|
|
|
Cholinergic
|
- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
|
|
Cannabinoidergic
|
- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
- Endocannabinoid enhancer (eCBE)
- Endocannabinoid reuptake inhibitor (eCBRI)
|
|
Opioidergic
|
- Opioid modulator
- Opioid receptor agonist
- Opioid receptor antagonist
- Enkephalinase inhibitor
|
|
Other
|
- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
|
|
|
Miscellaneous
|
- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
|
|
|
UpToDate Contents
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English Journal
- Histamine infused into basolateral amygdala enhances memory consolidation of inhibitory avoidance.
- Benetti F, Izquierdo I.SourceCentro de Memória, Instituto do Cérebro (InsCER), Pontifícia Universidade Católica do Rio Grande do Sul, Porto Alegre, Brazil.
- The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP).Int J Neuropsychopharmacol.2013 Aug;16(7):1539-45. doi: 10.1017/S1461145712001514. Epub 2013 Jan 11.
- The role of the basolateral amygdala (BLA) in the consolidation of aversive memory is well established. Here we investigate the involvement of the histaminergic system in BLA on this variable. Rats were chronically implanted with bilateral cannulae in the BLA and after recovery were trained in a one
- PMID 23308396
- A Randomized Clinical Trial of Histamine 2 Receptor Antagonism in Treatment-Resistant Schizophrenia.
- Meskanen K, Ekelund H, Laitinen J, Neuvonen PJ, Haukka J, Panula P, Ekelund J.SourceFrom the *University of Helsinki, Department of Psychiatry and Helsinki University Central Hospital, Helsinki; †Heureka, the Finnish Science Centre, Vantaa; ‡Hospital District of Helsinki and Uusimaa, Lohja; §Department ofClinical Pharmacology, University of Helsinki, and HUSLAB, Helsinki University Central Hospital; ∥Hjelt Institute, University of Helsinki; ¶Neuroscience Center and Institute of Biomedicine, Anatomy, Faculty of Medicine, University of Helsinki, Helsinki; #Vaasa Hospital District, Vaasa; and **Research Unit for Severe Mental Disorders, National Institute for Health and Welfare, Helsinki, Finland.
- Journal of clinical psychopharmacology.J Clin Psychopharmacol.2013 Aug;33(4):472-478.
- Histamine has important functions as regulator of several other key neurotransmitters. Patients with schizophrenia have lower histamine H1 receptor levels. Since a case report in 1990 of an effect of the H2 antagonist famotidine on negative symptoms in schizophrenia, some open-label trials have been
- PMID 23764683
- Pleiotropic effect of histamine H4 receptor modulation in the central nervous system.
- Galeotti N, Sanna MD, Ghelardini C.SourceDepartment of Preclinical and Clinical Pharmacology, University of Florence, Viale G. Pieraccini 6, I-50139 Florence, Italy. nicoletta.galeotti@unifi.it
- Neuropharmacology.Neuropharmacology.2013 Aug;71:141-7. doi: 10.1016/j.neuropharm.2013.03.026. Epub 2013 Apr 11.
- The histamine H4 receptor (H4R) is expressed primarily on cells involved in inflammation and immune responses. Recently, it has been reported the functional expression of H4R within neurons of the central nervous system, but their role has been poorly understood. The present study aimed to elucidate
- PMID 23583928
Japanese Journal
- RBL-2H3細胞およびラット腹腔滲出細胞に対するγ-アミノ酪酸のヒスタミン遊離抑制作用
- 川崎 梓,原 崇,城 斗志夫
- 日本食品科学工学会誌 61(8), 362-366, 2014
- γ-アミノ酪酸(GABA)は好塩基球様RBL-2H3細胞およびラット腹腔浸出細胞(PEC)に対し,10~1 000μmol/Lの範囲で濃度依存的にIgE誘導性およびイオノマイシン誘発性ヒスタミン遊離を抑制した.また,GABAB受容体作動薬バクロフェンもRBL-2H3細胞およびPECのヒスタミン遊離を抑制した.これらの結果から,GABAは好塩基球やマスト細胞に対する脱顆粒阻害活性を有し,この阻害活性 …
- NAID 130004695486
- アレルギー性鼻炎におけるヒスタミンH1受容体遺伝子発現亢進の分子機構とその制御
- 北村 嘉章,水口 博之,福井 裕行 [他],武田 憲昭
- 耳鼻咽喉科臨床 107(4), 261-270, 2014
- … We are focusing on the histamine H1 receptor (H1R) as an allergic disease-sensitive gene. … H1R is a rate-limiting molecule of the H1R signal because the signal is increased with elevated receptor expression levels. … The mechanism of H1R gene expression was revealed to play a key role in the receptor expression level in studies using cultured HeLa cells and allergic rhinitis model rats. …
- NAID 130003395637
- G タンパク質共役型受容体の構造解析に向けた戦略 ~ヒスタミンH1受容体を例に~
- 白石 充典
- 薬学雑誌. 乙号 133(5), 539-547, 2013
- … We also present our success in determining the crystal structure of the histamine H1 receptor (H1R) in complex with doxepin, an inverse agonist antihistamine. …
- NAID 130003361947
Related Links
- Histamine agonist. From Wikipedia, the free encyclopedia. Jump to: navigation, search. A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes. Betahistine is an example used to ...
- H2 antagonists, like H1 antagonists, are also inverse agonists and not true antagonists. They act on H2 histamine receptors found principally in the parietal cells of the gastric mucosa, which are part of ...
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- 関
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