- 関
- H3 agonist
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
PrepTutorEJDIC
- ヒスタミン(子宮収縮・血圧降下の薬)
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/12/04 02:40:25」(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
- Cyclizine
- Cyproheptadine
- Dacemazine
- Decloxizine
- Deptropine
- Dexbrompheniramine
- Dexchlorpheniramine
- Dimenhydrinate
- Dimetindene
- Diphenhydramine
- Diphenylpyraline
- Doxylamine
- Embramine
- Etodroxizine
- Etybenzatropine (ethylbenztropine)
- Etymemazine
- 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
- 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
- Lafutidine
- Lamtidine
- Lavoltidine (loxtidine)
- Lupitidine
- Metiamide
- Mifentidine
- Niperotidine
- Nizatidine
- Osutidine
- Oxmetidine
- Pibutidine
- Quisultazine (quisultidine)
- Ramixotidine
- Ranitidine
- Roxatidine
- Sufotidine
- Tiotidine
- Tuvatidine
- Venritidine
- Xaltidine
|
|
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
- 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 |
|
|
Index of the respiratory system
|
|
Description |
- Anatomy
- Physiology
- Development
|
|
Disease |
- Congenital
- Neoplasms and cancer
- Chest trauma
- Infection
- common cold
- pneumonia
- tuberculosis
- Other
- Symptoms and signs
|
|
Treatment |
- Procedures
- Drugs
- nasal
- throat
- obstructive airway diseases
- cough and cold
- histaminergics
- pulmonary arterial hypertension
- other
- Surgery
|
|
|
Neuromodulation
|
|
Types |
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Antagonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- Inverse agonist
- ♦ 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))
|
|
Endocannabinoid
|
- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
|
|
Opioidergic
|
- Opioid modulator
- Opioid receptor agonist
- Opioid receptor antagonist
|
|
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 may contribute to vortioxetine's procognitive effects; possibly through an orexigenic mechanism.
- Smagin GN1, Song D1, Budac DP2, Waller JA3, Li Y3, Pehrson AL3, Sánchez C4.
- Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2016 Jul 4;68:25-30. doi: 10.1016/j.pnpbp.2016.03.001. Epub 2016 Mar 2.
- Vortioxetine is a novel multimodal antidepressant that acts as a serotonin (5-HT)3, 5-HT7, and 5-HT1D receptor antagonist; 5-HT1B receptor partial agonist; 5-HT1A receptor agonist; and 5-HT transporter inhibitor in vitro. In preclinical and clinical studies vortioxetine demonstrates positive effects
- PMID 26945513
- Clinical trials with H3-receptor inverse agonists: What they tell us about the role of histamine in the human brain.
- Schwartz JC1, Lecomte JM2.
- Neuropharmacology.Neuropharmacology.2016 Jul;106:35-6. doi: 10.1016/j.neuropharm.2016.04.006. Epub 2016 Apr 7.
- PMID 27060410
- Role of histamine H1-receptor on behavioral states and wake maintenance during deficiency of a brain activating system: A study using a knockout mouse model.
- Parmentier R1, Zhao Y2, Perier M1, Akaoka H1, Lintunen M3, Hou Y4, Panula P3, Watanabe T5, Franco P1, Lin JS6.
- Neuropharmacology.Neuropharmacology.2016 Jul;106:20-34. doi: 10.1016/j.neuropharm.2015.12.014. Epub 2015 Dec 23.
- Using knockout (KO) mice lacking the histamine (HA)-synthesizing enzyme (histidine decarboxylase, HDC), we have previously shown the importance of histaminergic neurons in maintaining wakefulness (W) under behavioral challenges. Since the central actions of HA are mediated by several receptor subtyp
- PMID 26723880
Japanese Journal
- The Affinity of Histamine for Gq Protein-Coupled Histamine H-Receptors Is Predominantly Regulated by Their Internalization in Human Astrocytoma Cells
- Hishinuma Shigeru,Sato Yuko,Akatsu Chizuru [他]
- Journal of pharmacological sciences 119(3), 233-242, 2012-07
- NAID 40019345175
- Inverse Agonistic Activity of Antihistamines and Suppression of Histamine H Receptor Gene Expression
- Mizuguchi Hiroyuki,Ono Shohei,Hattori Masashi [他]
- Journal of pharmacological sciences 118(1), 117-121, 2012-01
- NAID 40019137498
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Related Pictures
★リンクテーブル★
[★]
H3受容体刺激薬、H3刺激薬、H3作用薬、H3受容体アゴニスト
- 関
- histamine agonist
[★]
- 英
- histamine agonist
- 関
- H3作用薬、ヒスタミン受容体刺激薬、H3刺激薬
[★]
- 英
- histamine agonist
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- ヒスタミン作動薬