A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes.
H1 agonists promote wakefulness.[1]
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 antagonist of the Histamine3 autoreceptor. Antagonizing H3 increases histaminergic tone.
See also
References
- ^ Sakai, N.; Nishino, S. (2013). "Wake-Promoting Medications". Encyclopedia of Sleep. Elsevier. pp. 627–633. doi:10.1016/b978-0-12-378610-4.00126-1. ISBN 978-0-12-378611-1.
Although centrally injected histamine or histaminergic H1 agonists promote wakefulness, the systemic administration of these compounds induces various unacceptable side effects via peripheral H1 receptor stimulation.
External links
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| H1 | | Agonists | |
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| 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
- Perlapine
- 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
- Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, brilaroxazine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine)
- Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
- 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: Azanator
- Belarizine
- Elbanizine
- Flotrenizine
- GSK1004723
- Napactadine
- Tagorizine
- Trelnarizine
- Trenizine
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| H2 | | Agonists | |
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| 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 | |
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| Antagonists |
- A-349821
- A-423579
- ABT-239
- ABT-652
- AZD5213
- Bavisant
- Betahistine
- Burimamide
- Ciproxifan
- Clobenpropit
- Conessine
- Enerisant
- GSK-189254
- Impentamine
- Iodophenpropit
- Irdabisant
- JNJ-5207852
- NNC 38-1049
- PF-03654746
- Pitolisant
- SCH-79687
- Thioperamide
- VUF-5681
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| H4 | | Agonists | |
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| Antagonists |
- JNJ-7777120
- Mianserin
- Seliforant
- Thioperamide
- Toreforant
- VUF-6002
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- See also
- Receptor/signaling modulators
- Monoamine metabolism modulators
- Monoamine reuptake inhibitors
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Pharmacomodulation |
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| Types |
- ♦ Receptor: Agonist
- Partial agonist
- Antagonist
- Inverse agonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
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| Classes | | Enzyme | see Enzyme inhibition |
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| Ion channel | See Ion channel modulators |
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Receptor & transporter | | BA/M | | Adrenergic | |
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| Dopaminergic | |
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| Histaminergic |
- Histamine receptor antagonist (H1
- H2
- H3)
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| Serotonergic |
- Serotonin receptor agonist
- Serotonin receptor antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
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| AA | | GABAergic | |
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| Glutamatergic |
- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
- Glutamate reuptake inhibitor
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| Cholinergic |
- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
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| Cannabinoidergic |
- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
- Endocannabinoid enhancer (eCBE)
- Endocannabinoid reuptake inhibitor (eCBRI)
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| Opioidergic |
- Opioid modulator
- Opioid receptor agonist
- Opioid receptor antagonist
- Enkephalinase inhibitor
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| Other |
- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
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| Miscellaneous | |
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