ジマプリット
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/02/15 09:45:42」(JST)
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Dimaprit
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Names |
IUPAC name
3-(dimethylamino)propyl carbamimidothioate
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Other names
3-dimethylaminopropyl sulfanylmethanimidamide
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Identifiers |
CAS Number
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65119-89-3 Y |
ChEMBL |
ChEMBL12344 N |
ChemSpider |
2968 |
IUPHAR/BPS
|
1248 |
Jmol interactive 3D |
Image |
KEGG |
C17930 |
PubChem |
3077 |
UNII |
ZZQ699148P N |
InChI
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InChI=1S/C6H15N3S/c1-9(2)4-3-5-10-6(7)8/h3-5H2,1-2H3,(H3,7,8)
Key: OLHQOJYVQUNWPL-UHFFFAOYSA-N
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InChI=1/C6H15N3S/c1-9(2)4-3-5-10-6(7)8/h3-5H2,1-2H3,(H3,7,8)
Key: OLHQOJYVQUNWPL-UHFFFAOYAQ
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Properties |
Chemical formula
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C6H15N3S |
Molar mass |
161.2684 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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N verify (what is YN ?) |
Infobox references |
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Dimaprit is a histamine analog working as a selective H2 histamine receptor agonist.[1][2][3]
References
- ^ Kartzung, Betram G.; Trevor, Anthony J., eds. (2014). Basic and Clinical Pharmacology (13th ed.). New York: McGraw-Hill Education. p. 364. ISBN 0071825053.
- ^ Kohno, S; Ogawa, K; Nabe, T; Yamamura, H; Ohata, K (May 1993). "Dimaprit, a Histamine H2-agonist, Inhibits Anaphylactic Histamine Release from Mast Cells and the Decreased Release is Restored by Thioperamide (H3-antagonist), but not by Cimetidine (H2-antagonist)". Japanese Journal of Pharmacology 62 (1): 75–9. PMID 7688057.
- ^ Nakamura, T; Ueno, Y; Goda, Y; Nakamura, A; Shinjo, K; Nagahisa, A (March 1997). "Efficacy of a Selective Histamine H2 Receptor Agonist, Dimaprit, in Experimental Models of Endotoxin Shock and Hepatitis in Mice". European Journal of Pharmacology 322 (1): 83–89. doi:10.1016/S0014-2999(96)00987-9.
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
- 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
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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
- NBI-98854
- Reserpine
- Rose bengal
- SD-809
- Tetrabenazine
- 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 |
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Others |
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English Journal
- Role of the thalamic submedius nucleus histamine H1 and H 2 and opioid receptors in modulation of formalin-induced orofacial pain in rats.
- Erfanparast A1, Tamaddonfard E, Taati M, Dabaghi M.
- Naunyn-Schmiedeberg's archives of pharmacology.Naunyn Schmiedebergs Arch Pharmacol.2015 Jun 16. [Epub ahead of print]
- Histamine and opioid systems are involved in supraspinal modulation of pain. In this study, we investigated the effects of separate and combined microinjections of agonists and antagonists of histamine H1 and H2 and opioid receptors into the thalamic submedius (Sm) nucleus on the formalin-induced or
- PMID 26077661
- Involvement of histaminergic inputs in the jaw-closing reflex arc.
- Gemba C1, Nakayama K2, Nakamura S2, Mochizuki A2, Inoue M3, Inoue T2.
- Journal of neurophysiology.J Neurophysiol.2015 Jun 1;113(10):3720-35. doi: 10.1152/jn.00515.2014. Epub 2015 Apr 22.
- Histamine receptors are densely expressed in the mesencephalic trigeminal nucleus (MesV) and trigeminal motor nucleus. However, little is known about the functional roles of neuronal histamine in controlling oral-motor activity. Thus, using the whole-cell recording technique in brainstem slice prepa
- PMID 25904711
- Cerebellar vermis H₂ receptors mediate fear memory consolidation in mice.
- Gianlorenço AC1, Riboldi AM2, Silva-Marques B3, Mattioli R4.
- Neuroscience letters.Neurosci Lett.2015 Feb 5;587:57-61. doi: 10.1016/j.neulet.2014.12.017. Epub 2014 Dec 15.
- Histaminergic fibers are present in the molecular and granular layers of the cerebellum and have a high density in the vermis and flocullus. Evidence supports that the cerebellar histaminergic system is involved in memory consolidation. Our recent study showed that histamine injections facilitate th
- PMID 25524412
Japanese Journal
- Cytokine responses of intraepithelial lymphocytes are regulated by histamine H2 receptor
- Effects of activation of central nervous histamine receptors in cardiovascular regulation; studies in H1 and H2 receptor gene knockout mice
- Naunyn-Schmiedeberg's archives of pharmacology 371, 99-106, 2006-12-14
- NAID 120000787414
- Curcuma longa Extract Protects against Gastric Ulcers by Blocking H_2 Histamine Receptors(Pharmacology)
Related Links
- Dimaprit. From Wikipedia, the free encyclopedia. Jump to: navigation, search. Dimaprit. IUPAC name. 3-dimethylaminopropyl ... Dimaprit is a histamine analog working as a H2 receptor agonist. [edit] References. Katzung, Bertram G. Basic and ...
★リンクテーブル★
[★]
- 英
- histamine receptor
- 関
- ヒスタミン、抗ヒスタミン薬、受容体
- H1R:平滑筋、血管内皮、神経→血管拡張、血管透過性↑、気管収縮、知覚神経刺激によるかゆみ・痛み
- H2R:胃、心臓、中枢、リンパ→胃酸分泌促進
- H3R:中枢、気道、消化管。ヒスタミン合成やNeuro transmitterの遊離抑制
- H4R:リンパ球をはじめとする免疫炭層細胞、骨髄、脾臓。機能は不明
- H1Rはα1受容体と似ている。Gαqと共役している
- H2Rはβ1受容体と似ている。Gαsと共役している
ヒスタミン受容体 (GOO.630)
[★]
- 英
- dimaprit