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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/01/29 13:57:26」(JST)
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Clobenpropit
|
Systematic (IUPAC) name |
N'-[(4-chlorophenyl)methyl]-1-[3-(3H-imidazol-4-yl)propylsulfanyl]formamidine |
Clinical data |
Legal status |
? |
Identifiers |
CAS number |
145231-45-4 |
ATC code |
None |
PubChem |
CID 2790 |
IUPHAR ligand |
1223 |
ChemSpider |
2688 |
ChEMBL |
CHEMBL14690 |
Chemical data |
Formula |
C14H17ClN4S |
Mol. mass |
308.83 g/mol |
SMILES
- C1=CC(=CC=C1CN=C(N)SCCCC2=CN=CN2)Cl
|
Clobenpropit is a histamine H3 receptor antagonist.[1] It has neuroprotective effects via stimulation of GABA release in the brain.[2]
See also[edit]
References[edit]
- ^ Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P (2007). "The human histamine H3 receptor couples to GIRK channels in Xenopus oocytes". European Journal of Pharmacology 567 (3): 206–210. doi:10.1016/j.ejphar.2007.04.032. PMID 17537431.
- ^ Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z (2007). "The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons". European Journal of Pharmacology 563 (1-3): 117–123. doi:10.1016/j.ejphar.2007.01.069. PMID 17350613.
Histaminergics
|
|
Receptor |
H1
|
- Agonists: 2-Pyridylethylamine
- Betahistine
- Histamine
- HTMT
- UR-AK49
Antagonists: 1st 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
- Deptropine
- Dexbrompheniramine
- Dexchlorpheniramine
- Dimenhydrinate
- Dimetindene
- Diphenhydramine
- Diphenylpyraline
- Doxylamine
- Embramine
- Etodroxizine
- Etybenzatropine/Ethylbenztropine
- Etymemazine
- Flunarizine
- Histapyrrodine
- Homochlorcyclizine
- Hydroxyethylpromethazine
- Hydroxyzine
- Isopromethazine
- Isothipendyl
- Meclozine
- Mepyramine/Pyrilamine
- Mequitazine
- Methafurylene
- Methapyrilene
- Methdilazine
- Moxastine
- Niaprazine
- Orphenadrine
- Oxatomide
- Oxomemazine
- Phenindamine
- Pheniramine
- Phenyltoloxamine
- Pimethixene
- Piperoxan
- Pipoxizine
- Promethazine
- Propiomazine
- Pyrrobutamine
- Talastine
- Thenalidine
- Thenyldiamine
- Thiazinamium
- Thonzylamine
- Tolpropamine
- Tripelennamine
- Triprolidine
- 2nd generation: Acrivastine
- Alinastine
- Astemizole
- Azelastine
- Bamirastine
- Barmastine
- Bepiastine
- Bepotastine
- Bilastine
- Cabastinen
- Carebastine
- Cetirizine
- Clemastine
- Clemizole
- Clobenztropine
- Dorastine
- Ebastine
- Emedastine
- Epinastine
- Flezelastine
- Ketotifen
- Latrepirdine
- Levocabastine
- Linetastine
- Loratadine
- Mapinastine
- Mebhydrolin
- Mizolastine
- Moxastine
- Noberastine
- Octastine
- Olopatadine
- Perastine
- Piclopastine
- Rocastine
- Rupatadine
- Setastine
- Talastine
- Temelastine
- Terfenadine
- Zepastine
- 3rd generation: Desloratadine
- Fexofenadine
- Levocetirizine
- Ungrouped: Belarizine
- Efletirizine
- Elbanizine
- Flotrenizine
- Medrylamine
- Napactadine
- Pibaxizine
- Tagorizine
- Trelnarizine
- Trenizine
- Vapitadine
- Miscellaneous: Tricyclic antidepressants (amitriptyline,
- doxepin,
- trimipramine, etc)
- Tetracyclic antidepressants (mianserin,
- mirtazapine, etc)
- Typical antipsychotics (chlorpromazine,
- thioridazine, etc)
- Atypical antipsychotics (clozapine,
- olanzapine,
- quetiapine, etc)
|
|
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
- Betahistine
- Burimamide
- Ciproxifan
- Clobenpropit
- Conessine
- GSK-189,254
- Impentamine
- Iodophenpropit
- JNJ-5,207,852
- MK-0249
- NNC-38-1,049
- PF-03654746
- Pitolisant
- SCH-79,687
- Thioperamide
- VUF-5,681
|
|
H4
|
- Agonists: 4-Methylhistamine
- Histamine
- VUF-8,430
Antagonists: JNJ-7,777,120
- Thioperamide
- VUF-6,002
|
|
|
Transporter |
VMAT
|
- Inhibitors: Ibogaine
- Reserpine
- Tetrabenazine
|
|
|
Enzyme |
HDC
|
- Inhibitors: Catechin
- Meciadanol
- Naringenin
- Tritoqualine
|
|
HNMT
|
- Inhibitors: Amodiaquine
- Diphenhydramine
- Harmaline
- Metoprine
- Quinacrine
- SKF-91,488
- Tacrine
|
|
DAO
|
- Inhibitors: Aminoguanidine
|
|
|
Others |
Endogenous
|
- Histamine; Precursors: L-Histidine; Cofactors: Vitamin B6
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|
|
English Journal
- Hippocampal-Dependent Antidepressant Action of the H3 Receptor Antagonist Clobenpropit in a Rat Model of Depression.
- Femenía T1, Magara S1, DuPont CM1, Lindskog M2.
- The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP).Int J Neuropsychopharmacol.2015 Mar 11;18(9). pii: pyv032. doi: 10.1093/ijnp/pyv032.
- BACKGROUND: Histamine is a modulatory neurotransmitter regulating neuronal activity. Antidepressant drugs target modulatory neurotransmitters, thus ultimately regulating glutamatergic transmission and plasticity. Histamine H3 receptor (H3R) antagonists have both pro-cognitive and antidepressant effe
- PMID 25762718
- Enhancement of ionizing radiation response by histamine in vitro and in vivo in human breast cancer.
- Martinel Lamas DJ1, Cortina JE, Ventura C, Sterle HA, Valli E, Balestrasse KB, Blanco H, Cremaschi GA, Rivera ES, Medina VA.
- Cancer biology & therapy.Cancer Biol Ther.2015;16(1):137-48. doi: 10.4161/15384047.2014.987091.
- The radioprotective potential of histamine on healthy tissue has been previously demonstrated. The aims of this work were to investigate the combinatorial effect of histamine or its receptor ligands and gamma radiation in vitro on the radiobiological response of 2 breast cancer cell lines (MDA-MB-23
- PMID 25482934
Japanese Journal
- R-(?)-α-Methylhistamine, a Histamine H3 Receptor Agonist, Induces Endothelium-Dependent Vasodilation in Rat Mesenteric Resistance Arteries
- Sun Pengyuan,Jin Xin,Koyama Toshihiro,Li Simin,Kitamura Yoshihisa,Kawasaki Hiromu
- Biological & Pharmaceutical Bulletin 33(1), 58-63, 2010
- … This vasodilation was abolished by endothelium removal and attenuated by histamine H3 receptor antagonists, thioperamide and clobenpropit, but not by chlorpheniramine (histamine H1 receptor antagonist) and cimetidine (histamine H2 receptor antagonist). …
- NAID 130000140192
Related Links
- 「Clobenpropit Dihydrobromide, VUF 9153 コスモ・バイオ株式会社 SANTA CRUZ BIOTECHNOLOGY,INC.」の製品詳細情報ページです。バイオ百科では、その他の関連製品も簡単に検索することができます。
- Buy Clobenpropit Dihydrobromide, VUF 9153 (CAS 145231-45-4), a histamine H3 receptor antagonist, from Santa Cruz. MF: C14H17ClN4S 2HBr, MW: 470.65 ... アプリケーション: A histamine H3 receptor antagonist CAS 番号:
★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)