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Receptors, Histamine H3

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Definition: A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)  DF: RECEPT H3    Other names Histamine H3 Receptors; Receptors, H3; Receptor, Histamine H3; H3 Receptors, Histamine; H3 Receptor, Histamine; Histamine H3 Receptor; H3 Receptors
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
5-(4-(3-(2-methylpyrrolidin-1-yl)propoxy)phenyl)-2-pyridin-2-yl-2H-pyridazin-3-one  0   *Pyridazines Histamine Antagonists Receptors, Histamine H3. J Med Chem. 2012 Jan 12;55(1):414-23.
6-(4-(3-(2-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-pyridazin-3-one  0   *Pyridazines *Pyrrolidines Receptors, Histamine H3. J Med Chem 2011 Jul 14;54(13):4781-92
1-(2-(4-cyclobutyl-(1,4)diazepane-1-carbonyl)-4-(3-fluorophenoxy)pyrrolidin-1-yl)ethanone  0   *Azepines *Pyrrolidines Receptors, Histamine H3. Bioorg Med Chem Lett 2010 May 1;20(9):2755-60
5-(fluoromethoxy)-N-methyl-3-oxo-N-(2-piperidin-1-ylethyl)-3H-spiro(2-benzofuran-1,1'-cyclohexane)-4'-carboxamide  0   *Benzofurans *Piperidines Deuterium Fluorine Radioisotopes Receptors, Histamine H3. Synapse 2009 Dec;63(121):1122-32
5-methoxy-N-methyl-3-oxo-N-(2-piperidin-1-ylethyl)-3H-spiro(2-benzofuran-1,1'-cyclohexane)-4'-carboxamide  0   *Benzofurans *Piperidines Carbon Radioisotopes Receptors, Histamine H3. Synapse 2009 Dec;63(121):1122-32
1-(3-(4-tert-butylphenoxy)propyl)-4-piperidino-piperidine  0   *Piperidines Ligands Receptors, Histamine H3. Bioorg Med Chem 2008 Sep 15;16(18):8729-36
2-((2-(1H-imidazol-4-yl)ethyl)sulfanyl)-1,3-benzothiazole  0   *Imidazoles *Benzothiazoles Receptors, Histamine H3. Chem Biodivers 2008 Jan;5(1):140-52
2-(1,3-dimethyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline  0   *Pyrazoles *Quinolines Receptors, Histamine H3. J Med Chem 2007 Nov 1;50(22):5439-48
2-(2,7-dimethylpyrazolo(1,5-a)pyrimidin-6-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline  0   *Pyrimidines *Quinolines Receptors, Histamine H3. J Med Chem 2007 Nov 1;50(22):5439-48
6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-pyridinecarboxamide  0   *Benzazepines Niacinamide/*analogs & derivatives Receptors, Histamine H3. J Pharmacol Exp Ther 2007 Jun;321(3):1032-45
1-(1-methylethyl)-4-((1-(6-(trifluoromethyl)-3-pyridinyl)-4-piperidinyl)carbonyl)hexahydro-1H-1,4-diazepine  0   *Azepines *Pyridines Receptors, Histamine H3. Biochem Pharmacol 2007 Apr 15;73(8):1182-94
5-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-2-pyrazinecarboxamide  0   *Benzazepines *Pyrazines Receptors, Histamine H3. Biochem Pharmacol 2007 Apr 15;73(8):1182-94
1-(3-(3-(4-chlorophenyl)propoxy)propyl)piperidine  0   *Piperidines Receptors, Histamine H3. J Pharmacol Exp Ther 2007 Jan;320(1):365-75
4-(3-(4-piperidin-1-ylbut-1-ynyl)benzyl)morpholine  0   *Morpholines *Piperidines Receptors, Histamine H3. Nucl Med Biol 2006 Aug;33(6):80-10
1-(3-(4-(1,1-dimethylpropyl)phenoxy)propyl)piperidine  0   *Piperidines Receptors, Histamine H3. Bioorg Med Chem 2006 May 15;14(10):3522-9
(2-(2-(2-methylpyrrolidin-1-yl)ethyl)benzofuran-5-yl)(5-nitropyridin-2-yl)amine  0   *Benzofurans *Pyrrolidines Receptors, Histamine H3/antagonists & inhibitors. J Med Chem 2005 Oct 6;48(20):6482-90
4-(imidazol-4-ylmethyl)-1-methylpiperidine  0   *Imidazoles *Piperidines Receptors, Histamine H3/agonists. J Med Chem 2005 Mar 24;48(6):2100-7
4-(2-(2-(2-methyl-1-pyrrolidinyl)ethyl)-1-benzofuran-5-yl)benzonitrile  0   *Benzofurans *Pyrrolidines Receptors, Histamine H3/antagonists & inhibitors. J Med Chem 2005 Jan 13;48(1):38-55
1-(4-(3-piperidin-1-ylpropoxy)benzyl)piperidine  0   *Piperidines Receptors, Histamine H3/antagonists & inhibitors. J Med Chem 2003 Aug 28;46(18):3938-44
SCH 79687  0   *Imidazoles *Phenylurea Compounds Receptors, Histamine H3/antagonists & inhibitors. J Pharmacol Exp Ther 2003 Jun;305(3):1037-44
N-(2-(4-(3-(4-(cyclopropylcarbonyl)phenoxy)propyl)-1-piperazinyl)-1-methyl-2-oxoethyl)-2-furamide  0   *Piperazines Receptors, Histamine H3/antagonists & inhibitors. J Pharmacol Exp Ther 2003 Jun;305(3):887-96
4-((3-(4-(2-aminopropanoyl)-1-piperazinyl)propoxy)phenyl)cyclopropylmethanone  0   *Piperazines Receptors, Histamine H3/antagonists & inhibitors. J Pharmacol Exp Ther 2003 Jun;305(3):887-96
2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane  0   *Cyclopropanes *Imidazoles Receptors, Histamine H3/agonists. J Med Chem 2003 May 8;46(10):1980-8
3-(1H-imidazol-4-yl)propyl N-(1,2,2-trimethylpropyl) carbamate  0   *Carbamates *Imidazoles Receptors, Histamine H3/antagonists & inhibitors. J Med Chem 2002 Aug 29;45(18):4000-10
SP9144 receptor  0   *Receptors, Histamine H3. J Pharmacol Exp Ther 2001 Mar;296(3):1058-66
proxyfan  0   *Imidazoles Receptors, Histamine H3/antagonists & inhibitors. Nature 2000 Dec 14;408(6814):860-4
imoproxifan  0   *Imidazoles *Oximes Receptors, Histamine H3/antagonists & inhibitors. J Med Chem 2000 Aug 24;43(17):3335-43
N-(4-chlorobenzyl)-N-(6-pyrrolidin-1-ylhexyl)guanidine  0   *Guanidines *Pyrrolidines Receptors, Histamine H3/antagonists & inhibitors. J Med Chem 2000 Jun 15;43(12):2362-70
N-(4-chlorobenzyl)-N-(7-pyrrolidin-1-ylheptyl)guanidine  0   *Guanidines *Pyrrolidines Receptors, Histamine H3/antagonists & inhibitors. J Med Chem 2000 Jun 15;43(12):2362-70
FUB 271  0   *Imidazoles *Iodobenzenes Iodine Radioisotopes Receptors, Histamine H3/antagonists & inhibitors. Nucl Med Biol 1999 Aug;26(6):651-9
GR 190028  0   *Imidazoles *Oxadiazoles Iodine Radioisotopes Receptors, Histamine H3/antagonists & inhibitors. Nucl Med Biol 1999 Aug;26(6):651-9
4-(4-methyl-3-pyrrolidinyl)-1H-imidazole dihydrochloride  0   *Imidazoles *Pyrrolidines Receptors, Histamine H3/agonists. J Pharmacol Exp Ther 1998 Oct;287(1):43-50
4-ethynylphenyl 3-(1H-imidazol-4-yl)propyl ether  0   *Ethers *Imidazoles Receptors, Histamine H3. J Med Chem 1998 Oct 8;41(21):4171-6
4-(2-(5,5-dimethylhex-1-ynyl)cyclopropyl)imidazole  0   *Imidazoles Stereoisomerism Receptors, Histamine H3/antagonists & inhibitors. Eur J Pharmacol 1998 Jun 26;351(3):307-11
4-(6-cyclohexylhex-3-enyl)imidazole  0   *Imidazoles Ligands Stereoisomerism Receptors, Histamine H3/antagonists & inhibitors. Eur J Pharmacol 1998 Jun 26;351(3):307-11
FUB 181  0   *Imidazoles Receptors, Histamine H3. Arch Pharm (Weinheim) 1998 Jun;331(6):211-8
AQ 0145  0   *Amidines *Imidazoles Adamantane/*analogs & derivatives Receptors, Histamine H3/antagonists & inhibitors. Methods Find Exp Clin Pharmacol 1995 Nov;17 Suppl C:70-3
4-(1-cyclohexylpentanoyl-4-piperidyl)-1H-imidazole  0   *Imidazoles Receptors, Histamine H3/antagonists & inhibitors. J Pharamcol Exp Ther 1995 Nov;275(2):598-604

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012
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