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Histamine H3 receptor
A histamine H3 receptor that is encoded in the genome of rat. [OMA:Q9QYN8, PRO:DNx]
Synonyms
H3R;
HH3R
Research
Bioassay Publications (47)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (8.51) | 18.2507 |
| 2000's | 23 (48.94) | 29.6817 |
| 2010's | 19 (40.43) | 24.3611 |
| 2020's | 1 (2.13) | 2.80 |
Compounds (42)
Drugs with Potency Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gossypol | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 0 |
| toxoflavin | Rattus norvegicus (Norway rat) | Potency | 3.9811 | 1 | 0 |
| nsc 663284 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 0 |
| irl 2500 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| bvt.948 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 0 |
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tyramine | Rattus norvegicus (Norway rat) | Km | 104.7000 | 1 | 1 |
| cep 26401 | Rattus norvegicus (Norway rat) | Kb | 0.0011 | 1 | 1 |
Different antagonist binding properties of human and rat histamine H3 receptors.Bioorganic & medicinal chemistry letters, , Apr-09, Volume: 11, Issue:7, 2001
New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.Bioorganic & medicinal chemistry letters, , May-19, Volume: 8, Issue:10, 1998
Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
A new family of H3 receptor antagonists based on the natural product Conessine.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
Benzylpiperidine variations on histamine H3 receptor ligands for improved drug-likeness.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
Radiofluorinated histamine H₃ receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.Bioorganic & medicinal chemistry, , May-01, Volume: 20, Issue:9, 2012
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Design, synthesis, and MedChemComm, , Feb-01, Volume: 10, Issue:2, 2019
[no title available]Bioorganic & medicinal chemistry, , 05-15, Volume: 26, Issue:9, 2018
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Different antagonist binding properties of human and rat histamine H3 receptors.Bioorganic & medicinal chemistry letters, , Apr-09, Volume: 11, Issue:7, 2001
New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.Bioorganic & medicinal chemistry letters, , May-19, Volume: 8, Issue:10, 1998
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.The Journal of pharmacology and experimental therapeutics, , Volume: 309, Issue:1, 2004
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Different antagonist binding properties of human and rat histamine H3 receptors.Bioorganic & medicinal chemistry letters, , Apr-09, Volume: 11, Issue:7, 2001
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
Design, synthesis, and structure-activity relationships of acetylene-based histamine H3 receptor antagonists.Journal of medicinal chemistry, , Mar-11, Volume: 42, Issue:5, 1999
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
In vitro studies on a class of quinoline containing histamine H3 antagonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.Journal of medicinal chemistry, , Oct-06, Volume: 48, Issue:20, 2005
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Structural modifications in the distal, regulatory region of histamine HEuropean journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
[no title available]Bioorganic & medicinal chemistry, , 05-15, Volume: 26, Issue:9, 2018
[no title available]Bioorganic & medicinal chemistry, , 05-15, Volume: 25, Issue:10, 2017
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.European journal of medicinal chemistry, , May-05, Volume: 95, 2015
Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 24, Issue:5, 2014
Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011