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Histamine H1 receptor
A histamine H1 receptor that is encoded in the genome of rat. [OMA:P31390, PRO:DNx]
Synonyms
H1R;
HH1R
Research
Bioassay Publications (10)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (10.00) | 18.7374 |
| 1990's | 5 (50.00) | 18.2507 |
| 2000's | 4 (40.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (23)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| histamine | Rattus norvegicus (Norway rat) | IC50 | 0.1585 | 1 | 3 |
| histamine | Rattus norvegicus (Norway rat) | Ki | 15,848,900,000.0000 | 1 | 1 |
| amitriptyline | Rattus norvegicus (Norway rat) | IC50 | 0.0000 | 1 | 2 |
| clomipramine | Rattus norvegicus (Norway rat) | IC50 | 0.0002 | 1 | 2 |
| desipramine | Rattus norvegicus (Norway rat) | IC50 | 0.0008 | 1 | 2 |
| doxepin | Rattus norvegicus (Norway rat) | IC50 | 0.0000 | 1 | 2 |
| haloperidol | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 2 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 1 | 1 |
| imipramine | Rattus norvegicus (Norway rat) | IC50 | 0.0001 | 1 | 2 |
| loxapine | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 2 |
| mianserin | Rattus norvegicus (Norway rat) | IC50 | 0.0000 | 1 | 2 |
| nortriptyline | Rattus norvegicus (Norway rat) | IC50 | 0.0000 | 1 | 2 |
| ondansetron | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 3 |
| pyrilamine | Rattus norvegicus (Norway rat) | IC50 | 0.0126 | 1 | 3 |
| pyrilamine | Rattus norvegicus (Norway rat) | Ki | 501,187,000,000,000.0000 | 1 | 1 |
| thioridazine | Rattus norvegicus (Norway rat) | IC50 | 0.0990 | 1 | 1 |
| tripelennamine | Rattus norvegicus (Norway rat) | IC50 | 0.0398 | 1 | 3 |
| tripelennamine | Rattus norvegicus (Norway rat) | Ki | 100,000,000,000,000.0000 | 1 | 1 |
| dimethindene | Rattus norvegicus (Norway rat) | Ki | 0.0007 | 1 | 8 |
| 2-(2-aminoethyl)pyridine | Rattus norvegicus (Norway rat) | IC50 | 1.2589 | 1 | 3 |
| 2-(2-aminoethyl)pyridine | Rattus norvegicus (Norway rat) | Ki | 6,309,570,000.0000 | 1 | 1 |
| 2-(3-trifluoromethylphenyl)histamine | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 3 |
| 2-(3-trifluoromethylphenyl)histamine | Rattus norvegicus (Norway rat) | Ki | 251,189,000,000.0000 | 1 | 1 |
| cilansetron | Rattus norvegicus (Norway rat) | Ki | 6.5000 | 1 | 3 |
| a 304121 | Rattus norvegicus (Norway rat) | Ki | 69.1831 | 1 | 3 |
| histaprodifen | Rattus norvegicus (Norway rat) | IC50 | 0.7943 | 1 | 3 |
| histaprodifen | Rattus norvegicus (Norway rat) | Ki | 501,187,000,000.0000 | 1 | 1 |
| clozapine | Rattus norvegicus (Norway rat) | IC50 | 0.0230 | 1 | 2 |
| clozapine | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 1 | 2 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| histamine | Rattus norvegicus (Norway rat) | EC50 | 4.4668 | 1 | 1 |
| monorden | Rattus norvegicus (Norway rat) | Kd | 0.0027 | 1 | 1 |
| methylhistaprodifen | Rattus norvegicus (Norway rat) | EC50 | 0.1585 | 1 | 1 |
| histaprodifen | Rattus norvegicus (Norway rat) | EC50 | 0.8511 | 1 | 1 |
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
N(alpha)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996