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Histamine H1 receptor
A histamine H1 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P35367]
Synonyms
H1R;
HH1R
Research
Bioassay Publications (115)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (1.74) | 18.2507 |
| 2000's | 46 (40.00) | 29.6817 |
| 2010's | 56 (48.70) | 24.3611 |
| 2020's | 11 (9.57) | 2.80 |
Compounds (124)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| histamine | Homo sapiens (human) | IC50 | 0.1585 | 1 | 2 |
| histamine | Homo sapiens (human) | Ki | 1,440,809,206.6944 | 11 | 11 |
| octoclothepine | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| adiphenine | Homo sapiens (human) | IC50 | 112.2020 | 1 | 1 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.0048 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | Ki | 0.0008 | 2 | 1 |
| amoxapine | Homo sapiens (human) | IC50 | 0.0990 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.0110 | 1 | 0 |
| astemizole | Homo sapiens (human) | IC50 | 0.0140 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.0022 | 3 | 2 |
| azelastine | Homo sapiens (human) | Ki | 0.0012 | 3 | 3 |
| cetirizine | Homo sapiens (human) | Ki | 0.0379 | 11 | 11 |
| chlordiazepoxide | Homo sapiens (human) | IC50 | 1.7950 | 1 | 0 |
| chlordiazepoxide | Homo sapiens (human) | Ki | 0.2080 | 1 | 0 |
| chlorpheniramine | Homo sapiens (human) | IC50 | 0.0660 | 1 | 1 |
| chlorpheniramine | Homo sapiens (human) | Ki | 0.0041 | 2 | 3 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.0145 | 2 | 1 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0031 | 2 | 1 |
| citalopram | Homo sapiens (human) | IC50 | 3.1940 | 1 | 0 |
| citalopram | Homo sapiens (human) | Ki | 0.3710 | 1 | 0 |
| clomipramine | Homo sapiens (human) | IC50 | 0.0850 | 1 | 0 |
| clomipramine | Homo sapiens (human) | Ki | 0.0098 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 29.4060 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 3.4160 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | IC50 | 0.0037 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.0004 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | IC50 | 0.1710 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | Ki | 0.0174 | 2 | 1 |
| domperidone | Homo sapiens (human) | IC50 | 1.3440 | 1 | 0 |
| domperidone | Homo sapiens (human) | Ki | 0.1560 | 1 | 0 |
| doxepin | Homo sapiens (human) | IC50 | 0.0006 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.0002 | 3 | 2 |
| droperidol | Homo sapiens (human) | IC50 | 4.5190 | 1 | 0 |
| droperidol | Homo sapiens (human) | Ki | 0.5250 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.0283 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 0.0033 | 1 | 0 |
| fentanyl | Homo sapiens (human) | IC50 | 147.9110 | 1 | 1 |
| fexofenadine | Homo sapiens (human) | IC50 | 0.0622 | 4 | 4 |
| fexofenadine | Homo sapiens (human) | Ki | 0.0270 | 1 | 1 |
| fluphenazine | Homo sapiens (human) | IC50 | 0.0400 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 0.0223 | 2 | 1 |
| haloperidol | Homo sapiens (human) | IC50 | 2.7810 | 1 | 0 |
| haloperidol | Homo sapiens (human) | Ki | 0.4746 | 5 | 4 |
| hydroxyzine | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| ifenprodil | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| imipramine | Homo sapiens (human) | IC50 | 0.0270 | 1 | 1 |
| imipramine | Homo sapiens (human) | Ki | 0.0100 | 1 | 1 |
| ketanserin | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| ketotifen | Homo sapiens (human) | IC50 | 0.0011 | 2 | 1 |
| ketotifen | Homo sapiens (human) | Ki | 0.0001 | 2 | 1 |
| loratadine | Homo sapiens (human) | IC50 | 0.2300 | 2 | 1 |
| loratadine | Homo sapiens (human) | Ki | 0.1955 | 4 | 3 |
| maprotiline | Homo sapiens (human) | IC50 | 0.0088 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.0013 | 2 | 1 |
| methapyrilene | Homo sapiens (human) | IC50 | 0.0160 | 1 | 0 |
| methapyrilene | Homo sapiens (human) | Ki | 0.0018 | 1 | 0 |
| mianserin | Homo sapiens (human) | IC50 | 0.0024 | 2 | 1 |
| mianserin | Homo sapiens (human) | Ki | 0.0009 | 2 | 1 |
| mirtazapine | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.0500 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.0059 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | IC50 | 49.4823 | 2 | 1 |
| orphenadrine | Homo sapiens (human) | Ki | 0.1440 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | IC50 | 0.0240 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.0028 | 1 | 0 |
| procyclidine | Homo sapiens (human) | IC50 | 17.7828 | 1 | 1 |
| promazine | Homo sapiens (human) | IC50 | 1.2291 | 2 | 1 |
| promazine | Homo sapiens (human) | Ki | 0.0004 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 0.0041 | 2 | 1 |
| promethazine | Homo sapiens (human) | Ki | 0.0003 | 1 | 0 |
| pyrilamine | Homo sapiens (human) | IC50 | 0.0166 | 15 | 15 |
| pyrilamine | Homo sapiens (human) | Ki | 45,562,454,545,454.5500 | 11 | 10 |
| quetiapine | Homo sapiens (human) | IC50 | 0.0396 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 0.0129 | 5 | 4 |
| risperidone | Homo sapiens (human) | IC50 | 0.4515 | 6 | 5 |
| risperidone | Homo sapiens (human) | Ki | 0.0309 | 8 | 7 |
| terfenadine | Homo sapiens (human) | IC50 | 0.0115 | 2 | 1 |
| terfenadine | Homo sapiens (human) | Ki | 0.0335 | 3 | 2 |
| thioridazine | Homo sapiens (human) | IC50 | 0.0720 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.0084 | 1 | 0 |
| trazodone | Homo sapiens (human) | IC50 | 0.3610 | 1 | 0 |
| trazodone | Homo sapiens (human) | Ki | 0.0420 | 1 | 0 |
| tripelennamine | Homo sapiens (human) | IC50 | 0.0398 | 1 | 2 |
| tripelennamine | Homo sapiens (human) | Ki | 100,000,000,000,000.0000 | 1 | 1 |
| zotepine | Homo sapiens (human) | Ki | 0.0020 | 2 | 2 |
| lysergic acid diethylamide | Homo sapiens (human) | Ki | 1.5400 | 1 | 1 |
| phentolamine | Homo sapiens (human) | IC50 | 316.2280 | 1 | 1 |
| mepazine | Homo sapiens (human) | IC50 | 0.0270 | 1 | 0 |
| mepazine | Homo sapiens (human) | Ki | 0.0031 | 1 | 0 |
| cyclizine | Homo sapiens (human) | IC50 | 0.0380 | 1 | 0 |
| cyclizine | Homo sapiens (human) | Ki | 0.0044 | 1 | 0 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| dibenzepin | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| dimenhydrinate | Homo sapiens (human) | IC50 | 0.3190 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | Ki | 0.0370 | 1 | 0 |
| azacyclonol | Homo sapiens (human) | Ki | 0.6590 | 1 | 1 |
| dimethindene | Homo sapiens (human) | Ki | 0.0007 | 1 | 1 |
| clemastine | Homo sapiens (human) | IC50 | 0.0004 | 1 | 0 |
| clemastine | Homo sapiens (human) | Ki | 0.0000 | 1 | 0 |
| metergoline | Homo sapiens (human) | IC50 | 4.1330 | 1 | 0 |
| metergoline | Homo sapiens (human) | Ki | 0.4800 | 1 | 0 |
| lisuride | Homo sapiens (human) | IC50 | 0.1600 | 1 | 0 |
| lisuride | Homo sapiens (human) | Ki | 0.0190 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | IC50 | 0.0063 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | Ki | 0.0007 | 1 | 0 |
| penfluridol | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| sertindole | Homo sapiens (human) | Ki | 0.2853 | 2 | 2 |
| sch 37370 | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| aripiprazole | Homo sapiens (human) | IC50 | 0.4200 | 3 | 3 |
| aripiprazole | Homo sapiens (human) | Ki | 0.0400 | 4 | 4 |
| ziprasidone | Homo sapiens (human) | Ki | 0.1531 | 4 | 4 |
| mizolastine | Homo sapiens (human) | Ki | 0.0027 | 1 | 1 |
| 2-(2-aminoethyl)pyridine | Homo sapiens (human) | IC50 | 1.2589 | 1 | 2 |
| 2-(2-aminoethyl)pyridine | Homo sapiens (human) | Ki | 6,309,570,000.0000 | 1 | 1 |
| 3,3-diphenylpropylamine | Homo sapiens (human) | Ki | 5.1720 | 2 | 3 |
| gr 127935 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| desloratadine | Homo sapiens (human) | IC50 | 0.0059 | 2 | 1 |
| desloratadine | Homo sapiens (human) | Ki | 0.0012 | 3 | 2 |
| rupatadine | Homo sapiens (human) | IC50 | 0.0039 | 1 | 1 |
| rupatadine | Homo sapiens (human) | Ki | 0.0040 | 1 | 1 |
| sonepiprazole | Homo sapiens (human) | Ki | 1.6000 | 1 | 1 |
| asenapine | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| latrepirdine | Homo sapiens (human) | IC50 | 0.8695 | 4 | 4 |
| conessine | Homo sapiens (human) | Ki | 6.6716 | 2 | 6 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 5.1768 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 2.4759 | 1 | 0 |
| chlorprothixene | Homo sapiens (human) | IC50 | 0.4360 | 1 | 2 |
| chlorprothixene | Homo sapiens (human) | Ki | 0.0038 | 1 | 1 |
| doxepin hydrochloride | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| lobeline | Homo sapiens (human) | IC50 | 44.6684 | 1 | 1 |
| flunarizine | Homo sapiens (human) | IC50 | 0.1580 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 0.0180 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 0.0032 | 1 | 0 |
| benztropine | Homo sapiens (human) | Ki | 0.0004 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 0.0740 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.0086 | 1 | 0 |
| thioperamide | Homo sapiens (human) | Ki | 6.2659 | 3 | 8 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| jnj 7777120 | Homo sapiens (human) | Ki | 5.4572 | 4 | 17 |
| ketotifen fumarate | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| triprolidine | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| 2-(3-trifluoromethylphenyl)histamine | Homo sapiens (human) | IC50 | 1.0000 | 1 | 2 |
| 2-(3-trifluoromethylphenyl)histamine | Homo sapiens (human) | Ki | 251,189,000,000.0000 | 1 | 1 |
| sb 277011 | Homo sapiens (human) | Ki | 0.6310 | 2 | 2 |
| l 745870 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| mdl 100907 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| ciproxifan | Homo sapiens (human) | Ki | 5.5547 | 3 | 8 |
| abt-100 | Homo sapiens (human) | Ki | 10.0000 | 1 | 0 |
| dibutyl phthalate | Homo sapiens (human) | Ki | 2.5119 | 1 | 1 |
| n-demethylloperamide | Homo sapiens (human) | Ki | 0.0042 | 1 | 1 |
| a 304121 | Homo sapiens (human) | Ki | 69.1831 | 1 | 2 |
| 4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 0.8633 | 2 | 4 |
| n-(4-((4-(dimethylamino)quinazolin-2-yl)amino)cyclohexyl)-3,4-difluorobenzamide hydrochloride | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
| jnj 10181457 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pitolisant | Homo sapiens (human) | Ki | 1.1482 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 0.6100 | 1 | 1 |
| gsk239512 | Homo sapiens (human) | Ki | 2.5119 | 1 | 1 |
| 9-(aminomethyl)-9,10-dihydroanthracene | Homo sapiens (human) | Ki | 0.1380 | 2 | 3 |
| n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | Ki | 7.8800 | 1 | 1 |
| histaprodifen | Homo sapiens (human) | IC50 | 0.7943 | 1 | 2 |
| histaprodifen | Homo sapiens (human) | Ki | 501,187,000,000.0000 | 1 | 1 |
| cariprazine | Homo sapiens (human) | Ki | 0.0232 | 1 | 1 |
| methimepip | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| mk-0249 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| octoclothepine, (s)-isomer | Homo sapiens (human) | Ki | 0.0150 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| gsk 1004723 | Homo sapiens (human) | Ki | 0.0115 | 4 | 4 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| LSM-2536 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 3.1740 | 2 | 4 |
| clozapine | Homo sapiens (human) | IC50 | 0.0049 | 1 | 0 |
| clozapine | Homo sapiens (human) | Ki | 0.0035 | 8 | 7 |
| olanzapine | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
| olanzapine | Homo sapiens (human) | Ki | 0.0034 | 7 | 6 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| pyrilamine | Homo sapiens (human) | Kb | 0.0003 | 1 | 1 |
| metergoline | Homo sapiens (human) | Activity | 0.0982 | 1 | 1 |
| ziprasidone | Homo sapiens (human) | Activity | 0.0430 | 1 | 1 |
| clozapine | Homo sapiens (human) | Activity | 0.0012 | 1 | 1 |
| clozapine | Homo sapiens (human) | INH | 0.0012 | 1 | 1 |
| norclozapine | Homo sapiens (human) | INH | 0.0031 | 1 | 1 |
[no title available]Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the HEuropean journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Linking agonist binding to histamine H1 receptor activation.Nature chemical biology, , Volume: 1, Issue:2, 2005
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
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
[no title available],
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine HBioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
The discovery of quinoline based single-ligand human HBioorganic & medicinal chemistry letters, , 12-15, Volume: 26, Issue:24, 2016
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.Bioorganic & medicinal chemistry, , Oct-15, Volume: 20, Issue:20, 2012
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Linking agonist binding to histamine H1 receptor activation.Nature chemical biology, , Volume: 1, Issue:2, 2005
5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:11, 2007
Polypharmacology - foe or friend?Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
[no title available],
Identification of Ligand Binding Hot Spots of the Histamine HJournal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
[no title available],
CNS drug design: balancing physicochemical properties for optimal brain exposure.Journal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H(1) antagonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 19, Issue:10, 2009
Further evaluation of the tropane analogs of haloperidol.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
[no title available],
Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 30, Issue:21, 2020
Polypharmacology - foe or friend?Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
[no title available],
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine HJournal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Norpiperidine imidazoazepines as a new class of potent, selective, and nonsedative H1 antihistamines.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
[no title available],
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Identification of Ligand Binding Hot Spots of the Histamine HJournal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor.Journal of medicinal chemistry, , Aug-23, Volume: 55, Issue:16, 2012
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
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
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.Journal of natural products, , Volume: 69, Issue:3, 2006
Linking agonist binding to histamine H1 receptor activation.Nature chemical biology, , Volume: 1, Issue:2, 2005
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
[no title available],
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 30, Issue:20, 2020
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 30, Issue:8, 2020
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
CNS drug design: balancing physicochemical properties for optimal brain exposure.Journal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
[no title available],
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
[no title available]Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine HJournal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and HBioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Route to Prolonged Residence Time at the Histamine HJournal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
[no title available],
Route to Prolonged Residence Time at the Histamine HJournal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 20, Issue:1, 2010
Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 19, Issue:12, 2009
Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor.Journal of medicinal chemistry, , Aug-23, Volume: 55, Issue:16, 2012
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
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
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.The Journal of pharmacology and experimental therapeutics, , Volume: 309, Issue:1, 2004
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
The discovery of the benzazepine class of histamine H3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
The discovery of quinoline based single-ligand human HBioorganic & medicinal chemistry letters, , 12-15, Volume: 26, Issue:24, 2016
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.Bioorganic & medicinal chemistry, , Oct-15, Volume: 20, Issue:20, 2012
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
[no title available]Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| histamine receptor activity | molecular function | Combining with histamine to initiate a change in cell activity. Histamine is a physiologically active amine, found in plant and animal tissue and released from mast cells as part of an allergic reaction in humans. [GOC:ai] |
| G protein-coupled serotonin receptor activity | molecular function | Combining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai] |
| neurotransmitter receptor activity | molecular function | Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 12 target(s):
| Target | Category | Definition |
|---|
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| memory | biological process | The activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089] |
| visual learning | biological process | Any process in an organism in which a change in behavior of an individual occurs in response to repeated exposure to a visual cue. [GOC:jid, ISBN:0582227089] |
| regulation of vascular permeability | biological process | Any process that modulates the extent to which blood vessels can be pervaded by fluid. [GOC:jl] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| regulation of synaptic plasticity | biological process | A process that modulates synaptic plasticity, the ability of synapses to change as circumstances require. They may alter function, such as increasing or decreasing their sensitivity, or they may increase or decrease in actual numbers. [GOC:dph, GOC:jid, GOC:tb, PMID:11891290] |
| cellular response to histamine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a histamine stimulus. Histamine, the biogenic amine 2-(1H-imidazol-4-yl)ethanamine, is involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter. [GOC:mah] |
| G protein-coupled serotonin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled serotonin receptor binding to one of its physiological ligands. [GOC:mah] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |