Page last updated: 2024-08-07 16:16:38
Histamine H2 receptor
A histamine H2 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P25021]
Synonyms
H2R;
HH2R;
Gastric receptor I
Research
Bioassay Publications (44)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (4.55) | 18.2507 |
| 2000's | 17 (38.64) | 29.6817 |
| 2010's | 20 (45.45) | 24.3611 |
| 2020's | 5 (11.36) | 2.80 |
Compounds (80)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| metergoline | Homo sapiens (human) | Activity | 0.1040 | 1 | 1 |
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the HEuropean journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
[no title available]Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 11-15, Volume: 52, 2021
Fluorescent HACS medicinal chemistry letters, , Aug-13, Volume: 11, Issue:8, 2020
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
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
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
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
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
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
Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H-imidazole.Journal of medicinal chemistry, , Jan-20, Volume: 38, Issue:2, 1995
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
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
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
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
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
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
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
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
[no title available],
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
[no title available]Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DJournal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.Journal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Fluorescent HACS medicinal chemistry letters, , Aug-13, Volume: 11, Issue:8, 2020
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
New analogs of burimamide as potent and selective histamine H3 receptor antagonists: the effect of chain length variation of the alkyl spacer and modifications of the N-thiourea substituent.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
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
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 2 target(s):
| Target | Category | Definition |
|---|
| 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 |
|---|
| 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] |
| 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] |
Involved In
This protein is involved in 6 target(s):
| Target | Category | Definition |
|---|
| gastric acid secretion | biological process | The regulated release of gastric acid (hydrochloric acid) by parietal or oxyntic cells during digestion. [GOC:hjd] |
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| 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] |
| 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] |
| 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] |