EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0223-5234, 08/2014, Volume 83, pp. 534 - 546
A series of novel 2-amino-4-(4-methylpiperazin-1-yl)-1,3,5-triazine derivatives with different aryl substituents in the 6-position was designed, synthesized...
Histamine H-4 receptor | CHEMISTRY, MEDICINAL | CYTOCHROMES | METABOLISM | Anti-inflammatory properties | METASITE | 2,4,6-Trisubstituted 1,3,5-triazines | 4-Methylpiperazines | INHIBITOR | BINDING | 2,4-DIAMINO-1,3,5-TRIAZINE DERIVATIVES
Histamine H-4 receptor | CHEMISTRY, MEDICINAL | CYTOCHROMES | METABOLISM | Anti-inflammatory properties | METASITE | 2,4,6-Trisubstituted 1,3,5-triazines | 4-Methylpiperazines | INHIBITOR | BINDING | 2,4-DIAMINO-1,3,5-TRIAZINE DERIVATIVES
Journal Article
EUROPEAN JOURNAL OF PHARMACOLOGY, ISSN 0014-2999, 10/2011, Volume 668, Issue 1-2, pp. 1 - 5
The discovery of the histamine H-4 receptor has added a new chapter to the century of extensive biogenic amine research. The human histamine H-4 receptor is...
Allergy | EOSINOPHILS | Autoimmune disease | Inflammation | MODEL | MEDIATES CHEMOTAXIS | MURINE | RESPONSES | Histamine H-4 receptor | Immunology | CELL-MIGRATION | EXPRESS | PHARMACOLOGY & PHARMACY | Antagonist | ANTAGONISTS | BINDING
Allergy | EOSINOPHILS | Autoimmune disease | Inflammation | MODEL | MEDIATES CHEMOTAXIS | MURINE | RESPONSES | Histamine H-4 receptor | Immunology | CELL-MIGRATION | EXPRESS | PHARMACOLOGY & PHARMACY | Antagonist | ANTAGONISTS | BINDING
Journal Article
FRONTIERS IN PHARMACOLOGY, ISSN 1663-9812, 03/2015, Volume 6
The histamine H-4 receptor (H4R) was first noted as a sequence in genomic databases that had features of a class A G-protein coupled receptor. This putative...
pruritus | ALLERGIC CONTACT-DERMATITIS | COLLAGEN-INDUCED ARTHRITIS | histamine | DENDRITIC CELLS | PHARMACOLOGICAL CHARACTERIZATION | MAST-CELLS | atopic dermatitis | asthma | H4 RECEPTOR | ATOPIC-DERMATITIS | HUMAN EOSINOPHILS | arthritis | PHARMACOLOGY & PHARMACY | MOLECULAR-CLONING | T-CELLS
pruritus | ALLERGIC CONTACT-DERMATITIS | COLLAGEN-INDUCED ARTHRITIS | histamine | DENDRITIC CELLS | PHARMACOLOGICAL CHARACTERIZATION | MAST-CELLS | atopic dermatitis | asthma | H4 RECEPTOR | ATOPIC-DERMATITIS | HUMAN EOSINOPHILS | arthritis | PHARMACOLOGY & PHARMACY | MOLECULAR-CLONING | T-CELLS
Journal Article
JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY, ISSN 0091-6749, 03/2009, Volume 123, Issue 3, pp. 619 - 625
Background: Histamine influences T-cell reactions via histamine receptors I and 2. The histamine receptor 4 (H4R) is the most recently identified histamine...
ACTIVATION | ANTIHISTAMINES | DENDRITIC CELLS | PRURITUS | AIRWAY INFLAMMATION | IMMUNOLOGY | T cells | IL-31 | SCRATCHING BEHAVIOR | Histamine | ATOPIC-DERMATITIS | ALLERGY | MICE | H-4 receptor | T-CELLS
ACTIVATION | ANTIHISTAMINES | DENDRITIC CELLS | PRURITUS | AIRWAY INFLAMMATION | IMMUNOLOGY | T cells | IL-31 | SCRATCHING BEHAVIOR | Histamine | ATOPIC-DERMATITIS | ALLERGY | MICE | H-4 receptor | T-CELLS
Journal Article
ORAL DISEASES, ISSN 1354-523X, 04/2015, Volume 21, Issue 3, pp. 378 - 385
ObjectivesOral lichen planus (OLP) is an autoimmune disease characterized by a band-like T-cell infiltrate below the apoptotic epithelial cells and degenerated...
KINASE | NOD1 | oral lichen planus | mast cells | RESPONSES | INHIBITION | EPITHELIAL-CELLS | oral pathology | DENTISTRY, ORAL SURGERY & MEDICINE | TOLL-LIKE RECEPTORS | histamine H-4 receptor | cytokines | EXPRESSION
KINASE | NOD1 | oral lichen planus | mast cells | RESPONSES | INHIBITION | EPITHELIAL-CELLS | oral pathology | DENTISTRY, ORAL SURGERY & MEDICINE | TOLL-LIKE RECEPTORS | histamine H-4 receptor | cytokines | EXPRESSION
Journal Article
BRITISH JOURNAL OF PHARMACOLOGY, ISSN 0007-1188, 09/2013, Volume 170, Issue 1, pp. 136 - 143
Background and Purpose Since the identification of the histamine H-4 receptor, several ligands activating this receptor have been described and more compounds...
histamine | clobenpropit | VUF8430 | PHARMACOLOGY & PHARMACY | histamine H-4 receptor | 4-methylhistamine | ST-1006 | UR-PI376
histamine | clobenpropit | VUF8430 | PHARMACOLOGY & PHARMACY | histamine H-4 receptor | 4-methylhistamine | ST-1006 | UR-PI376
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 05/2009, Volume 157, Issue 1, pp. 24 - 33
Since its discovery at the beginning of the 20th century, histamine has been established to play a pathophysiological regulatory role in cellular events...
Allergy; asthma | receptor ligands | Histamine | receptor | Histamine h | Immunomodulation | Rheumatoid arthritis | Inflammation | Pruritus | Immune system | pruritus | immunomodulation | histamine | PHARMACOLOGICAL CHARACTERIZATION | 1ST POTENT | allergy | asthma | T-CELL | rheumatoid arthritis | MAST-CELL | NEUTROPHIL RECRUITMENT | MEDIATES CHEMOTAXIS | H4 RECEPTOR | SYNOVIAL-CELLS | HUMAN EOSINOPHILS | inflammation | immune system | PHARMACOLOGY & PHARMACY | histamine H-4 receptor | MOLECULAR-CLONING | H-4 receptor ligands
Allergy; asthma | receptor ligands | Histamine | receptor | Histamine h | Immunomodulation | Rheumatoid arthritis | Inflammation | Pruritus | Immune system | pruritus | immunomodulation | histamine | PHARMACOLOGICAL CHARACTERIZATION | 1ST POTENT | allergy | asthma | T-CELL | rheumatoid arthritis | MAST-CELL | NEUTROPHIL RECRUITMENT | MEDIATES CHEMOTAXIS | H4 RECEPTOR | SYNOVIAL-CELLS | HUMAN EOSINOPHILS | inflammation | immune system | PHARMACOLOGY & PHARMACY | histamine H-4 receptor | MOLECULAR-CLONING | H-4 receptor ligands
Journal Article
EXPERT OPINION ON INVESTIGATIONAL DRUGS, ISSN 1354-3784, 10/2009, Volume 18, Issue 10, pp. 1519 - 1531
The identification of histamine H-3 (H3R) and H-4 (H4R) receptors some years ago revived interest in histamine research and exposed attractive perspectives for...
epilepsy | RHEUMATOID-ARTHRITIS | histamine | attention deficit hyperactivity disorder | H3R | MAST-CELLS | schizophrenia | INVERSE AGONISTS | inflammation | H-3-RECEPTOR LIGANDS | PHARMACOLOGY & PHARMACY | autoimmune disorders | pain | SYNOVIAL TISSUE | BRAIN HISTAMINE | H4R | H4 RECEPTORS | 1ST POTENT | allergy | sleep/wake | neuronal diseases | NEUROPATHIC PAIN | ANTIINFLAMMATORY PROPERTIES | arthritis | cancer | cognitive impairment | drug target
epilepsy | RHEUMATOID-ARTHRITIS | histamine | attention deficit hyperactivity disorder | H3R | MAST-CELLS | schizophrenia | INVERSE AGONISTS | inflammation | H-3-RECEPTOR LIGANDS | PHARMACOLOGY & PHARMACY | autoimmune disorders | pain | SYNOVIAL TISSUE | BRAIN HISTAMINE | H4R | H4 RECEPTORS | 1ST POTENT | allergy | sleep/wake | neuronal diseases | NEUROPATHIC PAIN | ANTIINFLAMMATORY PROPERTIES | arthritis | cancer | cognitive impairment | drug target
Journal Article
JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0022-2623, 04/2008, Volume 51, Issue 8, pp. 2457 - 2467
Using a previously reported flexible alignment model we have designed, synthesized, and evaluated a series of compounds at the human histamine H-4 receptor...
CELLS | POTENT | CHEMISTRY, MEDICINAL | INDOLE | CLONING | HUMAN HISTAMINE-RECEPTOR | PHARMACOLOGICAL CHARACTERIZATION | INFLAMMATION | BENZIMIDAZOLE | ANTAGONISTS | EXPRESSION
CELLS | POTENT | CHEMISTRY, MEDICINAL | INDOLE | CLONING | HUMAN HISTAMINE-RECEPTOR | PHARMACOLOGICAL CHARACTERIZATION | INFLAMMATION | BENZIMIDAZOLE | ANTAGONISTS | EXPRESSION
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 05/2009, Volume 157, Issue 1, pp. 14 - 23
The elucidation of the human genome has had a major impact on histamine receptor research. The identification of the human H-4 receptor by several groups has...
Heterogeneity | Signal transduction | receptor | Species difference | Histamine h | Isoforms | Biochemistry | Molecular pharmacology | Selective agonists and antagonists | signal transduction | CRYSTAL-STRUCTURE | molecular pharmacology | isoforms | AGONIST BINDING | N-GLYCOSYLATION | H-4-RECEPTOR AGONIST | SPLICE VARIANTS | heterogeneity | MEDIATES CHEMOTAXIS | species difference | H4 RECEPTOR | HUMAN EOSINOPHILS | PROTEIN-COUPLED RECEPTOR | FUNCTIONAL EXPRESSION | biochemistry | selective agonists and antagonists | PHARMACOLOGY & PHARMACY | histamine H-4 receptor
Heterogeneity | Signal transduction | receptor | Species difference | Histamine h | Isoforms | Biochemistry | Molecular pharmacology | Selective agonists and antagonists | signal transduction | CRYSTAL-STRUCTURE | molecular pharmacology | isoforms | AGONIST BINDING | N-GLYCOSYLATION | H-4-RECEPTOR AGONIST | SPLICE VARIANTS | heterogeneity | MEDIATES CHEMOTAXIS | species difference | H4 RECEPTOR | HUMAN EOSINOPHILS | PROTEIN-COUPLED RECEPTOR | FUNCTIONAL EXPRESSION | biochemistry | selective agonists and antagonists | PHARMACOLOGY & PHARMACY | histamine H-4 receptor
Journal Article
BIOCHEMICAL PHARMACOLOGY, ISSN 0006-2952, 11/2015, Volume 98, Issue 1, pp. 102 - 109
Millions of people worldwide are suffering from inflammatory bowel disease (IBD), which severely affects patients' life qualities and even life expectancies....
Inflammatory bowel diseases | ACTIVATION | Cytokines | MAST-CELLS | ULCERATIVE-COLITIS | AIRWAY INFLAMMATION | CD4(+) T-CELLS | KNOCKOUT MICE | H4 RECEPTOR | Experimental colitis | Histamine | Histamine H-4 receptor | INFLAMMATORY-BOWEL-DISEASE | MODELS | PHARMACOLOGY & PHARMACY | SEX-DIFFERENCES
Inflammatory bowel diseases | ACTIVATION | Cytokines | MAST-CELLS | ULCERATIVE-COLITIS | AIRWAY INFLAMMATION | CD4(+) T-CELLS | KNOCKOUT MICE | H4 RECEPTOR | Experimental colitis | Histamine | Histamine H-4 receptor | INFLAMMATORY-BOWEL-DISEASE | MODELS | PHARMACOLOGY & PHARMACY | SEX-DIFFERENCES
Journal Article
BIOCHEMICAL PHARMACOLOGY, ISSN 0006-2952, 03/2016, Volume 103, pp. 74 - 84
The human histamine H-4 receptor (H4R) is a G alpha(i/o)-coupled receptor which is mainly expressed on hematopoietic cells. Accordingly, the receptor is...
HUMAN DENDRITIC CELLS | EOL-1 CELLS | Inflammation | Macrophages | HUMAN MONOCYTES | Monocytes | HUMAN EOSINOPHILS | PHARMACOLOGY & PHARMACY | Histamine receptor | DIFFERENTIATION | HISTONE DEACETYLASE INHIBITORS | UP-REGULATION | T-CELLS | Eosinophils
HUMAN DENDRITIC CELLS | EOL-1 CELLS | Inflammation | Macrophages | HUMAN MONOCYTES | Monocytes | HUMAN EOSINOPHILS | PHARMACOLOGY & PHARMACY | Histamine receptor | DIFFERENTIATION | HISTONE DEACETYLASE INHIBITORS | UP-REGULATION | T-CELLS | Eosinophils
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 05/2009, Volume 157, Issue 1, pp. 55 - 63
The histamine H-4 receptor is the most recently identified of the G protein-coupled histamine receptor family and binds several neuroactive drugs, including...
Human | Brain | receptor | Mouse | Histamine h | Neurons | JNJ 10191584 | Hyperpolarization | CORTEX IN-VITRO | CELLS | HUMAN BRAIN | RAT | PHARMACOLOGICAL CHARACTERIZATION | FRONTAL-CORTEX | 1ST POTENT | brain | neurons | SPLICE VARIANTS | mouse | PHARMACOLOGY & PHARMACY | histamine H-4 receptor | hyperpolarization | MOLECULAR-CLONING | ANTAGONISTS | human
Human | Brain | receptor | Mouse | Histamine h | Neurons | JNJ 10191584 | Hyperpolarization | CORTEX IN-VITRO | CELLS | HUMAN BRAIN | RAT | PHARMACOLOGICAL CHARACTERIZATION | FRONTAL-CORTEX | 1ST POTENT | brain | neurons | SPLICE VARIANTS | mouse | PHARMACOLOGY & PHARMACY | histamine H-4 receptor | hyperpolarization | MOLECULAR-CLONING | ANTAGONISTS | human
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 02/2015, Volume 25, Issue 4, pp. 956 - 959
Previously disclosed H-4 receptor modulators, the triamino substituted pyridines and pyrimidines, contain a free primary amino (-NH2) group. In this Letter we...
CHEMISTRY, MEDICINAL | Pyridine | LIGANDS | Pyridazine | CHEMISTRY, ORGANIC | Antagonists | Histamine H-4 | Pyrimidine
CHEMISTRY, MEDICINAL | Pyridine | LIGANDS | Pyridazine | CHEMISTRY, ORGANIC | Antagonists | Histamine H-4 | Pyrimidine
Journal Article
EXPERIMENTAL DERMATOLOGY, ISSN 0906-6705, 01/2009, Volume 18, Issue 1, pp. 57 - 63
Effects of the histamine H-4 receptor antagonist JNJ 7777120 (1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine) were tested in two models of allergic...
pruritus | ALLERGIC CONTACT-DERMATITIS | AWD 12-281 | HUMAN SKIN | PHOSPHODIESTERASE-4 INHIBITOR | 1ST POTENT | JNJ 7777120 | MEDIATES CHEMOTAXIS | DERMATOLOGY | DENDRITIC CELL-FUNCTION | allergic dermatitis | ELICITATION PHASE | histamine H-4 receptor | MICE
pruritus | ALLERGIC CONTACT-DERMATITIS | AWD 12-281 | HUMAN SKIN | PHOSPHODIESTERASE-4 INHIBITOR | 1ST POTENT | JNJ 7777120 | MEDIATES CHEMOTAXIS | DERMATOLOGY | DENDRITIC CELL-FUNCTION | allergic dermatitis | ELICITATION PHASE | histamine H-4 receptor | MICE
Journal Article
Bioorganic and Medicinal Chemistry, ISSN 0968-0896, 04/2019, Volume 27, Issue 7, pp. 1254 - 1262
This study focuses on the design, synthesis, molecular modeling and biological evaluation of a novel group of alkyl-1,3,5-triazinyl-methylpiperazines. New...
ligands | Docking | Pain | receptors | 1,3,5-Triazine | Histamine H | ACTIVATION | CHEMISTRY, MEDICINAL | Histamine H-4 ligands | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | Histamine H-4 receptors | H-4-RECEPTOR | DISCOVERY | H4 RECEPTOR | NEUROPATHIC PAIN | JNJ7777120 | MODELS
ligands | Docking | Pain | receptors | 1,3,5-Triazine | Histamine H | ACTIVATION | CHEMISTRY, MEDICINAL | Histamine H-4 ligands | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | Histamine H-4 receptors | H-4-RECEPTOR | DISCOVERY | H4 RECEPTOR | NEUROPATHIC PAIN | JNJ7777120 | MODELS
Journal Article
Pain, ISSN 0304-3959, 2015, Volume 156, Issue 12, pp. 2492 - 2504
Histamine plays a complex role in pain modulation with opposite roles in nociception for histamine receptor subtypes 1, 2, and 3. The histamine H-4 receptor...
Histamine H 4 receptors | P38 | JNK | Central nervous system | ERK | Neuropathic pain | MECHANICAL ALLODYNIA | PROTEIN-KINASE | MAST-CELLS | Histamine H-4 receptors | RAT MODELS | NEUROSCIENCES | CLINICAL NEUROLOGY | H4 RECEPTOR | INFLAMMATION | SPINAL NERVE LIGATION | TERMINAL KINASE JNK | NEURONS | ANESTHESIOLOGY | MOLECULAR-CLONING
Histamine H 4 receptors | P38 | JNK | Central nervous system | ERK | Neuropathic pain | MECHANICAL ALLODYNIA | PROTEIN-KINASE | MAST-CELLS | Histamine H-4 receptors | RAT MODELS | NEUROSCIENCES | CLINICAL NEUROLOGY | H4 RECEPTOR | INFLAMMATION | SPINAL NERVE LIGATION | TERMINAL KINASE JNK | NEURONS | ANESTHESIOLOGY | MOLECULAR-CLONING
Journal Article
FRONTIERS IN BIOSCIENCE-LANDMARK, ISSN 1093-9946, 01/2016, Volume 21, pp. 597 - 619
First cloned in 2000, the human Histamine H-4 Receptor (hH(4)R) is the last member of the histamine receptors family discovered so far, it belongs to the GPCR...
3D-structure prediction | RESOLUTION CRYSTAL-STRUCTURE | H4R - H-4 receptor | BIOCHEMISTRY & MOLECULAR BIOLOGY | PROTEIN-COUPLED RECEPTORS | Review | Drug Discovery | MUSCARINIC ACETYLCHOLINE-RECEPTOR | CELL BIOLOGY | HISTAMINE H4 RECEPTOR | DOPAMINE D2 RECEPTOR | homology modeling | LIGAND-BINDING MODES | G-protein coupled receptors (GPCRs) | MEMBRANE-PROTEINS | HOMOLOGY MODEL | MOLECULAR-MECHANISMS
3D-structure prediction | RESOLUTION CRYSTAL-STRUCTURE | H4R - H-4 receptor | BIOCHEMISTRY & MOLECULAR BIOLOGY | PROTEIN-COUPLED RECEPTORS | Review | Drug Discovery | MUSCARINIC ACETYLCHOLINE-RECEPTOR | CELL BIOLOGY | HISTAMINE H4 RECEPTOR | DOPAMINE D2 RECEPTOR | homology modeling | LIGAND-BINDING MODES | G-protein coupled receptors (GPCRs) | MEMBRANE-PROTEINS | HOMOLOGY MODEL | MOLECULAR-MECHANISMS
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 10/2015, Volume 103, pp. 238 - 251
Within the constantly growing number of histamine H 4 (H 4 R) receptor ligands there is a large group of azine derivatives. A series of novel compounds in the...
4-Methylpiperazines | Histamine H4 receptor | 1,3,5-Triazin-2-amines | Anti-inflammatory properties | CHEMISTRY, MEDICINAL | ANTAGONIST | ANTIHISTAMINES | PHARMACOLOGICAL CHARACTERIZATION | NEUROBLASTOMA | INFLAMMATORY DISORDERS | Histamine H-4 receptor | POTENT | ANTIINFLAMMATORY PROPERTIES | CLONING | INHIBITOR | DERIVATIVES
4-Methylpiperazines | Histamine H4 receptor | 1,3,5-Triazin-2-amines | Anti-inflammatory properties | CHEMISTRY, MEDICINAL | ANTAGONIST | ANTIHISTAMINES | PHARMACOLOGICAL CHARACTERIZATION | NEUROBLASTOMA | INFLAMMATORY DISORDERS | Histamine H-4 receptor | POTENT | ANTIINFLAMMATORY PROPERTIES | CLONING | INHIBITOR | DERIVATIVES
Journal Article
20.
EXPERIMENTAL AUTOIMMUNE MYOCARDITIS IN RATS AND THERAPEUTIC HISTAMINE H-1 - H-4 RECEPTOR INHIBITION
JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY, ISSN 0867-5910, 12/2018, Volume 69, Issue 6, pp. 889 - 900
Myocarditis, a life threatening disease, is still not adequately treated. Histamine plays an important role in physiology and pathophysiology of cardiovascular...
STANDARDIZATION | ACTIVATION | PHYSIOLOGY | HEART-FAILURE | experimental autoimmune myocarditis | histamine receptors' antagonists | MEDIATES CHEMOTAXIS | IMMUNE | INFLAMMATION | PHARMACOLOGY | angiotensin converting enzyme inhibitor | QUINAPRIL | EXPRESSION | PROGRESSION | dilated cardiomyopathy
STANDARDIZATION | ACTIVATION | PHYSIOLOGY | HEART-FAILURE | experimental autoimmune myocarditis | histamine receptors' antagonists | MEDIATES CHEMOTAXIS | IMMUNE | INFLAMMATION | PHARMACOLOGY | angiotensin converting enzyme inhibitor | QUINAPRIL | EXPRESSION | PROGRESSION | dilated cardiomyopathy
Journal Article
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