The histamine receptors are a class of G-protein coupled receptors with histamine as their endogenous ligand.[1] There are four known histamine receptors: [edit] Comparison There are several splice variants of H3 present in various species. Though all of the receptors are 7-transmembrane g protein coupled receptors, H1 and H2 are quite different from H3 and H4 in their activities. H1 causes an increase in PIP2 hydrolysis, H2 stimulates gastric acid secretion, and H3 mediates feedback inhibition of histamine. [edit] References - ^ Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacol. Rev. 49 (3): 253–78. PMID 9311023. http://pharmrev.aspetjournals.org/cgi/content/abstract/49/3/253.
- ^ Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP (2003). "Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells". J. Pharmacol. Exp. Ther. 305 (3): 1212–21. doi:10.1124/jpet.102.046581. PMID 12626656.
[edit] External links | Transmembrane receptor: G protein-coupled receptors | | | Class A: Rhodopsin like | | | | | | | | | | | | | | | GPR ( 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182) | | | | Adenosine ( A1, A2A, A2B, A3) · P2Y ( 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14) | | | | | | | Other | Acetylcholine ( M1, M2, M3, M4, M5) · Adrenomedullin · Anaphylatoxin ( C3a, C5a) · Angiotensin ( 1, 2) · Apelin · Bile acid · Bombesin ( BRS3, GRPR, NMBR) · Bradykinin ( B1, B2) · Cannabinoid ( CB1, CB2) · Chemokine · Cholecystokinin ( A, B) · Dopamine ( D1, D2, D3, D4, D5) · EBI2 · Endothelin ( A, B) · Estrogen · Formyl peptide ( 1, 2, 3) · Free fatty acid ( 1, 2, 3, 4) · FSH · Galanin ( 1, 2, 3) · Gonadotropin-releasing hormone ( 1, 2) · GHB receptor · Ghrelin · Histamine ( H1, H2, H3, H4) · Kisspeptin · Luteinizing hormone/choriogonadotropin · lysophosphatidic acid ( 1, 2, 3) · Lysophospholipid ( 1, 2, 3, 4, 5, 6, 7, 8) · MAS ( 1, 1L, D, E, F, G, X1, X2, X3, X4) · Melanocortin ( 1, 2, 3, 4, 5) · MCHR ( 1, 2) · Melatonin ( 1A, 1B, 1C) · Niacin ( 1, 2) · Motilin · Opioid ( Delta, Kappa, Mu, Nociceptin & Zeta, but not Sigma) · Olfactory · Opsin ( 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) · Orexin ( 1, 2) · Oxytocin · Oxoglutarate · PAF · Prokineticin ( 1, 2) · Prolactin-releasing peptide · Protease-activated ( 1, 2, 3, 4) · Relaxin ( 1, 2, 3, 4) · Somatostatin ( 1, 2, 3, 4, 5) · Sphingosine-1-phosphate ( 1, 2, 3, 4, 5) · SREB · Succinate · TAAR ( 1, 2, 3, 5, 6, 8, 9) · Tachykinin ( 1, 2, 3) · Thyrotropin · Thyrotropin-releasing hormone · Urotensin-II · Vasopressin ( 1A, 1B, 2) | | | | Class B: Secretin like | | | GPR ( 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157) | | | Other | Brain-specific angiogenesis inhibitor ( 1, 2, 3) · Cadherin ( 1, 2, 3) · Calcitonin · CALCRL · CD97 · Corticotropin-releasing hormone ( 1, 2) · EMR ( 1, 2, 3) · Glucagon ( GR, GIPR, GLP1R, GLP2R) · Growth hormone releasing hormone · PACAPR1 · GPR · Latrophilin ( 1, 2, 3, ELTD1) · Methuselah-like proteins · Parathyroid hormone ( 1, 2) · Secretin · Vasoactive intestinal peptide ( 1, 2) | | | Class C: Metabotropic
glutamate / pheromone | | | TAS1R ( 1, 2, 3) · TAS2R ( 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50) | | | Other | Calcium-sensing receptor · GABA B ( 1, 2) · Glutamate receptor ( Metabotropic glutamate ( 1, 2, 3, 4, 5, 6, 7, 8)) · GPRC6A · GPR ( 156, 158, 179) · RAIG ( 1, 2, 3, 4) | | | | Frizzled / Smoothened | | | | Histaminergics | | Receptor
Ligands | | | Agonists: 2-Pyridylethylamine • Betahistine • Histamine • HTMT • UR-AK49 Antagonists: 1st Generation: Alimemazine • Azatadine • Bamipine • Bepotastine • Bromazine • Brompheniramine • Buclizine • Carbinoxamine • Chlorcyclizine • Chloropyramine • Chlorothen • Chlorpheniramine • Chlorphenoxamine • Cinnarizine • Clemastine • Clobenzepam • Clocinizine • Cyclizine • Cyproheptadine • Dacemazine • Deptropine • Dexbrompheniramine • Dexchlorpheniramine • Dimetindene • Diphenhydramine • Diphenylpyraline • Doxylamine • Embramine • Etymemazine • Histapyrrodine • Hydroxyethylpromethazine • Hydroxyzine • Iproheptine • Isopromethazine • Isothipendyl • Meclizine • Mepyramine (Pyrilamine) • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • p-Methyldiphenhydramine • Pheniramine • Phenyltoloxamine • Promethazine • Pyrrobutamine • Setastine • Talastine • Thenalidine • Thenyldiamine • Thiazinamium • Thonzylamine • Tolpropamine • Tripelennamine • Triprolidine; 2nd Generation: Acrivastine • Antazoline • Astemizole • Azatadine • Azelastine • Bamipine • Cetirizine • Clemizole • Clobenztropine • Deptropine • Dimebon • Ebastine • Emedastine • Epinastine • Ketotifen • Levocabastine • Loratadine • Mebhydrolin • Mizolastine • Olopatadine • Phenindamine • Pimethixene • Pyrrobutamine • Rupatadine • Terfenadine • Thenalidine • Tritoqualine; 3rd Generation: Desloratadine • Fexofenadine • Levocetirizine; Miscellaneous: Tricyclic Antidepressants ( Amitriptyline, Doxepin, Trimipramine, etc) • Tetracyclic Antidepressants ( Mianserin, Mirtazapine, etc) • Serotonin Antagonists and Reuptake Inhibitors ( Trazodone, Nefazodone) • Typical Antipsychotics ( Chlorpromazine, Thioridazine, etc) • Atypical Antipsychotics ( Clozapine, Olanzapine, Quetiapine, etc) | | | | | | | | | | | | | | | Reuptake
Inhibitors | | | Enzyme
Inhibitors | | | | Others | | | |
