| Target
Information |
| Name | Histamine H2 receptor |
| Type of target | Successful target |
| Synonyms | Gastric receptor I |
| H2R |
| Histamine receptor 2 |
| Disease | Epidermal hyperplasia | [1] |
Lasting tachycardia
[ICD9: 427, 785.0 ICD10: I47-I49, R00.0] | [2] |
Peptic ulcer
[ICD9: 531-534 ICD10: K25-K27] | [3] |
| Systemic arterial vasodilation | [4] |
Zollinger-Ellison syndrome
[ICD9: 251.5 ICD10: E16.4] | [5] |
| Drug(s) | Betazole |  | Approved | Test gastric secretory function | [6] |
| Cimetidine | | Approved | Acid-reflux disorders | [1][7][3] |
| Famotidine | | Approved | Peptic ulcer disease | [1][4][8][3][5] |
| Nizatidine | | Approved | Acid-reflux disorders | [9] |
| Ranitidine | | Approved | Peptic ulcer disease | [10][2][3] |
| BioChemical Class | G-protein coupled receptor (rhodopsin family) |
| UniProt ID | P25021 |
| Function | The H2 subclass of histamine receptors mediates gastric acid secretion and also appears to regulate gastrointestinal motility and intestinal secretion., and it plays possible role in regulating cell growth and differentiation. |
| Sequence | MAPNGTASSFCLDSTACKITITVVLAVLILITVAGNVVVCLAVGLNRRLRNLTNCFIVSL
AITDLLLGLLVLPFSAIYQLSCKWSFGKVFCNIYTSLDVMLCTASILNLFMISLDRYCAV
MDPLRYPVLVTPVRVAISLVLIWVISITLSFLSIHLGWNSRNETSKGNHTTSKCKVQVNE
VYGLVDGLVTFYLPLLIMCITYYRIFKVARDQAKRINHISSWKAATIREHKATVTLAAVM
GAFIICWFPYFTAFVYRGLRGDDAINEVLEAIVLWLGYANSALNPILYAALNRDFRTGYQ
QLFCCRLANRNSHKTSLRSNASQLSRTQSREPRQQEEKPLKLQVWSGTEVTAPQGATDR
|
| Related US Patent | 6,274,160 |
| 6,353,005 |
| 6,362,202 |
| 6,548,518 |
| 6,552,045 |
| 6,663,888 |
| Target Validation | Click to Find Target Validation Information. |
| Inhibitor | (+/-)-nantenine | | [11] |
| 4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | | [12] |
| MIANSERIN HYDROCHLORIDE | | [13] |
| VUF-10148 | | [14] |
| WAY-207024 | | [15] |
| Agonist | Dimaprit | | |
| Histamine | | [16] |
| Antagonist | Betazole | | [6] |
| Cimetidine | | [1][7][3] |
| Famotidine | | [1][4][8][3][5] |
| Gaster | | [17][10] |
| Metiamide | | [18] |
| Nizatidine | | [9] |
| Ranitidine | | [10][2][3] |
| Cross References |
3D Structure
Related Literature
On-Line
Medical Dictionary |
| Ref 1 | Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. J Invest Dermatol. 2001 Feb;116(2):261-5. To Reference |
| Ref 2 | Hemodynamic significance of histamine synthesis and histamine H1- and H2-receptor gene expression during endotoxemia. Naunyn Schmiedebergs Arch Pharmacol. 2002 Dec;366(6):513-21. Epub 2002 Oct 29. To Reference |
| Ref 3 | Effect of the H2 histamine receptor antagonist on oxygen metabolism in some morphotic blood elements in patients with ulcer disease. Hepatogastroenterology. 1998 Jan-Feb;45(19):276-80. To Reference |
| Ref 4 | Analysis of Vancomycin in the Hindlimb Vascular Bed of the Rat. Am J Ther. 1996 Oct;3(10):681-687. To Reference |
| Ref 5 | Eur J Clin Invest. 1989 Feb;19(1):1-10.Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H1, H2 and H3 receptor agonists and antagonists. To Reference |
| Ref 6 | Effect of nizatidine and cimetidine on betazole-stimulated gastric secretion of normal subjects: comparison of effects on acid, water, and pepsin. Am J Gastroenterol. 1988 Jan;83(1):32-6. To Reference |
| Ref 7 | Characterization and modulation of antigen-induced effects in isolated rat heart. J Cardiovasc Pharmacol. 1991 Oct;18(4):556-65. To Reference |
| Ref 8 | Blastocyst H(2) receptor is the target for uterine histamine in implantation in the mouse. Development. 2000 Jun;127(12):2643-51. To Reference |
| Ref 9 | Does the use of nizatidine, as a pro-kinetic agent, improve gastric emptying in patients post-oesophagectomy? J Gastrointest Surg. 2009 Mar;13(3):432-7. Epub 2008 Nov 1. To Reference |
| Ref 10 | Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference |
| Ref 11 | Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. To Reference |
| Ref 12 | J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference |
| Ref 13 | J Med Chem. 1983 Aug;26(8):1116-22.Synthesis and biological properties of thiophene ring analogues of mianserin. To Reference |
| Ref 14 | J Med Chem. 2008 Apr 24;51(8):2457-67. Epub 2008 Mar 22.Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. To Reference |
| Ref 15 | J Med Chem. 2009 Apr 9;52(7):2148-52.Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R). To Reference |
| Ref 16 | Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6. To Reference |
| Ref 17 | Afferent signalling from the acid-challenged rat stomach is inhibited and gastric acid elimination is enhanced by lafutidine. BMC Gastroenterol. 2009 Jun 2;9:40. To Reference |
| Ref 18 | Black JW, Duncan WA, Emmett JC, Ganellin CR, Hesselbo T, Parsons ME, Wyllie JH: Metiamide—an orally active histamine H2-receptor antagonist. 1973. Agents Actions. 1994 Dec;43(3-4):91-5; discussion 96. To Reference |
