Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00087

Target Information
NameHistamine H2 receptor    
Type of targetSuccessful target    
SynonymsGastric receptor I    
H2R    
Histamine receptor 2    
DiseaseEpidermal 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)BetazoleApprovedTest gastric secretory function[6]
CimetidineApprovedAcid-reflux disorders[1][7][3]
FamotidineApprovedPeptic ulcer disease[1][4][8][3][5]
NizatidineApprovedAcid-reflux disorders[9]
RanitidineApprovedPeptic ulcer disease[10][2][3]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
UniProt IDP25021
FunctionThe 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.    
SequenceMAPNGTASSFCLDSTACKITITVVLAVLILITVAGNVVVCLAVGLNRRLRNLTNCFIVSL AITDLLLGLLVLPFSAIYQLSCKWSFGKVFCNIYTSLDVMLCTASILNLFMISLDRYCAV MDPLRYPVLVTPVRVAISLVLIWVISITLSFLSIHLGWNSRNETSKGNHTTSKCKVQVNE VYGLVDGLVTFYLPLLIMCITYYRIFKVARDQAKRINHISSWKAATIREHKATVTLAAVM GAFIICWFPYFTAFVYRGLRGDDAINEVLEAIVLWLGYANSALNPILYAALNRDFRTGYQ QLFCCRLANRNSHKTSLRSNASQLSRTQSREPRQQEEKPLKLQVWSGTEVTAPQGATDR
Related US Patent6,274,160
6,353,005
6,362,202
6,548,518
6,552,045
6,663,888
Target ValidationClick 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]
AgonistDimaprit
Histamine[16]
AntagonistBetazole[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 1Histamine 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 2Hemodynamic 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 3Effect 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 4Analysis of Vancomycin in the Hindlimb Vascular Bed of the Rat. Am J Ther. 1996 Oct;3(10):681-687. To Reference
Ref 5Eur 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 6Effect 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 7Characterization and modulation of antigen-induced effects in isolated rat heart. J Cardiovasc Pharmacol. 1991 Oct;18(4):556-65. To Reference
Ref 8Blastocyst H(2) receptor is the target for uterine histamine in implantation in the mouse. Development. 2000 Jun;127(12):2643-51. To Reference
Ref 9Does 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 10Nat 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 11Bioorg 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 12J 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 13J Med Chem. 1983 Aug;26(8):1116-22.Synthesis and biological properties of thiophene ring analogues of mianserin. To Reference
Ref 14J 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 15J 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 16Cloning 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 17Afferent 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 18Black 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



 

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