Therapeutic Targets Database
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TTD Target ID: TTDC00111

Target Information
NameB2 bradykinin receptor    
Type of targetClinical trial target    
SynonymsB2R    
BK B(2) receptor    
BK-2 receptor    
Bradykinin B2 receptor    
DiseaseAlzheimer's disease
[ICD9: 331.0   ICD10: G30]
[1]
Analgesics
[ICD9: 338   ICD10: R52]
[2]
Arthritis
[ICD9: 710-719   ICD10: M00-M25]
[1]
Asthma
[ICD9: 493   ICD10: J45]
[1]
Brain Cancer
[ICD9: 191   ICD10: C71]
[3][4]
Cardiac hypertrophy
[ICD9: 429.3   ICD10: I51.7]
[1]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[1]
Cerebral edema
[ICD9: 348.5   ICD10: G93.6]
[1]
Chronic rhinitis
[ICD9: 472.0, 477   ICD10: J00, J30, J31.0]
[1]
Colitis
[ICD9: 556.9   ICD10: K50-K52]
[1]
Diabetic disorders
[ICD9: 250   ICD10: E08-E13]
[1]
Diabetic nephropathy
[ICD9: 250.4   ICD10: E10.2, E11.2, E13.2]
[5]
Hepatorenal syndrome[1]
Hereditary Angioedema (HAE)
[ICD9: 277.6   ICD10: D84.1]
[6][7][8]
Hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[1]
Liver Disease
[ICD9: 570-574   ICD10: K70-K77]
[6][7][8]
Lung cancer
[ICD9: 162   ICD10: C33-C34]
[1]
Myocardial infarction
[ICD9: 410   ICD10: I21, I22]
[1]
Pancreatitis
[ICD9: 577.0-577.1   ICD10: K85, K86.0K86.1]
[1]
Pediatric[3][4]
Restenosis[1]
Sepsis
[ICD9: 995.91   ICD10: A40, A41]
[1]
Tissue injury[1]
Traumatic brain injuries
[ICD9: 800, 801, 803, 804, 850-854   ICD10: S06]
[9][10]
Visceral pain
[ICD9: 338,780   ICD10: R52, G89]
[2]
Drug(s)IcatibantPhase III, Positive phase III resultsHereditary Angioedema (HAE)[6][7][8]
IcatibantPhase IIa completedLiver Disease[6][7][8]
AnatibantPhase IITraumatic Brain Injuries[9][10]
LabradimilDiscontinuedBrain Cancer, Pediatric[3][4]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Complement and coagulation cascades
Neuroactive ligand-receptor interaction
Regulation of actin cytoskeleton
UniProt IDP30411
FunctionReceptor for bradykinin. It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system.    
SequenceMFSPWKISMFLSVREDSVPTTASFSADMLNVTLQGPTLNGTFAQSKCPQVEWLGWLNTIQ PPFLWVLFVLATLENIFVLSVFCLHKSSCTVAEIYLGNLAAADLILACGLPFWAITISNN FDWLFGETLCRVVNAIISMNLYSSICFLMLVSIDRYLALVKTMSMGRMRGVRWAKLYSLV IWGCTLLLSSPMLVFRTMKEYSDEGHNVTACVISYPSLIWEVFTNMLLNVVGFLLPLSVI TFCTMQIMQVLRNNEMQKFKEIQTERRATVLVLVVLLLFIICWLPFQISTFLDTLHRLGI LSSCQDERIIDVITQIASFMAYSNSCLNPLVYVIVGKRFRKKSWEVYQGVCQKGGCRSEP IQMENSMGTLRTSISVERQIHKLQDWAGSRQ
Related US Patent6,479,515
6,500,831
6,531,480
Target ValidationClick to Find Target Validation Information.    
Inhibitor (D)Arg-Arg-Pro-Hyp-Gly-Phe-Ser-[11]
(D)Arg-Arg-Pro-Hyp-Gly-Thi-Cys-[11]
(D)Arg-Arg-Pro-Hyp-Gly-Thi-Ser-[11]
(D)Arg-Arg-Pro-Hyp-Gly-Thi-Ser-[11]
BRADYKININ[12]
FR-173657[13]
H-DArg-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH (JMV1638)[12]
H-DArg-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH (JMV1431)[12]
H-Lys-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH (JMV1645)[12]
H-Lys-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH (JMV1669)[12]
NPC-567[14]
Quinapril analogue[15]
AgonistLabradimil[3][4]
AntagonistAnatibant[9][10]
Icatibant[6][7][8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Bradykinin B2 receptor as a potential therapeutic target. Drug News Perspect. 2000 May;13(4):213-25. To Reference
Ref 2Kallikrein-kinin system in acute pancreatitis: potential of B(2)-bradykinin antagonists and kallikrein inhibitors. Pharmacology. 2000 Apr;60(3):113-20. To Reference
Ref 3Metabolically stable bradykinin B2 receptor agonists enhance transvascular drug delivery into malignant brain tumors by increasing drug half-life. J Transl Med. 2009 May 13;7:33. To Reference
Ref 4Bradykinin receptor agonist facilitates low-dose cyclosporine-A protection against 6-hydroxydopamine neurotoxicity. Brain Res. 2002 Nov 29;956(2):211-20. To Reference
Ref 5Induction of B1 receptors in streptozotocin diabetic rats: possible involvement in the control of hyperglycemia-induced glomerular Erk 1 and 2 phosphorylation. Can J Physiol Pharmacol. 2002 Apr;80(4):328-33. To Reference
Ref 6Bradykinin receptor antagonists--a review of the patent literature 2005-2008. Expert Opin Ther Pat. 2009 Jul;19(7):919-41. To Reference
Ref 7Pharmacological characterization of the bradykinin B2 receptor antagonist MEN16132 in rat in vitro bioassays. Eur J Pharmacol. 2009 Aug 1;615(1-3):10-6. Epub 2009 May 13. To Reference
Ref 8Bradykinin in the heart: friend or foe? Circulation. 1999 Dec 7;100(23):2305-7. To Reference
Ref 9Inhibition of bradykinin B2 receptors before, not after onset of experimental subarachnoid hemorrhage prevents brain edema formation and improves functional outcome. Crit Care Med. 2009 Jul;37(7):2228-34. To Reference
Ref 10Anatibant, a selective non-peptide bradykinin B2 receptor antagonist, reduces intracranial hypertension and histopathological damage after experimental traumatic brain injury. Neurosci Lett. 2009 Apr 24;454(2):115-7. Epub 2009 Feb 11. To Reference
Ref 11J Med Chem. 1991 Mar;34(3):1230-3.Design and conformational analysis of several highly potent bradykinin receptor antagonists. To Reference
Ref 12J Med Chem. 2000 Jun 15;43(12):2382-6.Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists. To Reference
Ref 13J Med Chem. 2009 Jul 23;52(14):4370-9.Novel small molecule bradykinin B2 receptor antagonists. To Reference
Ref 14J Med Chem. 2008 Nov 27;51(22):7094-8.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. To Reference
Ref 15Bioorg. Med. Chem. Lett. 5(4):367-370 (1995) To Reference



 

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