General Information of DTT (ID: TTGY8IW)

DTT Name B2 bradykinin receptor (BDKRB2) DTT Info
Gene Name BDKRB2

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
1 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Icatibant DMQPTOZ Hereditary angioedema 4A00.14 Approved [1]
------------------------------------------------------------------------------------
5 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Anatibant DMG7IEN Traumatic brain injury NA07.Z Phase 2 [2]
DELTIBANT DM5CB8U Sepsis 1G40-1G41 Phase 2 [3]
DM199 DM0157T Cerebral ischemia 8B11 Phase 2 [4]
Fasitibant chloride DM563NC Osteoarthritis FA00-FA05 Phase 2 [5]
BRADYKININ DM4R6UV N. A. N. A. Phase 1 [6]
------------------------------------------------------------------------------------
7 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Labradimil DMSFL76 Brain cancer 2A00 Discontinued in Phase 2 [7]
NPC-567 DMAVZ1F Rhinitis FA20 Discontinued in Phase 2 [8]
CP-0597 DMS23JX Asthma CA23 Terminated [9]
FR-172357 DMY1LRI Inflammation 1A00-CA43.1 Terminated [10]
FR-173657 DM37OS4 N. A. N. A. Terminated [11]
JSM-10292 DMU5TGC Pain MG30-MG3Z Terminated [12]
NPC-17731 DMGVIZY Asthma CA23 Terminated [13]
------------------------------------------------------------------------------------
⏷ Show the Full List of 7 Discontinued Drug(s)
27 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(D)Arg-Arg-Pro-Hyp-Gly-Phe-Ser-(d)Phe-Phe-Arg DMWE42T Discovery agent N.A. Investigative [14]
(D)Arg-Arg-Pro-Hyp-Gly-Thi-Cys-(D)Phe-Phe-Cys-Arg DMYSE3O Discovery agent N.A. Investigative [14]
(D)Arg-Arg-Pro-Hyp-Gly-Thi-Ser-(D)Tic-Aoc-Arg DMLSJKM Discovery agent N.A. Investigative [14]
(D)Arg-Arg-Pro-Hyp-Gly-Thi-Ser-(D)Tic-Tic-Arg DMP0627 Discovery agent N.A. Investigative [14]
bradyzide DM0DWSR Discovery agent N.A. Investigative [15]
Breceptin DM21ZBU Solid tumour/cancer 2A00-2F9Z Investigative [16]
chroman 28 DMVDB7S Discovery agent N.A. Investigative [17]
FR167344 DM2W5VA Discovery agent N.A. Investigative [18]
FR190997 DM0G4HP Discovery agent N.A. Investigative [19]
FR191413 DM75VHN Discovery agent N.A. Investigative [20]
H-DArg-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH(JMV1638) DM6839G Discovery agent N.A. Investigative [6]
H-Lys-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH(JMV1645) DMDXIS7 Discovery agent N.A. Investigative [6]
H-Lys-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH(JMV1669) DMTGU0L Discovery agent N.A. Investigative [6]
JMV1431 DMAR3M2 Discovery agent N.A. Investigative [6]
kallidin DMRT6OP Discovery agent N.A. Investigative [21]
LF-160335 DMOEQTN Discovery agent N.A. Investigative [22]
Met-Lys-bradykinin DMZBLQD Discovery agent N.A. Investigative [23]
NPC-349 DMU426Z Discovery agent N.A. Investigative [21]
PMID12723943C12 DMR1MCD Discovery agent N.A. Investigative [24]
PMID12812482C11 DMYXDK5 Discovery agent N.A. Investigative [25]
PS020990 DMK6HMS Discovery agent N.A. Investigative [26]
Quinapril analogue DM0BEZS Discovery agent N.A. Investigative [27]
T-kinin DMYGXHK Discovery agent N.A. Investigative [28]
WIN 64338 DMTE0YJ Discovery agent N.A. Investigative [29]
[des-Arg9]bradykinin DMEL0SZ Discovery agent N.A. Investigative [30]
[Leu8,des-Arg9]bradykinin DM3JHRC Discovery agent N.A. Investigative [31]
[Sar,D-Phe8,des-Arg9]bradykinin DMUF7DP Discovery agent N.A. Investigative [28]
------------------------------------------------------------------------------------
⏷ Show the Full List of 27 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Bradykinin receptor antagonists--a review of the patent literature 2005-2008. Expert Opin Ther Pat. 2009 Jul;19(7):919-41.
2 Inhibition 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.
3 CP-0127, a novel potent bradykinin antagonist, increases survival in rat and rabbit models of endotoxin shock. Agents Actions Suppl. 1992;38 ( Pt 3):413-20.
4 Pharmacological effects of recombinant human tissue kallikrein on bradykinin B2 receptors. Pharmacol Res Perspect. 2015 Mar;3(2):e00119.
5 Fasitibant chloride, a kinin B receptor antagonist, and dexamethasone interact to inhibit carrageenan-induced inflammatory arthritis in rats. Br J Pharmacol. 2012 Jun;166(4):1403-10.
6 Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists. J Med Chem. 2000 Jun 15;43(12):2382-6.
7 Metabolically 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.
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... J Med Chem. 2008 Nov 27;51(22):7094-8.
9 CP-0597, a selective bradykinin B2 receptor antagonist, inhibits brain injury in a rat model of reversible middle cerebral artery occlusion. Stroke. 1997 Jul;28(7):1430-6.
10 Characterization of FR 172357, a new non-peptide bradykinin B(2) receptor antagonist, in human, pig and rabbit preparations. Eur J Pharmacol. 1999 Dec 10;386(1):25-31.
11 Novel small molecule bradykinin B2 receptor antagonists. J Med Chem. 2009 Jul 23;52(14):4370-9.
12 Binding characteristics of [3H]-JSM10292: a new cell membrane-permeant non-peptide bradykinin B2 receptor antagonist. Br J Pharmacol. 2012 Oct;167(4):839-53.
13 Antinociceptive profile of the pseudopeptide B2 bradykinin receptor antagonist NPC 18688 in mice. Br J Pharmacol. 1996 Feb;117(3):552-558.
14 Design and conformational analysis of several highly potent bradykinin receptor antagonists. J Med Chem. 1991 Mar;34(3):1230-3.
15 Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia. Br J Pharmacol. 2000 Jan;129(1):77-86.
16 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 42).
17 Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity. J Med Chem. 2007 Feb 22;50(4):607-10.
18 Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657. Mol Pharmacol. 1997 Feb;51(2):171-6.
19 Nonpeptide mimic of bradykinin with long-acting properties at the bradykinin B2 receptor. Mol Pharmacol. 1997 Jul;52(1):16-20.
20 Discovery of the first non-peptide full agonists for the human bradykinin B(2) receptor incorporating 4-(2-picolyloxy)quinoline and 1-(2-picolyl)benzimidazole frameworks. J Med Chem. 2004 May 20;47(11):2853-63.
21 Differential pharmacology of cloned human and mouse B2 bradykinin receptors. Mol Pharmacol. 1994 Jan;45(1):1-8.
22 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
23 Expression cloning of a human B1 bradykinin receptor. J Biol Chem. 1994 Aug 26;269(34):21583-6.
24 Benzodiazepines as potent and selective bradykinin B1 antagonists. J Med Chem. 2003 May 8;46(10):1803-6.
25 Discovery of a potent, non-peptide bradykinin B1 receptor antagonist. J Am Chem Soc. 2003 Jun 25;125(25):7516-7.
26 Small molecule antagonists of the bradykinin B1 receptor. Immunopharmacology. 1999 Sep;43(2-3):169-77.
27 Ace inhibitors as a template for the design of bradykinin B2 receptor antagonists, Bioorg. Med. Chem. Lett. 5(4):367-370 (1995).
28 Molecular characterisation of cloned bradykinin B1 receptors from rat and human. Eur J Pharmacol. 1999 Jun 25;374(3):423-33.
29 Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor. J Med Chem. 1993 Aug 20;36(17):2583-4.
30 Stable expression of human kinin B1 receptor in 293 cells: pharmacological and functional characterization. Br J Pharmacol. 1997 Sep;122(2):393-9.
31 Partial agonists and full antagonists at the human and murine bradykinin B1 receptors. Can J Physiol Pharmacol. 1997 Jun;75(6):735-40.