General Information of Drug (ID: DM4R6UV)

Drug Name
BRADYKININ Drug Info
Synonyms
BRADYKININ; Kallidin I; 58-82-2; L-Bradykinin; Synthetic bradykinin; Bradykinin (synthetic); Callidin I; UNII-S8TIM42R2W; Kallidin 9; BRS 640; PRS 640; S8TIM42R2W; CHEBI:3165; CHEMBL406291; Bradykinin, Lysyl; BK; Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg; EINECS 200-398-8; L-arginyl-L-prolyl-L-prolylglycyl-L-phenylalanyl-L-seryl-L-prolyl-L-phenylalanyl-L-arginine
Cross-matching ID
PubChem CID
439201
ChEBI ID
CHEBI:3165
CAS Number
CAS 58-82-2
TTD Drug ID
DM4R6UV
INTEDE Drug ID
DR1812

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Icatibant DMQPTOZ Hereditary angioedema 4A00.14 Approved [13]
Fasitibant chloride DM563NC Osteoarthritis FA00-FA05 Phase 2 [14]
DELTIBANT DM5CB8U Sepsis 1G40-1G41 Phase 2 [15]
Anatibant DMG7IEN Traumatic brain injury NA07.Z Phase 2 [16]
DM199 DM0157T Cerebral ischemia 8B11 Phase 2 [17]
NPC-567 DMAVZ1F Rhinitis FA20 Discontinued in Phase 2 [18]
Labradimil DMSFL76 Brain cancer 2A00 Discontinued in Phase 2 [19]
NPC-17731 DMGVIZY Asthma CA23 Terminated [20]
JSM-10292 DMU5TGC Pain MG30-MG3Z Terminated [21]
CP-0597 DMS23JX Asthma CA23 Terminated [22]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Angiotensin-(1-7) DM76GZ0 Sarcoma 2A60-2C35 Phase 3 [23]
Drug(s) Metabolized By Carboxypeptidase M (CPM)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Epidermal growth factor DMVONE6 Vulnerary ND56.Z Approved [24]
Drug(s) Metabolized By Prolyl endopeptidase (PREP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gonadorelin DMAQ469 Amenorrhea GA20.0 Approved [25]
Drug(s) Metabolized By Thimet oligopeptidase (THOP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gonadorelin DMAQ469 Amenorrhea GA20.0 Approved [26]
Drug(s) Affected By Nitric oxide synthase 3 (NOS3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [27]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [28]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [29]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [30]
Methotrexate DM2TEOL Anterior urethra cancer Approved [31]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [32]
Quercetin DM3NC4M Obesity 5B81 Approved [33]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [34]
Fructose DM43AN2 Vomiting MD90 Approved [35]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [36]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
B2 bradykinin receptor (BDKRB2) TTGY8IW BKRB2_HUMAN Inhibitor [1]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cathepsin K (CTSK) DEG3S8C CATK_HUMAN Substrate [2]
Angiotensin-converting enzyme 2 (ACE2) DEGPI81 ACE2_HUMAN Substrate [3]
Arginine carboxypeptidase (CPN1) DEPWYLT CBPN_HUMAN Substrate [4]
Soluble aminopeptidase P (sAmp) DE8E6X9 XPP1_HUMAN Substrate [5]
Carboxypeptidase M (CPM) DE1TNRG CBPM_HUMAN Substrate [6]
Cathepsin H (CTSH) DEHEZPI CATH_HUMAN Substrate [7]
Dipeptidyl peptidase II (DPP7) DEIORCK DPP2_HUMAN Substrate [8]
PABA peptide hydrolase (MEP1B) DEKBXUC MEP1B_HUMAN Substrate [9]
Prolyl endopeptidase (PREP) DEVSCNZ PPCE_HUMAN Substrate [10]
Thimet oligopeptidase (THOP1) DE95LJC THOP1_HUMAN Substrate [11]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Nitric oxide synthase 3 (NOS3) OTLDT7NR NOS3_HUMAN Gene/Protein Processing [12]

References

1 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.
2 A cysteine-type carboxypeptidase, cathepsin X, generates peptide receptor agonists. Int Immunopharmacol. 2010 Jan;10(1):134-9.
3 Nunn's Applied Respiratory Physiology (Eighth Edition). Chapter 11 - Nonrespiratory Functions of the Lung.2017, Pages 203-214.e2
4 Regulation of chemerin bioactivity by plasma carboxypeptidase N, carboxypeptidase B (activated thrombin-activable fibrinolysis inhibitor), and platelets. J Biol Chem. 2009 Jan 9;284(2):751-8.
5 Cloning, expression, and characterization of human cytosolic aminopeptidase P: a single manganese(II)-dependent enzyme. Biochemistry. 2000 Dec 12;39(49):15121-8.
6 Interactions between carboxypeptidase M and kinin B1 receptor in endothelial cells. Inflamm Res. 2019 Oct;68(10):845-855.
7 Human brain cathepsin H as a neuropeptide and bradykinin metabolizing enzyme. Peptides. 2003 Dec;24(12):1977-84.
8 Purification of two dipeptidyl aminopeptidases II from rat brain and their action on proline-containing neuropeptides. J Neurochem. 1989 Apr;52(4):1284-93.
9 Human and mouse homo-oligomeric meprin A metalloendopeptidase: substrate and inhibitor specificities. Biol Chem. 2007 Nov;388(11):1163-72.
10 Bradykinin release and inactivation in brain of rats submitted to an experimental model of Alzheimer's disease. Peptides. 2006 Dec;27(12):3363-9.
11 Expression and activity of thimet oligopeptidase (TOP) are modified in the hippocampus of subjects with temporal lobe epilepsy (TLE). Epilepsia. 2014 May;55(5):754-62.
12 Bradykinin stimulation of nitric oxide production is not sufficient for gamma-globin induction. Srp Arh Celok Lek. 2014 Mar-Apr;142(3-4):189-96. doi: 10.2298/sarh1404189c.
13 Bradykinin receptor antagonists--a review of the patent literature 2005-2008. Expert Opin Ther Pat. 2009 Jul;19(7):919-41.
14 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.
15 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.
16 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.
17 Pharmacological effects of recombinant human tissue kallikrein on bradykinin B2 receptors. Pharmacol Res Perspect. 2015 Mar;3(2):e00119.
18 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.
19 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.
20 Antinociceptive profile of the pseudopeptide B2 bradykinin receptor antagonist NPC 18688 in mice. Br J Pharmacol. 1996 Feb;117(3):552-558.
21 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.
22 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.
23 Metabolism of angiotensin-(1-7) by angiotensin-converting enzyme. Hypertension. 1998 Jan;31(1 Pt 2):362-7.
24 Extracellular conversion of epidermal growth factor (EGF) to des-Arg53-EGF by carboxypeptidase M. J Biol Chem. 1995 Jul 21;270(29):17154-8.
25 Ion-exchange chromatography: basic principles and application to the partial purification of soluble mammalian prolyl oligopeptidase. Methods Mol Biol. 2011;681:215-28.
26 Sleep deprivation changes thimet oligopeptidase (THOP1) expression and activity in rat brain. Heliyon. 2019 Nov 26;5(11):e02896.
27 Protective effects of S-carvedilol on doxorubicin-induced damages to human umbilical vein endothelial cells and rats. J Appl Toxicol. 2019 Aug;39(8):1233-1244. doi: 10.1002/jat.3809. Epub 2019 May 7.
28 Oxidative stress in kidney transplant patients with calcineurin inhibitor-induced hypertension: effect of ramipril. J Cardiovasc Pharmacol. 2002 Oct;40(4):625-31.
29 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
30 Hydrogen peroxide decreases endothelial nitric oxide synthase promoter activity through the inhibition of Sp1 activity. DNA Cell Biol. 2009 Mar;28(3):119-29.
31 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
32 Simvastatin inhibits cigarette smoking-induced emphysema and pulmonary hypertension in rat lungs. Am J Respir Crit Care Med. 2005 Oct 15;172(8):987-93. doi: 10.1164/rccm.200501-041OC. Epub 2005 Jul 7.
33 A blend of polyphenolic compounds explains the stimulatory effect of red wine on human endothelial NO synthase. Nitric Oxide. 2005 Mar;12(2):97-104.
34 The thiazolidinedione drug troglitazone up-regulates nitric oxide synthase expression in vascular endothelial cells. J Diabetes Complications. 2006 Sep-Oct;20(5):336-42.
35 Fructose induces the inflammatory molecule ICAM-1 in endothelial cells. J Am Soc Nephrol. 2008 Sep;19(9):1712-20.
36 Upregulation of nitric oxide production in vascular endothelial cells by all-trans retinoic acid through the phosphoinositide 3-kinase/Akt pathway. Circulation. 2005 Aug 2;112(5):727-36. doi: 10.1161/CIRCULATIONAHA.104.500959. Epub 2005 Jul 25.