Preclinical pharmacology, metabolic stability, pharmacokinetics and toxicology of the peptidic kinin B1 receptor antagonist R-954

Peptides

Volumn 52, Issue , 2014, Pages 82-89

  Gobeil Jr , Fernand ^a,b   Sirois, Pierre ^c   Regoli, Domenico ^a  

^a UNIVERSITY OF SHERBROOKE   (Canada)

^b UNIVERSITÉ DE SHERBROOKE   (Canada)

^c LAVAL UNIVERSITY   (Canada)

Author keywords

B1 receptor; Kinins; Peptidic antagonist; Pharmacokinetics; Rats; Toxicology

Indexed keywords

ANGIOTENSIN 2 RECEPTOR; ANTIDIABETIC AGENT; BOMBESIN RECEPTOR; CANNABINOID 1 RECEPTOR; CYTOCHROME P450; KININ B1 RECEPTOR ANTAGONIST; R 954; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ADRENAL GLAND; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BILE; BILIARY EXCRETION; BINDING AFFINITY; BLADDER; BLOOD; BONE MARROW; BRAIN; CIRCULATION; CONTROLLED STUDY; DIABETES MELLITUS; DIASTOLIC BLOOD PRESSURE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SPECIFICITY; DRUG STABILITY; DRUG TOLERABILITY; ENZYME ACTIVITY; ENZYME INHIBITION; EYE; FEMALE; HEART; HEART RATE; IC 50; INJECTION SITE; KIDNEY; LARGE INTESTINE; LIMIT OF DETECTION; LIVER; LIVER CLEARANCE; LUNG; MALE; MEAN ARTERIAL PRESSURE; MOUSE; NONHUMAN; PLASMA CONCENTRATION-TIME CURVE; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; RAT; RECEPTOR BINDING; RETROPERITONEAL FAT; SEX DIFFERENCE; SKELETAL MUSCLE; SKIN; SPINAL CORD; STREPTOZOTOCIN-INDUCED DIABETES MELLITUS; SYSTOLIC BLOOD PRESSURE; TESTIS; TISSUE DISTRIBUTION; TISSUE HOMOGENATE; URINE;

B1 RECEPTOR; KININS; PEPTIDIC ANTAGONIST; PHARMACOKINETICS; RATS; TOXICOLOGY;

ANIMALS; BRADYKININ; DIABETES MELLITUS, EXPERIMENTAL; HUMANS; NEOPLASMS; NERVOUS SYSTEM DISEASES; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; RECEPTOR, BRADYKININ B1;

EID: 84891814053     PISSN: 01969781     EISSN: 18735169     Source Type: Journal    
DOI: 10.1016/j.peptides.2013.12.009     Document Type: Article

References (57)

1. S. Bélanger, V. Bovenzi, J. Côté, W. Neugebauer, M. Amblard, and J. Martinez et al. Structure-activity relationships of novel peptide agonists of the human bradykinin B2 receptor Peptides 30 2009 777 787
2. J.B. Calixto, R. Medeiros, E.S. Fernandes, J. Ferreira, D.A. Cabrini, and M.M. Campos Kinin B1 receptors: key G-protein-coupled receptors and their role in inflammatory and painful processes Br J Pharmacol 143 2004 803 818
3. G. Campanholle, R.G. Landgraf, E. Borducchi, P. Semedo, P.H. Wang, and M.T. Amano et al. Bradykinin inducible receptor is essential to lipopolysaccharide-induced acute lung injury in mice Eur J Pharmacol 634 2010 132 137
4. M.M. Campos, B. Ongali, H. De Souza Buck, J.P. Schanstra, J.P. Girolami, and J.G. Chabot et al. Expression and distribution of kinin B1 receptor in the rat brain and alterations induced by diabetes in the model of streptozotocin Synapse 57 2005 29 37
5. O.L. Catanzaro, D. Dziubecki, P. Obregon, R.R. Rodriguez, and P. Sirois Antidiabetic efficacy of bradykinin antagonist R-954 on glucose tolerance test in diabetic type 1 mice Neuropeptides 44 2010 187 189
6. R. Couture, M. Harrisson, R.M. Vianna, and F. Cloutier Kinin receptors in pain and inflammation Eur J Pharmacol 429 2001 161 176
7. H. De Brito Gariepy, P. Carayon, B. Ferrari, and R. Couture Contribution of the central dopaminergic system in the anti-hypertensive effect of kinin B1 receptor antagonists in two rat models of hypertension Neuropeptides 44 2010 191 198
8. J.P. Dias, S. Talbot, J. Senecal, P. Carayon, and R. Couture Kinin B1 receptor enhances the oxidative stress in a rat model of insulin resistance: outcome in hypertension, allodynia and metabolic complications PLoS ONE 5 2010 e12622
9. G. Drapeau, R. Audet, L. Levesque, D. Godin, and F. Marceau Development and in vivo evaluation of metabolically resistant antagonists of B1 receptors for kinins J Pharmacol Exp Ther 266 1993 192 199
10. J. Eric, B.H. Gabra, and P. Sirois Implication of the bradykinin receptors in antigen-induced pulmonary inflammation in mice Br J Pharmacol 138 2003 1589 1597
11. P.D. Fernandes, M. Gomes Nde, and P. Sirois The bradykinin B1 receptor antagonist R-954 inhibits Ehrlich tumor growth in rodents Peptides 32 2011 1849 1854
12. B.H. Gabra, N. Berthiaume, P. Sirois, F. Nantel, and B. Battistini The kinin system mediates hyperalgesia through the inducible bradykinin B1 receptor subtype: evidence in various experimental animal models of type 1 and type 2 diabetic neuropathy Biol Chem 387 2006 127 143
13. B.H. Gabra, V.F. Merino, M. Bader, J.B. Pesquero, and P. Sirois Absence of diabetic hyperalgesia in bradykinin B1 receptor-knockout mice Regul Pept 127 2005 245 248
14. B.H. Gabra, and P. Sirois Role of bradykinin B(1) receptors in diabetes-induced hyperalgesia in streptozotocin-treated mice Eur J Pharmacol 457 2002 115 124
15. B.H. Gabra, and P. Sirois Beneficial effect of chronic treatment with the selective bradykinin B1 receptor antagonists, R-715 and R-954, in attenuating streptozotocin-diabetic thermal hyperalgesia in mice Peptides 24 2003 1131 1139
16. B.H. Gabra, and P. Sirois Kinin B1 receptor antagonists inhibit diabetes-induced hyperalgesia in mice Neuropeptides 37 2003 36 44
17. B.H. Gabra, and P. Sirois Pathways for the bradykinin B1 receptor-mediated diabetic hyperalgesia in mice Inflamm Res 53 2004 653 657
18. B.H. Gabra, and P. Sirois Hyperalgesia in non-obese diabetic (NOD) mice: a role for the inducible bradykinin B1 receptor Eur J Pharmacol 514 2005 61 67
19. R. Gama Landgraf, S. Jancar, A.A. Steil, and P. Sirois Modulation of allergic and immune complex-induced lung inflammation by bradykinin receptor antagonists Inflamm Res 53 2004 78 83
20. L. Gera, J.M. Stewart, E.T. Whalley, M. Burkard, and J.S. Zuzack New bradykinin antagonists having very high potency at B1 receptors Immunopharmacology 33 1996 183 185
21. F. Gobeil Jr., S. Charland, C. Filteau, S.I. Perron, W. Neugebauer, and D. Regoli Kinin B1 receptor antagonists containing alpha-methyl-l-phenylalanine: in vitro and in vivo antagonistic activities Hypertension 33 1999 823 829
22. F. Gobeil Jr., W. Neugebauer, C. Filteau, D. Jukic, S.N. Allogho, and L.H. Pheng et al. Structure-activity studies of B1 receptor-related peptides. Antagonists Hypertension 28 1996 833 839
23. F. Gobeil Jr., L.H. Pheng, I. Badini, X.K. Nguyen-Le, A. Pizard, and A. Rizzi et al. Receptors for kinins in the human isolated umbilical vein Br J Pharmacol 118 1996 289 294
24. W.L. Hanson, R.G. McCullough, W.M. Selig, M. Wieczorek, S. Ross, and E.T. Whalley et al. In vivo pharmacological profile of novel, potent, stable BK antagonists at B1 and B2 receptors Immunopharmacology 33 1996 191 193
25. G.N. Kaufman, C. Zaouter, B. Valteau, P. Sirois, and F. Moldovan Nociceptive tolerance is improved by bradykinin receptor B1 antagonism and joint morphology is protected by both endothelin type A and bradykinin receptor B1 antagonism in a surgical model of osteoarthritis Arthritis Res Ther 13 2011 R76
26. M. Kirby Painful diabetic neuropathy - current understanding and management for the primary care team Br J Diabetes Vasc Dis 3 2003 138 144
27. B. Lacoste, X.K. Tong, K. Lahjouji, R. Couture, and E. Hamel Cognitive and cerebrovascular improvements following kinin B1 receptor blockade in Alzheimer's disease mice J Neuroinflammation 10 2013 57
28. S.R. Lawson, B.H. Gabra, B. Guerin, W. Neugebauer, F. Nantel, and B. Battistini et al. Enhanced dermal and retinal vascular permeability in streptozotocin-induced type 1 diabetes in Wistar rats: blockade with a selective bradykinin B1 receptor antagonist Regul Pept 124 2005 221 224
29. S.R. Lawson, B.H. Gabra, F. Nantel, B. Battistini, and P. Sirois Effects of a selective bradykinin B1 receptor antagonist on increased plasma extravasation in streptozotocin-induced diabetic rats: distinct vasculopathic profile of major key organs Eur J Pharmacol 514 2005 69 78
30. L.M. Leeb-Lundberg, F. Marceau, W. Muller-Esterl, D.J. Pettibone, and B.L. Zuraw International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences Pharmacol Rev 57 2005 27 77
31. C. Lungu, J.P. Dias, C.E. Franca, B. Ongali, D. Regoli, and F. Moldovan et al. Involvement of kinin B1 receptor and oxidative stress in sensory abnormalities and arterial hypertension in an experimental rat model of insulin resistance Neuropeptides 41 2007 375 387
32. R.A. Malik, S. Tesfaye, and D. Ziegler Medical strategies to reduce amputation in patients with type 2 diabetes Diabet Med 30 2013 893 900
33. F. Marceau Kinin B1 receptors: a review Immunopharmacology 30 1995 1 26
34. J.G. Menke, J.A. Borkowski, K.K. Bierilo, T. MacNeil, A.W. Derrick, and K.A. Schneck et al. Expression cloning of a human B1 bradykinin receptor J Biol Chem 269 1994 21583 21586
35. W. Neugebauer, P.A. Blais, S. Halle, C. Filteau, D. Regoli, and F. Gobeil Jr. Kinin B1 receptor antagonists with multi-enzymatic resistance properties Can J Physiol Pharmacol 80 2002 287 292
36. S. Nightingale The neuropathic pain market Nat Rev Drug Discov 11 2012 101 102
37. B. Ongali, M.M. Campos, G. Bregola, D. Rodi, D. Regoli, and G. Thibault et al. Autoradiographic analysis of rat brain kinin B1 and B2 receptors: normal distribution and alterations induced by epilepsy J Comp Neurol 461 2003 506 519
38. S.H. Padia, and R.M. Carey AT2 receptors: beneficial counter-regulatory role in cardiovascular and renal function Pflugers Arch 465 2013 99 110
39. D. Pruneau, A. Duvoid, J.M. Luccarini, P. Belichard, and J.C. Bonnafous The kinin B1 receptor antagonist des-Arg9-[Leu8]bradykinin: an antagonist of the angiotensin AT1 receptor which also binds to the AT2 receptor Br J Pharmacol 114 1995 115 118
40. D. Regoli, and J. Barabe Pharmacology of bradykinin and related kinins Pharmacol Rev 32 1980 1 46
41. D. Regoli, J. Barabe, and W.K. Park Receptors for bradykinin in rabbit aortae Can J Physiol Pharmacol 55 1977 855 867
42. Regoli D, Neugebauer W, Gobeil F Jr., Gabra B, Sirois P. Selective bradykinin (BK) B1 peptidic receptor antagonists and uses thereof. USPTO. US Patent 7,211,566; 2007.
43. D. Regoli, S. Nsa Allogho, A. Rizzi, and F. Gobeil Jr. Bradykinin receptors and their antagonists Eur J Pharmacol 348 1998 1 10
44. D. Regoli, W.K. Park, and F. Rioux Pharmacology of angiotensin Pharmacol Rev 26 1974 69 123
45. D. Regoli, G.E. Plante, and F. Gobeil Jr. Impact of kinins in the treatment of cardiovascular diseases Pharmacol Ther 135 2012 94 111
46. N.E. Rhaleb, F. Gobeil Jr., and D. Regoli Non-selectivity of new bradykinin antagonists for B1 receptors Life Sci 51 1992 PL211
47. D. Rodi, A. Buzzi, M. Barbieri, S. Zucchini, G. Verlengia, and A. Binaschi et al. Bradykinin B receptors increase hippocampal excitability and susceptibility to seizures in mice Neuroscience 248C 2013 392 402
48. D. Rodi, R. Couture, B. Ongali, and M. Simonato Targeting kinin receptors for the treatment of neurological diseases Curr Pharm Des 11 2005 1313 1326
49. B. Simard, B.H. Gabra, and P. Sirois Inhibitory effect of a novel bradykinin B1 receptor antagonist, R-954, on enhanced vascular permeability in type 1 diabetic mice Can J Physiol Pharmacol 80 2002 1203 1207
50. J.M. Stewart, L. Gera, W. Hanson, J.S. Zuzack, M. Burkard, and R. McCullough et al. A new generation of bradykinin antagonists Immunopharmacology 33 1996 51 60
51. S. Talbot, and R. Couture Emerging role of microglial kinin B1 receptor in diabetic pain neuropathy Exp Neurol 234 2012 373 381
52. H.A. Torres, F. Louise Motta, V.M. Sales, C. Batista, J.M. da Silva, and T. Vignoli et al. Kinin B1 receptor gene ablation affects hypothalamic CART productionb Biol Chem 394 2013 901 908
53. P.H. Wang, G. Campanholle, M.A. Cenedeze, C.Q. Feitoza, G.M. Goncalves, and R.G. Landgraf et al. Bradykinin [corrected] B1 receptor antagonism is beneficial in renal ischemia-reperfusion injury PLoS ONE 3 2008 e3050
54. N. Warde Osteoarthritis: local antagonism of endothelin-1 and bradykinin receptors improves OA pain and joint morphology in rats Nat Rev Rheumatol 7 2011 375
55. E.T. Whalley, C.D. Figueroa, L. Gera, and K.D. Bhoola Discovery and therapeutic potential of kinin receptor antagonists Expert Opin Drug Discov 7 2012 1129 1148
56. A. Zuccollo, F. Cueva, M. Frontera, M. Navarro, and O. Catanzaro The role of the kallikrein-kinin system in type I diabetes (insulitis) Immunopharmacology 33 1996 349 350
57. A. Zuccollo, M. Navarro, and O. Catanzaro Effects of B1 and B2 kinin receptor antagonists in diabetic mice Can J Physiol Pharmacol 74 1996 586 589