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Gene Review

Bdkrb1  -  bradykinin receptor B1

Rattus norvegicus

Synonyms: B1 bradykinin receptor, B1R, B1bkr, BK-1 receptor, BKR, ...
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Disease relevance of Bdkrb1

  • In contrast, B1R mRNA was not detected in control rat urinary bladder; however, following acute (24 h) and chronic (8 day) CYP-induced cystitis in the rat, B1R mRNA was detected throughout the bladder [1].
  • The administration of B1 R antagonist resulted in renal interstitial and glomerular fibrosis in SHR-SP [2].
  • Since ERK 1 and 2 phosphorylation is an early event in the induction of matrix secretion and hyperproliferation associated with diabetic nephropathy, activation of B1R and B2R appears to be a useful pharmacological target in the management of this pathology [3].
  • Up-regulation of both BK-receptor (BKR) types in early stages of cardiac wound healing induced by ischemia and in chronic stages of cardiac remodeling induced by pressure-overload or by hyperglycemia indicates that kinins play a major role in the complex processes of cardiac tissue injury and repair [4].
  • Therefore we have examined B1 bradykinin receptor regulation in rat dorsal root ganglia in a model of inflammatory hyperalgesia, and correlated it with hyperalgesic behaviour [5].

High impact information on Bdkrb1

  • In competitive binding assays, unlabeled BK, Hoe 140 (a specific BK B2 receptor antagonist), and des-Arg9,[Leu8]BK (a BK B1 receptor antagonist) displaced [125I-Tyr8]BK with an IC50 of 4.3, 0.041, and 307 nmol/L, respectively [6].
  • Single-chain peptides combining AVP and BK directly, AVP(1-9)-BK(1-9) or via a flexible aminohexanoic acid (epsilonAhx) linker, AVP(1-9)-epsilonAhx-BK(1-9), bind with relatively high affinity to the bovine kidney medulla B2a bradykinin receptor (B2a BKR) [7].
  • Further development, combining the sequences of receptor subtype-selective antagonists, produced high-affinity chimeric antagonists of the V1a vasopressin receptor (V1a VPR) and the B2a BKR [7].
  • [Des-Arg10]-kallidin, a B1 receptor agonist, at concentrations of up to 10(-4) M did not induce any significant increase in CGRP outflow from the rat trachea [8].
  • Kinin B1 receptor up-regulation after lipopolysaccharide administration: role of proinflammatory cytokines and neutrophil influx [9].

Chemical compound and disease context of Bdkrb1


Biological context of Bdkrb1

  • Assignment of the kinin receptor B1 and B2 genes (Bdkrb1 and Bdkrb2) to rat chromosome 6q3.2 by FISH and radiation hybrid mapping [15].
  • The results indicate that both B1R and B2R contribute to the maintenance of normal BP, but one can compensate for inhibition of the other, and the chronic inhibition of both leads to significant upregulation in the genes of related vasoactive systems [16].
  • The infusion of B1 R antagonist for 4 weeks resulted in a significant elevation of blood pressure and urinary albumin excretion and a decrease in urinary NOx excretion in SHR-SP [2].
  • ERK 1 and 2 phosphorylation and expression of B1R and B2R were assessed by Western blot analysis [3].
  • B1R signaling suggests involvement in down-regulation of leukocyte activation, transmigration, and homing [17].

Anatomical context of Bdkrb1

  • Our findings indicate that the bradykinin 2 receptor (B2R) but not the bradykinin 1 receptor (B1R) is expressed in control bladder urothelium [1].
  • The occurrence of kinin-B1 receptor binding sites on acinar cell membranes was demonstrated by micro-autoradiography [18].
  • We have investigated the motor effects of i.v. or topical (onto the bladder serosa) administration of the selective kinin B1 receptor agonist [des-Arg9]-bradykinin ([des-Arg9]-BK) in the normal or inflamed (cyclophosphamide-induced) urinary bladder in urethane-anaesthetized rats [19].
  • In an acute model with two hours of ischaemia/two hours of reperfusion, application of the kinin-B1 receptor antagonist (CP-0298) alone, or in combination with kinin-B2 receptor antagonist (CP-0597), significantly reduced the number of adherent leukocytes in post-capillary venules [18].
  • The present study attempted to determine some of the mechanisms underlying B1R upregulation following tissue injury in rat portal vein [20].

Associations of Bdkrb1 with chemical compounds

  • Functional B1Rs were demonstrated by evoking ATP release and increases in [Ca(2+)](i) in CYP (24 h)-treated cultured rat urothelial cells with a selective B1 receptor agonist (des-Arg(9)-bradykinin) [1].
  • Only combined administration of B1R and B2R antagonists produced a significant BP increase from a baseline of 107-119 mmHg at end point, which could be partly prevented by losartan and was not associated with change in catecholamines, suggesting no involvement of the sympathoadrenal system [16].
  • Thus, the B1 receptor does not play a regulatory role in either the healthy or in STZ-diabetic heart [21].
  • Renal protective role of bradykinin B1 receptor in stroke-prone spontaneously hypertensive rats [2].
  • The partially purified BK receptor, enriched 1,500-fold, was then cross-linked to 125I-Tyr0-BK using disuccinimidyl suberate and purified to homogeneity as a single protein species on two-dimensional gel electrophoresis with a molecular mass of 81 kDa [22].

Physical interactions of Bdkrb1


Regulatory relationships of Bdkrb1

  • Superfusion with Bk (10 nM) increased [Ca++]i by 96 +/- 10 nM over basal levels in approximately 80% of the neurons tested that were not affected by a Bk-1 receptor antagonist but were inhibited 72% by a Bk-2 receptor antagonist [24].
  • In this study, we evaluated whether p42/p44 mitogen activated protein (MAP) and p38 stress activated protein (SAP) kinases were implicated in the activation of the gene encoding for the B1 receptor after heat stress in rat vascular smooth muscle cells (SMCs) [25].
  • Herein, we analyse the role of TNF-alpha and IL-1beta production for PAF-induced B1 receptor upregulation in the rat paw [26].

Other interactions of Bdkrb1


Analytical, diagnostic and therapeutic context of Bdkrb1


  1. Expression and function of bradykinin B1 and B2 receptors in normal and inflamed rat urinary bladder urothelium. Chopra, B., Barrick, S.R., Meyers, S., Beckel, J.M., Zeidel, M.L., Ford, A.P., de Groat, W.C., Birder, L.A. J. Physiol. (Lond.) (2005) [Pubmed]
  2. Renal protective role of bradykinin B1 receptor in stroke-prone spontaneously hypertensive rats. Hagiwara, M., Murakami, H., Ura, N., Agata, J., Yoshida, H., Higashiura, K., Shimamoto, K. Hypertens. Res. (2004) [Pubmed]
  3. Induction of B1 receptors in streptozotocin diabetic rats: possible involvement in the control of hyperglycemia-induced glomerular Erk 1 and 2 phosphorylation. Mage, M., Pécher, C., Neau, E., Cellier, E., Dos Reiss, M.L., Schanstra, J.P., Couture, R., Bascands, J.L., Girolami, J.P. Can. J. Physiol. Pharmacol. (2002) [Pubmed]
  4. Regulation of cardiac bradykinin B1- and B2-receptor mRNA in experimental ischemic, diabetic, and pressure-overload-induced cardiomyopathy. Spillmann, F., Altmann, C., Scheeler, M., Barbosa, M., Westermann, D., Schultheiss, H.P., Walther, T., Tschöpe, C. Int. Immunopharmacol. (2002) [Pubmed]
  5. Regulation and function of spinal and peripheral neuronal B1 bradykinin receptors in inflammatory mechanical hyperalgesia. Fox, A., Wotherspoon, G., McNair, K., Hudson, L., Patel, S., Gentry, C., Winter, J. Pain (2003) [Pubmed]
  6. Characterization of bradykinin B2 receptors in adult myocardium and neonatal rat cardiomyocytes. Minshall, R.D., Nakamura, F., Becker, R.P., Rabito, S.F. Circ. Res. (1995) [Pubmed]
  7. Chimeric strategies for the rational design of bioactive analogs of small peptide hormones. Howl, J., Langel, U., Hawtin, S.R., Valkna, A., Yarwood, N.J., Saar, K., Wheatley, M. FASEB J. (1997) [Pubmed]
  8. Pharmacology of the effects of bradykinin, serotonin, and histamine on the release of calcitonin gene-related peptide from C-fiber terminals in the rat trachea. Hua, X.Y., Yaksh, T.L. J. Neurosci. (1993) [Pubmed]
  9. Kinin B1 receptor up-regulation after lipopolysaccharide administration: role of proinflammatory cytokines and neutrophil influx. Passos, G.F., Fernandes, E.S., Campos, M.M., Araújo, J.G., Pesquero, J.L., Souza, G.E., Avellar, M.C., Teixeira, M.M., Calixto, J.B. J. Immunol. (2004) [Pubmed]
  10. Hyperalgesia in rats following intracerebroventricular administration of endotoxin: effect of bradykinin B1 and B2 receptor antagonist treatment. Walker, K., Dray, A., Perkins, M. Pain (1996) [Pubmed]
  11. Inflammation modulates the contribution of receptor-subtypes to bradykinin-induced hyperalgesia in the rat. Khasar, S.G., Miao, F.J., Levine, J.D. Neuroscience (1995) [Pubmed]
  12. Development of hyperthermia following intracerebroventricular administration of endotoxin in the rat: effect of kinin B1 and B2 receptor antagonists. Walker, K., Dray, A., Perkins, M. Br. J. Pharmacol. (1996) [Pubmed]
  13. Kinin B2 receptor is not involved in enalapril-induced apoptosis and regression of hypertrophy in spontaneously hypertensive rat aorta: possible role of B1 receptor. Duguay, D., Der Sarkissian, S., Kouz, R., Ongali, B., Couture, R., deBlois, D. Br. J. Pharmacol. (2004) [Pubmed]
  14. Inflammatory hyperalgesia induced by zymosan in the plantar tissue of the rat: effect of kinin receptor antagonists. Bélichard, P., Landry, M., Faye, P., Bachvarov, D.R., Bouthillier, J., Pruneau, D., Marceau, F. Immunopharmacology (2000) [Pubmed]
  15. Assignment of the kinin receptor B1 and B2 genes (Bdkrb1 and Bdkrb2) to rat chromosome 6q3.2 by FISH and radiation hybrid mapping. Gösele, C., Grützner, F., Pesquero, J.B., Silva, J.A., Junge, T., Ganten, D., Bader, M., Knoblauch, M. Cytogenet. Cell Genet. (2000) [Pubmed]
  16. Role of bradykinin B1 and B2 receptors in normal blood pressure regulation. Duka, A., Duka, I., Gao, G., Shenouda, S., Gavras, I., Gavras, H. Am. J. Physiol. Endocrinol. Metab. (2006) [Pubmed]
  17. Interactions between bradykinin (BK) and cell adhesion molecule (CAM) expression in peptidoglycan-polysaccharide (PG-PS)-induced arthritis. Sainz, I.M., Uknis, A.B., Isordia-Salas, I., Dela Cadena, R.A., Pixley, R.A., Colman, R.W. FASEB J. (2004) [Pubmed]
  18. Kinin-B1 receptors in ischaemia-induced pancreatitis: functional importance and cellular localisation. Kuebler, J.F., Schremmer-Danninger, E., Bhoola, K.D., Roscher, A.A., Messmer, K., Hoffmann, T.F. Biol. Chem. (2003) [Pubmed]
  19. Kinin B1 receptor-mediated motor responses in normal or inflamed rat urinary bladder in vivo. Lecci, A., Meini, S., Tramontana, M., Giuliani, S., Criscuoli, M., Maggi, C.A. Regul. Pept. (1999) [Pubmed]
  20. Bradykinin B1 receptor expression induced by tissue damage in the rat portal vein: a critical role for mitogen-activated protein kinase and nuclear factor-kappaB signaling pathways. Medeiros, R., Cabrini, D.A., Ferreira, J., Fernandes, E.S., Mori, M.A., Pesquero, J.B., Bader, M., Avellar, M.C., Campos, M.M., Calixto, J.B. Circ. Res. (2004) [Pubmed]
  21. Myocardial expression of rat bradykinin receptors and two tissue kallikrein genes in experimental diabetes. Tschöpe, C., Walther, T., Yu, M., Reinecke, A., Koch, M., Seligmann, C., Heringer, S.B., Pesquero, J.B., Bader, M., Schultheiss, H., Unger, T. Immunopharmacology (1999) [Pubmed]
  22. Purification and characterisation of B2 bradykinin receptor from rat uterus. Yaqoob, M., Snell, C.R. J. Neurochem. (1994) [Pubmed]
  23. B2-kinin receptor like binding in rat glomerular membranes. Bascands, J.L., Pécher, C., Cabos, G., Girolami, J.P. Biochem. Biophys. Res. Commun. (1989) [Pubmed]
  24. Bradykinin (Bk) increases cytosolic calcium in cultured rat myenteric neurons via Bk-2 type receptors coupled to mobilization of extracellular and intracellular sources of calcium: evidence that calcium influx is prostaglandin dependent. Gelperin, D., Mann, D., del Valle, J., Wiley, J.W. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  25. MAP-kinase dependent activation of kinin B1 receptor gene transcription after heat stress in rat vascular smooth muscle cells. Lagneux, C., Lebrin, F., Demenge, P., Godin-Ribuot, D., Ribuot, C. Int. Immunopharmacol. (2001) [Pubmed]
  26. Cytokines and neutrophils as important mediators of platelet-activating factor-induced kinin B1 receptor expression. Fernandes, E.S., Passos, G.F., Campos, M.M., de Souza, G.E., Fittipaldi, J.F., Pesquero, J.L., Teixeira, M.M., Calixto, J.B. Br. J. Pharmacol. (2005) [Pubmed]
  27. Inflammation modifies the role of cyclooxygenases in the contractile responses of the rat detrusor smooth muscle to kinin agonists. Meini, S., Lecci, A., Cucchi, P., Catalioto, R.M., Criscuoli, M., Maggi, C.A. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  28. Activity and functional significance of the renal kallikrein-kinin-system in polycystic kidney disease of the rat. Braun, C., Kleemann, T., Hilgenfeldt, U., Riester, U., Rohmeiss, P., van der Woude, F.J. Kidney Int. (2002) [Pubmed]
  29. Kinin-induced prolongation of action-potential duration in right ventricular muscle from rat: involvement of B1 and B2 receptors. Gouin, L., Cardinal, R., Adam, A., Drapeau, G., Nadeau, R. J. Cardiovasc. Pharmacol. (1996) [Pubmed]
  30. BK-induced cytosolic phospholipase A2 expression via sequential PKC-delta, p42/p44 MAPK, and NF-kappaB activation in rat brain astrocytes. Hsieh, H.L., Wu, C.Y., Hwang, T.L., Yen, M.H., Parker, P., Yang, C.M. J. Cell. Physiol. (2006) [Pubmed]
  31. Age-related changes of bradykinin B1 and B2 receptors in rat heart. Kintsurashvili, E., Duka, A., Ignjacev, I., Pattakos, G., Gavras, I., Gavras, H. Am. J. Physiol. Heart Circ. Physiol. (2005) [Pubmed]
  32. Molecular cloning and expression of rat bradykinin B1 receptor. Ni, A., Chai, K.X., Chao, L., Chao, J. Biochim. Biophys. Acta (1998) [Pubmed]
  33. Effects of dexamethasone and protein kinase C inhibitors on the induction of bradykinin B1 mRNA and the bradykinin B1 receptor-mediated contractile response in isolated rat ileum. Ueno, A., Dekura, E., Kosugi, Y., Yoshimura, M., Naraba, H., Kojima, F., Oh-ishi, S. Biochem. Pharmacol. (2002) [Pubmed]
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