Results 141 to 150 of about 5,853 (186)

Bradykinin B2 receptors – a target in diabetic nephropathy

Expert Opinion on Therapeutic Targets, 2005
Diabetic nephropathy is the leading cause of chronic renal failure in westernized countries. The polymorphism in angiotensin-converting enzyme (ACE), which leads to higher than normal levels of this enzyme, is a predictor of nephropathy in patients with diabetes.
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Characterization of a B2-bradykinin receptor in human glomerular podocytes

American Journal of Physiology-Renal Physiology, 1996
We characterized bradykinin (BK) receptors in a human line of glomerular visceral epithelial cells (hGVEC) transfected by the SV40 virus. [3H]BK bound specifically in a manner consistent with a single high-affinity site. Scatchard analysis yielded dissociation constant and maximum binding values of 0.28 +/- 0.04 nM and 76.6 +/- 4.9 fmol/mg ...
N, Ardaillou, V, Blaise, K, Costenbader, Y, Vassitch, R, Ardaillou   +4 more
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Role of ßarrestins in bradykinin B2 receptor-mediated signalling

Cellular Signalling, 2011
G protein-coupled receptors (GPCRs) can engage multiple pathways to activate ERK1/2 via both G proteins and/or ßarrestin. Receptor recruitment of ßarrestin is also important for GPCR desensitization, internalization and resensitization. Modulation of the receptor/ßarrestin interaction through modification of either component would presumably alter the ...
Brandon, Zimmerman, May, Simaan, Marie-Yvonne, Akoume, Nadia, Houri, Stéphanie, Chevallier, Philippe, Séguéla, Stéphane A, Laporte   +6 more
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Bradykinin B2 receptors in nodose ganglia of rat and human

European Journal of Pharmacology, 1998
The present study has employed in vitro electrophysiology to characterise the ability of bradykinin to depolarise the rat isolated nodose ganglion preparation, containing the perikarya of vagal afferent neurons. Both bradykinin and kallidin elicited a concentration-dependent (1-100 nM) depolarisation when applied to the superfusate bathing the nodose ...
E, Krstew, B, Jarrott, A J, Lawrence
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New highly potent bradykinin B2 receptor antagonists

Agents and Actions, 1991
pA2 values of new B2 receptor antagonists ranging from 7.51 to 8.86 were measured on the rabbit jugular vein, while lower values were observed in the other preparations (for instance, the hamster urinary bladder). The most potent antagonists were those containing a hydroxyproline (Hyp) in position 3, a D-Arg at the N-terminal and a Leu instead of a Phe
D, Regoli, N E, Rhaleb, C, Tousignant, N, Rouissi, F, Nantel, D, Jukic, G, Drapeau   +6 more
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Immunolocalization of Bradykinin B2 Receptors on Skeletal Muscle Cells

Diabetes, 1996
The kallikrein-kinin system has been implicated in the inflammatory process, blood pressure regulation, renal homeostasis, and glucose utilization. The effects of kallikrein and kinin on glucose uptake by the skeletal muscle are well established; however, the occurrence and the cellular distribution of the kinin receptor(s) mediating these effects in ...
C D, Figueroa, G, Dietze, W, Müller-Esterl   +2 more
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From Bradykinin B2 Receptor Antagonists to Orally Active and Selective Bradykinin B1 Receptor Antagonists

Journal of Medicinal Chemistry, 2012
The bradykinin (BK) B1 receptor is an attractive target for the treatment of chronic pain and inflammation. Starting from a dual B1 and B2 antagonist, novel antagonists were designed that display low-nanomolar affinity for human B1 receptor and selectivity over B2.
Martine, Barth, Michel, Bondoux, Jean-Michel, Luccarini, Vincent, Peyrou, Pierre, Dodey, Didier, Pruneau, Christine, Massardier, Jean-Luc, Paquet   +7 more
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Induction of human B2 bradykinin receptor mRNA and membrane receptors by IFNγ

Immunopharmacology, 1998
A potential mechanism for the increased sensitivity of inflamed tissues to bradykinin is the upregulation of bradykinin receptor expression. We report that recombinant human IFNgamma stimulated a concentration-dependent increase in cell surface bradykinin receptor expression in intact T24 human epithelial-like cells, determined by radioligand binding ...
C C, Lung, M A, Jagels, P J, Daffern, E M, Tan, B L, Zuraw   +4 more
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Bradykinin B2-Receptor-Mediated Positive Chronotropic Effect of Bradykinin in Isolated Rat Atria

Journal of Cardiovascular Pharmacology, 1998
The positive chronotropic effect of bradykinin was investigated in isolated spontaneously beating atria of the rat. Cumulative additions of bradykinin (0.3-100 nM) caused a concentration-dependent increase in the beating rate of the atria by maximally 35+/-4 beats/min, approximately 25% of the 1 microM isoprenaline-induced maximal responses.
Li, Qun, Zhang, Jie, Loro, Juan F., Pfaffendorf, Martin, Van Zwieten, Pieter A.   +4 more
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Antagonists of B ₂ bradykinin receptors

The FASEB Journal, 1989
Bradykinin and its active metabolites, produced by kallikreins at their sites of action, potently elicit a variety of biological effects: hypotension, bronchoconstriction, gut and uterine contraction, epithelial secretion in airway, gut, and exocrine glands, vascular permeability, pain, connective tissue proliferation, cytokine ...
L R, Steranka, S G, Farmer, R M, Burch
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