Results 141 to 150 of about 6,163 (183)
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Immunolocalization of Bradykinin B2 Receptors on Skeletal Muscle Cells
Diabetes, 1996The 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 +2 more
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Bradykinin B2 receptors in nodose ganglia of rat and human
European Journal of Pharmacology, 1998The 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, 1991pA2 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 +6 more
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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 +7 more
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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 +7 more
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Induction of human B2 bradykinin receptor mRNA and membrane receptors by IFNγ
Immunopharmacology, 1998A 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 +4 more
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Antagonists of B 2 bradykinin receptors
The FASEB Journal, 1989Bradykinin 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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Bradykinin B2-Receptor-Mediated Positive Chronotropic Effect of Bradykinin in Isolated Rat Atria
Journal of Cardiovascular Pharmacology, 1998The 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 +4 more
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Bradykinin B2 receptor-mediated chronotropic effect of bradykinin in isolated guinea pig atria
European Journal of Pharmacology, 1995The present study was undertaken to characterize the direct chronotropic effect of bradykinin in isolated spontaneously beating atria of the guinea pig. Bradykinin caused concentration-dependent increases in the beating rate of atria. In contrast, the active metabolite of bradykinin and the typical bradykinin B1 receptor agonist, Des-Arg9-bradykinin ...
B, Tesfamariam, G T, Allen, J R, Powell
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Simulations on the activation of the bradykinin B2 receptor
Biochemical Society Transactions, 1996S W, Doughty, C A, Reynolds
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Bradykinin B2 Receptor Antagonists for the Treatment of Pain
2004Publisher Summary The bradykinin B2 receptor is a mature G-protein coupled receptor target that has long offered the prospect of therapeutic intervention in pain and inflammation, but this has been notoriously difficult to achieve. This chapter discusses the kinin B2 receptor as a therapeutic target, peptide bradykinin B2 receptor antagonists, and ...
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