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Kinins antagonists

POTENTIAL THERAPEUTIC USES Bradykinin contributes to many of the effects of the ACE inhibitors (Eigure 24-2). Aprotinin, a kallikrein inhibitor, is administered to patients undergoing coronary bypass to minimize bleeding and blood requirements (see below). Kinin agonists potentially may increase the delivery of chemotherapeutic agents past the blood-brain barrier. Based on some of the actions outlined earlier, kinin antagonists are being tested in inflammatory conditions. [Pg.414]

Tissue-specific Agonists/Antagonists Tissue-type Plasminogen Activator T-kinin (Ile-Ser-Bradykinin)... [Pg.1504]

Complete C-fibre inhibitions can be produced under normal conditions but opiates do not always produce a complete analgesia in some clinical situations, especially when the pain arises from nerve damage. Reasons for this are suspected to be excessive NMDA-mediated activity which is hard to inhibit and the mobilisation of cholecysto-kinin in the spinal cord which can act as a physiological antagonist of opiate actions. The idea that pre-emptive analgesia aids post-operative pain relief by preventing the pain-induced activation of these systems is becoming popular. [Pg.470]

Bueb JL, Mousli M, Bronner C, Rouot B, Landry Y (1990) Activation of Gi-Uke proteins, a receptor-independent effect of kinins in mast cells. Mol Pharmacol 38 816—822 Burde R, Dippel E, Seifert R (1996) Receptor-independent G protein activation may account for the stimulatory effects of first-generation Hl-receptor antagonists in HL-60 cells, basophils, and mast cells. Biochem Pharmacol 51 125—131... [Pg.74]

Drugs that modify the activity of the kallikrein-kinin system are available, though none are in wide clinical use. Considerable effort has been directed toward developing kinin receptor antagonists, since such drugs have considerable therapeutic potential as anti-inflammatory and antinociceptive agents. Competitive antagonists of both and B2 receptors are available for research use. Examples of B receptor... [Pg.382]

Icatibant Selective antagonist of kinin B2 receptors Blocks effects of kinins on pain, hyperalgesia, and inflammation Potential use for inflammatory pain and inflammation... [Pg.391]

Overall, the kinins are an important part of a well-organized physiological system. The various aspects and interdependencies of the kinin system have been, and continue to be, the focus of intensive research efforts in many laboratories. Many pharmaceutical companies have identified this system as an ideal site for therapeutic intervention in many inflammatory diseases. Hence, there have been many diverse approaches taken toward the discovery of antagonists (peptide and nonpeptide) of B2 and B1 receptors. This review focuses on the structure-based design strategies pursued in our laboratories during the past several years. [Pg.121]

There have been a variety of single alanine point mutations experimentally introduced into both rat and human bradykinin B2 receptors. Several of these have been shown to decrease the affinity of bradykinin to the receptor and have been implicated structurally near the agonist binding site. In contrast, at the time of this manuscript, there have been no mutations reported that adversely affect the ability of any peptide antagonists to bind to the receptor. Furthermore, antibodies raised against the certain extracellular domains of the kinin receptor compete with bradykinin for binding to the receptor but have no inhibitory... [Pg.137]

Icatibant is a second generation B2 receptor antagonist. It is orally active, potent, and selective, has a long duration of action (> 60 minutes), and displays high B2 receptor affinity in humans and all other species in which it has been tested. Icatibant has been used extensively in animal studies to block exogenous and endogenous bradykinin and in human studies to evaluate the role of kinins in pain, hyperalgesia, and inflammation. [Pg.421]

Peculiarly little attention was aimed at the investiga tion of other 6-alkylpurine derivatives. Recently, cyto kinin activity was reported in some 6-(arylalkynyl), 6-(arylalkenyl)-, and 6-(atylalkyl)purines.21 We have recently described the cytostatic activity of 6-(trifluo-romethyl)purine riboside.22 The corticotropin-releasing hormone antagonist activity of some 2,8,9-trisubsti-tuted-6-arylpurines has been also reported.23... [Pg.1]

Kohzuki M, Yasujima M, Yoshida K et al. (1994) Antihypertensive and antiproteinuric effects of losartan in spontaneously hypertensive rats with chronic renal failure. Hy-pertens Res Clin Exp 17 173-178 Kohzuki M, Kanazawa M, Liu PF et al. (1995) Kinin and angiotensinll receptor antagonists in rats with chronic renal failure Chronic effects on cardio- and renoprotection of angiotensin converting enzyme inhibitors. J Hypertens 13 1785-1790... [Pg.127]

Two receptor subtypes can be distinguished AT-i, which mediates the above actions of angiotensin II and AT2, whose physiological role is still unclear. Losartan is an A receptor antagonist whose main (antihypertensive) and side effects resemble those of ACE inhibitors. However, because it does not inhibit degradation of kinins, it does not cause dry cough. Losartan is used in the therapy of hypertension. Other analogues are valsartan, irbesartan, eprosartan, and candesartan. 2005 Thieme and conditions of license. [Pg.128]


See other pages where Kinins antagonists is mentioned: [Pg.676]    [Pg.390]    [Pg.123]    [Pg.145]    [Pg.14]    [Pg.676]    [Pg.441]    [Pg.364]    [Pg.676]    [Pg.390]    [Pg.123]    [Pg.145]    [Pg.14]    [Pg.676]    [Pg.441]    [Pg.364]    [Pg.142]    [Pg.10]    [Pg.75]    [Pg.142]    [Pg.142]    [Pg.1068]    [Pg.77]    [Pg.78]    [Pg.110]    [Pg.105]    [Pg.439]    [Pg.904]    [Pg.124]    [Pg.239]    [Pg.382]    [Pg.382]    [Pg.251]    [Pg.421]    [Pg.1457]    [Pg.94]    [Pg.17]    [Pg.203]    [Pg.128]    [Pg.176]    [Pg.10]    [Pg.75]    [Pg.142]    [Pg.142]    [Pg.1068]   
See also in sourсe #XX -- [ Pg.412 , Pg.414 ]




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