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318     SECTION IV  Drugs with Important Actions on Smooth Muscle



                                                                                                        Clinical
                  Subclass, Drug     Mechanism of Action           Effects                              Applications
                  NEUROTENSIN ANTAGONISTS
                    •  Meclinertant  Antagonist of central and peripheral   Blocks some central and peripheral (vasodilator) actions   None identified
                                     neurotensin receptors         of neurotensin
                  CALCITONIN GENE-RELATED PEPTIDE ANTAGONISTS
                    •   Telcagepant,   Antagonists of the calcitonin gene-related   Blocks some central and peripheral (vasodilator) actions   Migraine 1
                    olcegepant       peptide (CGRP) receptor       of CGRP
                  NEUROPEPTIDE Y ANTAGONISTS
                    •  BIBP3226      Selective antagonist of neuropeptide   Blocks vasoconstrictor response to neurotensin  Potential antiobesity
                                     Y 1  receptors                                                     agent
                    •  BIIE0246: Selective for Y 2  receptor
                    •  MK-0557: Selective for Y 5  receptor
                  UROTENSIN ANTAGONISTS
                    •  Palosuran     Antagonist of urotensin receptors  Blocks vasoconstrictor action of urotensin  Potential for
                    •   GSK1440115: More                                                                treatment of diabetic
                    potent than palosuran                                                               renal failure and
                                                                                                        asthma 1
                 1
                 Undergoing preclinical or clinical evaluation.

                 PREP AR A TIONS                                     REFERENCES
                 A V AIL ABLE                                        Angiotensin

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                                          (SEE CHAPTER 11)           Castrop H et al: Physiology of kidney renin. Physiol Rev 2010;90:607.
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                                          (SEE CHAPTER 11)               cular disease. Clin Sci (Lond) 2016;130:1307.
                                  RENIN INHIBITOR                    Crowley SD, Coffman  TM: Recent advances involving the renin-angiotensin
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                 Aliskiren                Tekturna                   Damkjaer M et al: Renal renin secretion as regulator of body fluid homeostasis.
                                   KININ INHIBITOR                       Pflugers Archiv Eur J Physiol 2013;465:153.
                 Icatibant                Firazyr                    Danser AH: The role of the (pro)renin receptor in hypertensive disease. Am J
                                KALLIKREIN INHIBITORS                    Hypertens 2015;28:1187.
                 C1 esterase inhibitor, human  Cinryze, Berinert     Friis UG et al: Regulation of renin secretion by renal juxtaglomerular cells. Eur J
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                 Ecallantide              Kalbitor                   Harel Z et al: The effect of combination treatment with aliskiren and blockers
                             AVP RECEPTOR ANTAGONISTS                    of the renin-angiotensin system on hyperkalaemia and acute kidney injury:
                 Conivaptan               Vaprisol                       Systematic review and meta-analysis. BMJ 2012;344:e42.
                 Tolvaptan                Samsca                     Karnik SS et al: International Union of Basic and Clinical Pharmacology. XCIX.
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                 Aprepitant               Emend                      Kim SM, Briggs JP, Schnermann J: Convergence of major physiological stimuli
                             NATRIURETIC PEPTIDE AGONIST                 for renin release on the Gs-alpha/cyclic adenosine monophosphate signaling
                 Nesiritide               Natrecor                       pathway. Clin Exp Nephrol 2012;16:17.
                       DRUGS USED IN PULMONARY HYPERTENSION          Kurtz A: Renin release: Sites, mechanisms, and control. Annu Rev Physiol 2011;
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                 Ambrisentan              Letairis                   McMurray JJ et al: Effect of valsartan on the incidence of diabetes and cardiovas-
                 Bosentan                 Tracleer                       cular events. N Engl J Med 2010;362:1477.
                 Epoprostenol             Flolan, Veletri            Nguyen G: Renin, (pro)renin and receptor: An update. Clin Sci (Lond) 2011;
                 Iloprost                 Ventavis                       120:169.
                 Macitentan               Opsumit                    Zheng Z et al: A systematic review and meta-analysis of aliskiren and angiotensin
                                                                         receptor blockers in the management of essential hypertension. J Renin
                 Riociguat                Adempas                        Angiotensin Aldosterone Syst 2011;12:102.
                 Selexipag                Uptravi
                 Treprostinil             Tyvaso, Remodulin
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