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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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of prorenin, renin, and the (pro)renin receptor: Promising young players
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(SEE CHAPTER 11) Castrop H et al: Physiology of kidney renin. Physiol Rev 2010;90:607.
ANGIOTENSIN RECEPTOR BLOCKERS Chow BS, Allen TJ: Angiotensin II type 2 receptor (AT2R) in renal and cardiovas-
(SEE CHAPTER 11) cular disease. Clin Sci (Lond) 2016;130:1307.
RENIN INHIBITOR Crowley SD, Coffman TM: Recent advances involving the renin-angiotensin
system. Exp Cell Res 2012;318:1049.
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
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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.
Angiotensin receptors: Interpreters of pathophysiological angiotensinergic
SUBSTANCE P ANTAGONIST stimuli [corrected]. Pharmacol Rev 2015;67:754.
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.
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Ambrisentan Letairis McMurray JJ et al: Effect of valsartan on the incidence of diabetes and cardiovas-
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Epoprostenol Flolan, Veletri Nguyen G: Renin, (pro)renin and receptor: An update. Clin Sci (Lond) 2011;
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Selexipag Uptravi
Treprostinil Tyvaso, Remodulin