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- Title
Vasorelaxant effects of 2-nitro-1-phenyl-1-propanol in rat aorta.
- Authors
Brito, Teresinha Silva; Batista‐Lima, Francisco José; Gadelha, Kalinne Kelly Lima; Fonseca‐Magalhães, Patrícia Andrea; Lahlou, Saad; Magalhães, Pedro Jorge Caldas
- Abstract
2-Nitro-1-phenyl-1-propanol ( NPP) is a nitro alcohol that is known as an intermediate in the synthesis of sympathomimetic agents, such as norephedrine. The present study investigated the vasoactive effects of NPP on rat aorta. In endothelium-intact aortic rings, NPP fully relaxed contractions that were induced by phenylephrine, KCl, and U-46619. The relaxant effects of NPP on phenylephrine-elicited contractions remained unaffected by NG-nitro- l-arginine methyl ester ( l-NAME), indomethacin, propranolol, tetraethylammonium, 4-aminopyridine, and glibenclamide. Conversely, pretreatment with 1 H-[1,2,4]oxadiazolo[4,3- a]quinoxalin-1-one (ODQ), cis- N-(2-phenylcyclopentyl)-azacyclotridec-1-en-2-amine hydrochloride (MDL-12,330A), and N-[2-( P-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide dihydrochloride (H-89) reduced the ability of NPP to relax contractions that were elicited by phenylephrine. NPP inhibited the vasoconstrictor response that was induced by Ca2+ in aortic rings that were stimulated by pharmacomechanical or electromechanical coupling with phenylephrine and 60 mmol/L KCl, respectively, and after the depletion of intracellular Ca2+ stores. Such effects of NPP were significantly reversed by pretreatment with the guanylyl cyclase inhibitor ODQ and weakly influenced by the adenylyl cyclase inhibitor MDL-12,330A. In Ca2+-free medium, NPP inhibited transient contractions that were induced by phenylephrine but not caffeine. In homogenates of aortic rings, NPP increased cyclic guanosine 3′,5′-monophosphate ( cGMP) and cyclic adenosine 3′-5′-monophosphate levels, but this effect was statistically significant only for cGMP. In conclusion, in contrast to the vasoconstrictor amine norephedrine, NPP is a vasodilator in rat aorta, and its relaxant effects are likely attributable to cGMP production.
- Subjects
VASODILATION; PROPANOLS; NITROPHENYL compounds; VASOCONSTRICTORS; VASCULAR smooth muscle physiology; PHENYLPROPANOLAMINE
- Publication
Clinical & Experimental Pharmacology & Physiology, 2016, Vol 43, Issue 11, p1054
- ISSN
0305-1870
- Publication type
Article
- DOI
10.1111/1440-1681.12625