Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 5 de 5
Filter
Add more filters











Publication year range
1.
Braz J Med Biol Res ; 50(9): e5765, 2017 Aug 07.
Article in English | MEDLINE | ID: mdl-28793049

ABSTRACT

Clobenzorex is a metabolic precursor of amphetamine indicated for the treatment of obesity. Amphetamines have been involved with cardiovascular side effects such as hypertension and pulmonary arterial hypertension. The aim of the present study was to investigate whether the direct application of 10-9-10-5 M clobenzorex on isolated phenylephrine-precontracted rat aortic rings produces vascular effects, and if so, what mechanisms may be involved. Clobenzorex produced an immediate concentration-dependent vasorelaxant effect at the higher concentrations (10-7.5-10-5 M). The present outcome was not modified by 10-6 M atropine (an antagonist of muscarinic acetylcholine receptors), 3.1×10-7 M glibenclamide (an ATP-sensitive K+ channel blocker), 10-3 M 4-aminopyridine (4-AP; a voltage-activated K+ channel blocker), 10-5 M indomethacin (a prostaglandin synthesis inhibitor), 10-5 M clotrimazole (a cytochrome P450 inhibitor) or 10-5 M cycloheximide (a general protein synthesis inhibitor). Contrarily, the clobenzorex-induced vasorelaxation was significantly attenuated (P<0.05) by 10-5 M L-NAME (a direct inhibitor of nitric oxide synthase), 10-7 M ODQ (an inhibitor of nitric oxide-sensitive guanylyl cyclase), 10-6 M KT 5823 (an inhibitor of protein kinase G), 10-2 M TEA (a Ca2+-activated K+ channel blocker and non-specific voltage-activated K+ channel blocker) and 10-7 M apamin plus 10-7 M charybdotoxin (blockers of small- and large-conductance Ca2+-activated K+ channels, respectively), and was blocked by 8×10-2 M potassium (a high concentration) and removal of the vascular endothelium. These results suggest that the direct vasorelaxant effect by clobenzorex on phenylephrine-precontracted rat aortic rings involved stimulation of the NO/cGMP/PKG/Ca2+-activated K+ channel pathway.


Subject(s)
Amphetamines/pharmacology , Aorta, Thoracic/drug effects , Endothelium, Vascular/drug effects , Vasodilation , Vasodilator Agents/pharmacology , Animals , Calcium Channels/drug effects , Calcium Channels/metabolism , Male , Nitric Oxide Synthase Type III/drug effects , Nitric Oxide Synthase Type III/metabolism , Potassium Channels/drug effects , Potassium Channels/metabolism , Potassium Channels, Voltage-Gated/drug effects , Potassium Channels, Voltage-Gated/metabolism , Rats , Rats, Wistar
2.
Rev. bras. pesqui. méd. biol ; Braz. j. med. biol. res;50(9): e5765, 2017. tab, graf
Article in English | LILACS | ID: biblio-888990

ABSTRACT

Clobenzorex is a metabolic precursor of amphetamine indicated for the treatment of obesity. Amphetamines have been involved with cardiovascular side effects such as hypertension and pulmonary arterial hypertension. The aim of the present study was to investigate whether the direct application of 10-9-10-5 M clobenzorex on isolated phenylephrine-precontracted rat aortic rings produces vascular effects, and if so, what mechanisms may be involved. Clobenzorex produced an immediate concentration-dependent vasorelaxant effect at the higher concentrations (10-7.5-10-5 M). The present outcome was not modified by 10-6 M atropine (an antagonist of muscarinic acetylcholine receptors), 3.1×10-7 M glibenclamide (an ATP-sensitive K+ channel blocker), 10-3 M 4-aminopyridine (4-AP; a voltage-activated K+ channel blocker), 10-5 M indomethacin (a prostaglandin synthesis inhibitor), 10-5 M clotrimazole (a cytochrome P450 inhibitor) or 10-5 M cycloheximide (a general protein synthesis inhibitor). Contrarily, the clobenzorex-induced vasorelaxation was significantly attenuated (P<0.05) by 10-5 M L-NAME (a direct inhibitor of nitric oxide synthase), 10-7 M ODQ (an inhibitor of nitric oxide-sensitive guanylyl cyclase), 10-6 M KT 5823 (an inhibitor of protein kinase G), 10-2 M TEA (a Ca2+-activated K+ channel blocker and non-specific voltage-activated K+ channel blocker) and 10-7 M apamin plus 10-7 M charybdotoxin (blockers of small- and large-conductance Ca2+-activated K+ channels, respectively), and was blocked by 8×10-2 M potassium (a high concentration) and removal of the vascular endothelium. These results suggest that the direct vasorelaxant effect by clobenzorex on phenylephrine-precontracted rat aortic rings involved stimulation of the NO/cGMP/PKG/Ca2+-activated K+ channel pathway.


Subject(s)
Animals , Male , Rats , Amphetamines/pharmacology , Aorta, Thoracic/drug effects , Endothelium, Vascular/drug effects , Vasodilation , Vasodilator Agents/pharmacology , Calcium Channels/drug effects , Calcium Channels/metabolism , Nitric Oxide Synthase Type III/drug effects , Nitric Oxide Synthase Type III/metabolism , Potassium Channels, Voltage-Gated/drug effects , Potassium Channels, Voltage-Gated/metabolism , Potassium Channels/drug effects , Potassium Channels/metabolism , Rats, Wistar
5.
Rev. méd. IMSS ; 33(4): 429-34, jul.-ago. 1995. ilus, tab
Article in Spanish | LILACS | ID: lil-174175

ABSTRACT

Se efectuó un estudio en la población derechohabiente mayor de 15 años que demandaba los servicios médicos en una unidad de atención a la salud del primer nivel de atención del Instituto Mexicano del Seguro Social (IMSS) en la zona metropolitana de Guadalajara, Jalisco. El propósito fue identificar el nivel de educación para la salud de usuarios de los servicios y analizar el modelo de práctica educativa institutcional recibida por el derechohabiente. Mediante este proyecto de investigación se puede señalar que 27.1 por ciento de la población derechohabiente demandante tiene un adecuado nivel de educación para la salud, que la práctica educativa recibida se basa en la acumulación de información, y que ésta ha sido otorgada por un equipo disciplinario en salud, el cual refleja limitaciones en los métodos y técnicas de educación en salud.


Subject(s)
Adult , Middle Aged , Humans , Male , Female , Social Medicine/organization & administration , Social Security , Family Practice/trends , Health Education , Health Surveys , Health Care Levels
SELECTION OF CITATIONS
SEARCH DETAIL