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Effects of hydralazine on contractile responses to alpha 1 and alpha 2-adrenoceptor agonists in isolated rubbed rat aorta. 1994

M J Moina, and B Bardan, and M Campos Toimil, and A F Alzueta, and J Gil-Longo, and F Orallo
Departamento de Farmacología, Facultad de Farmacia, Universidad de Santiago, La Coruña, Spain.

1. Effects of hydralazine on contractile responses to noradrenaline (an alpha 1- and alpha 2-adrenoceptor agonist) to phenylephrine and methoxamine (both selective alpha 1-adrenoceptor agonists) and to clonidine and BHT-920 (both relatively selective alpha 2-adrenoceptor agonists) were examined in isolated rat aorta deprived of endothelium. Hydralazine (1 mM) produced a rightward shift with depression of the maximal tension of the concentration-response curves for all the agonists tested. The effects on curves for clonidine and BHT-920 (partial agonists) were greater than on curves for noradrenaline, phenylephrine and methoxamine (full agonists). 2. The inhibitory effect of prazosin (pA2, about 10) was much greater than that of yohimbine (pA2, about 7) for all the agonists. 3. In tissues pretreated with phenoxybenzamine, hydralazine (1 mM) inhibited the residual response to all the agonists. The inhibitory effect on residual response to full agonists was similar to that observed on response to partial agonists in tissues not treated with phenoxybenzamine. 4. The relationship between maximal response and percentage receptor occupancy was nonlinear for full agonists, but near-linear for partial agonists. 5. These results indicate that the responses induced by noradrenaline, phenylephrine, methoxamine, clonidine and BHT-920 in the rat aorta are due to the activation of alpha 1-adrenoceptors and confirm the vasorelaxant action of hydralazine. 6. These results also suggest that the differential effects of hydralazine on the responses to alpha-adrenoceptor agonists may be due to differences in the amount of receptor reserve available available in this blood vessel for full agonists (noradrenaline, phenylephrine or methoxamine) and partial agonists (clonidine or BHT-920).

UI MeSH Term Description Entries
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D004730 Endothelium, Vascular Single pavement layer of cells which line the luminal surface of the entire vascular system and regulate the transport of macromolecules and blood components. Capillary Endothelium,Vascular Endothelium,Capillary Endotheliums,Endothelium, Capillary,Endotheliums, Capillary,Endotheliums, Vascular,Vascular Endotheliums
D005260 Female Females
D006830 Hydralazine A direct-acting vasodilator that is used as an antihypertensive agent. Hydrallazin,Apresoline,Apressin,Apressoline,Hydralazine Hydrochloride,Hydralazine mono-Hydrochloride,Hydrazinophthalazine,Nepresol,Hydralazine mono Hydrochloride,Hydrochloride, Hydralazine,mono-Hydrochloride, Hydralazine
D000316 Adrenergic alpha-Agonists Drugs that selectively bind to and activate alpha adrenergic receptors. Adrenergic alpha-Receptor Agonists,alpha-Adrenergic Receptor Agonists,Adrenergic alpha-Agonist,Adrenergic alpha-Receptor Agonist,Receptor Agonists, Adrenergic alpha,Receptor Agonists, alpha-Adrenergic,alpha-Adrenergic Agonist,alpha-Adrenergic Agonists,alpha-Adrenergic Receptor Agonist,Adrenergic alpha Agonist,Adrenergic alpha Agonists,Adrenergic alpha Receptor Agonist,Adrenergic alpha Receptor Agonists,Agonist, Adrenergic alpha-Receptor,Agonist, alpha-Adrenergic,Agonist, alpha-Adrenergic Receptor,Agonists, Adrenergic alpha-Receptor,Agonists, alpha-Adrenergic,Agonists, alpha-Adrenergic Receptor,Receptor Agonist, alpha-Adrenergic,Receptor Agonists, alpha Adrenergic,alpha Adrenergic Agonist,alpha Adrenergic Agonists,alpha Adrenergic Receptor Agonist,alpha Adrenergic Receptor Agonists,alpha-Agonist, Adrenergic,alpha-Agonists, Adrenergic,alpha-Receptor Agonist, Adrenergic,alpha-Receptor Agonists, Adrenergic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001013 Aorta, Thoracic The portion of the descending aorta proceeding from the arch of the aorta and extending to the DIAPHRAGM, eventually connecting to the ABDOMINAL AORTA. Aorta, Ascending,Aorta, Descending,Aortic Arch,Aortic Root,Arch of the Aorta,Descending Aorta,Sinotubular Junction,Ascending Aorta,Thoracic Aorta,Aortic Roots,Arch, Aortic,Ascending Aortas,Junction, Sinotubular,Root, Aortic,Sinotubular Junctions
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats

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