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Ivorra M.D., Valiente M., Martínez S., Madrero Y., M.A. Noguera, Cassels B.K., Sobarzo E.M., D’Ocon P. 8-NH2-Boldine, an Antagonist of alpha1A and alpha1B Adrenoceptors without Affinity for the alpha1D Subtype: Structural Requirements for Aporphines at alpha1-Adrenoceptor Subtypes. Planta Med. 2005 Oct; 71 (10): 897-903 16254819 (P,S,G,E,B,D). Abstract: Structure-activity analysis of 21 aporphine derivatives was performed by examining their affinities for cloned human alpha (1A), alpha (1B) and alpha (1D) adrenoceptors (AR) using membranes prepared from rat-1 fibroblasts stably expressing each alpha (1)AR subtype. All the compounds tested competed for [(125)I]-HEAT binding with steep andmonophasic curves. The most interesting compound was 8-NH (2)-boldine, which retains the selective affinity for alpha(1A)-AR (pKi = 6.37 +/- 0.21) vs. alpha(1B)- AR (pKi = 5.53 +/- 0.11) exhibited by 1,2,9,10-tetraoxygenated aporphines, but shows low affinity for alpha(1D)-AR (pKi < 2.5). Binding studies on native adrenoceptors present in rat cerebral cortex confirms the results obtained for human cloned alpha (1)-AR subtypes. The compounds selective for the alpha (1A) subtype discriminate two binding sites in rat cerebral cortex confirming a mixed population of alpha (1A)- and alpha (1B)-AR in this tissue. All compounds are more selective as inhibitors of [ (3)H]-prazosin binding than of [ (3)H]-diltiazem binding to rat cerebral cortical membranes. A close relationship was found between affinities obtained for cloned alpha (1A)-AR and inhibitory potencies on noradrenaline-induced contraction or inositol phosphate accumulation in tail artery, confirming that there is a homogeneous functional population of alpha(1A)-AR in this vessel. On the contrary, a poor correlation seems to exist between the affinity of 8-NH (2)-boldine for cloned alpha (1D)-AR and its potency as an inhibitor of noradrenalineinduced contraction or inositol phosphate accumulation in rat aorta, which confirms that a heterogeneous population of alpha (1)-AR mediates the adrenergic response in this vessel.
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Ruiz A. T. G., Taffarello D., SouzaI V. H. S., CarvalhoI J. E., Pharmacology and toxicology of Peumus boldus and Baccharis genistelloides. Rev. bras. farmacogn. vol.18 no.2 João Pessoa Apr./June 2008. Abstract: There are a great number of medicinal plants without any scientific confirmation about their efficacy and safety. This paper is a short review about two medicinal plants, "boldo do chile" (Peumus boldus) and "carqueja" (Baccharis genistelloides). Pharmacological studies have confirmed several popular indications for P. boldus and B. genistelloides, besides have established a relationship between isolated compounds from these extracts and the pharmacological effects observed. On the other hand, toxicological researches have pointed out that P. boldus tea should not be consumed during a long period (potential hepatotoxicity) and by pregnant, especially during the first three months. Moreover, B. genistelloides tea must be prohibited for pregnant because of confirmed abortive action, and for patients using medicines for blood pressure disorders. These studies point out the continuous necessity of more studies about medicinal plants; only with this knowledge it will be possible a safe and efficient use.
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