Pharmacological Characterization of Compounds Containing the Pyrimidinone Ring on ? 1-Adrenergic Receptors in Aorta Of Rats

Pharmacological Characterization of Compounds Containing the Pyrimidinone Ring on ? 1-Adrenergic Receptors in Aorta Of Rats

• Autor
• Silvia Maria Luna Alves
• Co-autores
• Sidiane Barros da Silva , Wellington Francisco Pereira da Silva , Ruth Cristina Albuquerque dos Santos , Janaína Versiani dos Anjos , Alice Valença Araújo
• Resumo

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  Systemic Arterial Hypertension is an important public health problem and despite advances in antihypertensive therapy, most of the hypertensive individuals do not achieve adequate blood pressure levels. Pyrimidinone ring compounds may becandidates for antihypertensive drugs, since they antagonize ?1-adrenergic receptors, a targetfor antihypertensive drugs, such as prazosin. The aim of this study was to characterize the effects of SPRM09 e SPRM12, pyrimidinone ring compounds, on ?1-adrenergic receptors in rat aortas. Aortic rings with or without endothelium from Wistar rats (2-3 months) were mounted in an organ bath and their responses were recorded in an acquisition system. The cumulative concentration-effect curves for phenylephrine were constructed in the absence or in the presence of SPRM09 or SPRM12 (0.1 mmol/L). This study was approved by CEUA-UFPE (021446/2013-12). SPRM09 and SPRM12 reduced phenylephrine Emax only in aortas with endothelium (Control: Emax = 1.71±0.22g; pD2 = 7.45 ± 0.23, n = 7; + SPRM09: Emax = 1.13±0.18g; pD2 = 7.32 ± 0.32, n = 7, p <0.05; Control: Emax = 1.97±0.18g; pD2 = 7.4±0.20, n = 7; + SPRM12: Emax = 1.29±0.20 g; pD2 = 6.86±0.16, n = 7), but not in those without endothelium (Control: Control max = 2.27±0.16g; pD2 = 7.67 ± 0.65, n = 7; + SPRM09: Emax = 2.18±0.23g; pD2 = 7.93±0.35, n = 7, p> 0.05; + SPRM12: Emax = 2.08±0.20 g; pD2 = 7.62±0.19, n = 6). It is then suggested that the compounds are not antagonists of ?1-adrenergic receptors, but they may be ?2-adrenergic agonists.

   

• Palavras-chave
• Hypertension, receptors, alpha-adrenergic
• Modalidade
• Pôster
• Área Temática
• Sinalização celular