2-(4 '-aminobenzenamine)-pyrimidine, a new alpha-antagonist from Autonoe madeirensis

TY - JOUR

T1 - 2-(4 '-aminobenzenamine)-pyrimidine, a new alpha-antagonist from Autonoe madeirensis

AU - Dias, C

AU - Paulo, A

AU - Nascimento, J

AU - Houghton, P

AU - Hawkes, J E

AU - Goncalves, M L

PY - 2003

Y1 - 2003

N2 - A new natural pyrimidine derivative, 2-(4'-aminobenzenamine)pyrimidine (1), was isolated from the bulbs of Autonoe madeirensis, a Hyacinthaceae of the Madeira Archipelago (Portugal) and the structure determined on the basis of spectroscopic data. As some pyrimidine compounds are important alpha(1)-adrenergic antagonists, we investigated the effect of 1 on rat vas deferens contractility induced by the alpha(1)-agonist phenylephrine. In concentrations virtually devoid of effect on the rat vas deferens contractility, 1 shifted to the right the concentration-response curves of phenylephrine without changing the maximal effect. These results provide evidence that 1 acts as an alpha(1)-adrenoceptor antagonist and suggest a competitive mechanism of action.

AB - A new natural pyrimidine derivative, 2-(4'-aminobenzenamine)pyrimidine (1), was isolated from the bulbs of Autonoe madeirensis, a Hyacinthaceae of the Madeira Archipelago (Portugal) and the structure determined on the basis of spectroscopic data. As some pyrimidine compounds are important alpha(1)-adrenergic antagonists, we investigated the effect of 1 on rat vas deferens contractility induced by the alpha(1)-agonist phenylephrine. In concentrations virtually devoid of effect on the rat vas deferens contractility, 1 shifted to the right the concentration-response curves of phenylephrine without changing the maximal effect. These results provide evidence that 1 acts as an alpha(1)-adrenoceptor antagonist and suggest a competitive mechanism of action.

M3 - Article

VL - 69

SP - 1060

EP - 1062

JO - Planta Medica

JF - Planta Medica

IS - 11

ER -