Mutafova-Yambolieva V, Staneva-Stoytcheva D
Department of Experimental Pharmacology, Bulgarian Academy of Sciences, Sofia.
Methods Find Exp Clin Pharmacol. 1988 Sep;10(9):559-62.
The piperazinotetralin derivative P-11 applied in increasing concentrations (10(-12) to 10(-4)M) inhibited field electrical stimulation-induced contractions of isolated rabbit ear artery and this effect was not reversed by S-sulpiride (10(-6)M). This was probably due to the postsynaptic alpha receptor-blocking action of P-11. The compound also did not modify PGF2 alpha-induced contractions of isolated rabbit renal artery, suggesting the lack of action of P-11 on postsynaptic DA1 receptors. The lack of activity of P-11 on DA1 and DA2 peripheral receptors was associated with the chemical structure of the compound.
哌嗪并四氢萘衍生物P - 11在浓度逐渐增加(10⁻¹²至10⁻⁴M)时,可抑制离体兔耳动脉的场电刺激诱导收缩,且这种作用不会被S - 舒必利(10⁻⁶M)逆转。这可能是由于P - 11的突触后α受体阻断作用。该化合物也不会改变PGF2α诱导的离体兔肾动脉收缩,提示P - 11对突触后DA1受体无作用。P - 11对DA1和DA2外周受体缺乏活性与该化合物的化学结构有关。