Choppin A, O'Connor S E
Synthélabo Recherche (L.E.R.S.), Department of Biology, Bagneux, France.
Eur J Pharmacol. 1993 Feb 16;231(3):469-72. doi: 10.1016/0014-2999(93)90126-3.
Rabbit renal arteries were virtually unresponsive to 5-hydroxytryptamine (5-HT) and 5-carboxamidotryptamine (5-CT) under control conditions (including the presence of ketanserin 10(-6) M). However, both agents produced prominent contractions over the range 10(-9)-10(-5) M in tissues pre-contracted with threshold concentrations of either histamine or U46619. These responses were considered to be mediated by activation of 5-HT1-like receptors based on the potency order 5-CT > or = 5-HT and the sensitivity of agonist responses to antagonism by methiothepin (10(-7) M). Pre-contraction with different types of vasoconstrictor can therefore unmask functional 5-HT1-like receptors in rabbit renal artery.
在对照条件下(包括存在10⁻⁶ M酮色林),兔肾动脉对5-羟色胺(5-HT)和5-羧酰胺色胺(5-CT)几乎无反应。然而,在预先用组胺或U46619的阈浓度预收缩的组织中,这两种药物在10⁻⁹ - 10⁻⁵ M范围内均产生明显收缩。基于效价顺序5-CT≥5-HT以及激动剂反应对甲硫噻平(10⁻⁷ M)拮抗作用的敏感性,这些反应被认为是由5-HT1样受体激活介导的。因此,用不同类型的血管收缩剂进行预收缩可以揭示兔肾动脉中功能性5-HT1样受体。