普萘洛尔对[3H]5-羟色胺结合位点及5-羟色胺自身受体的立体选择性阻断作用。
Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol.
作者信息
Middlemiss D N
出版信息
Eur J Pharmacol. 1984 Jun 1;101(3-4):289-93. doi: 10.1016/0014-2999(84)90173-0.
(-)-Propranolol displaced 5-HT1 and 5-HT1B receptor binding (pIC50 6.76 and 6.31 respectively) and antagonized the inhibitory effect of 5-HT on continuous K+ (25 mM) evoked release of [3H]5-HT from superfused rat frontal cortex slices (apparent pA2 6.67). (+)-Propranolol was essentially inactive in all tests. The results support the claim that the 5-HT autoreceptor has a pharmacological resemblance to the 5-HT1 recognition site and in particular to the low affinity 5-HT1B subtype of this site.
（-）-普萘洛尔可取代5-HT1和5-HT1B受体结合（pIC50分别为6.76和6.31），并拮抗5-HT对持续钾离子（25 mM）诱发的[3H]5-HT从灌流大鼠额叶皮质切片中释放的抑制作用（表观pA2为6.67）。（+）-普萘洛尔在所有测试中基本无活性。这些结果支持了5-HT自身受体在药理学上与5-HT1识别位点相似，特别是与该位点的低亲和力5-HT1B亚型相似的观点。
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