DeMarinis R M, Lavanchy P, Hieble J P, Jim K F, Matthews W D
J Med Chem. 1985 Feb;28(2):245-8. doi: 10.1021/jm00380a017.
N-[2-Hydroxy-5-[2-(methylamino)ethyl]phenyl]methanesulfonamide (SK&F 102652) has been prepared and characterized pharmacologically. It is a potent agonist with an EC50 of 25 nM at alpha 1-adrenoceptors as determined in the isolated perfused rabbit ear artery. On the presynaptic alpha 2-adrenoceptors of the guinea pig atrium it was considerably weaker, demonstrating an EC50 for inhibition of neurotransmission of 1200 nM and thus an overall alpha 1/alpha 2 selectivity ratio of greater than or equal to 48. In the vascular smooth muscle of the canine saphenous vein an EC100 concentration of this agonist in the presence of zero external Ca2+ induced 37.9 +/- 1.4% of the maximal contractile response due to this agent while the endogenous ligand norepinephrine evoked only 14.5 +/- 0.4% of the maximum. In the presence of low (1 microM) external calcium, this agent produced 78.3 +/- 5.3% of maximum while norepinephrine gave 45.3 +/- 7.4%. This agent produces alpha 1-adrenoceptor-mediated contraction primarily by release of intracellular Ca2+ and should provide a useful tool for characterizing alpha 1-receptor subtypes.
N-[2-羟基-5-[2-(甲氨基)乙基]苯基]甲磺酰胺（SK&F 102652）已被制备并进行了药理学表征。在离体灌注兔耳动脉中测定，它是一种强效激动剂，在α1肾上腺素受体处的EC50为25 nM。在豚鼠心房的突触前α2肾上腺素受体上，它的活性要弱得多，抑制神经传递的EC50为1200 nM，因此总的α1/α2选择性比值大于或等于48。在犬隐静脉的血管平滑肌中，在零外源性Ca2+存在的情况下，该激动剂的EC100浓度诱导出该药物最大收缩反应的37.9±1.4%，而内源性配体去甲肾上腺素仅诱发最大反应的14.5±0.4%。在低（1μM）外源性钙存在的情况下，该药物产生最大反应的78.3±5.3%，而去甲肾上腺素产生45.3±7.4%。该药物主要通过释放细胞内Ca2+产生α1肾上腺素受体介导的收缩，应为表征α1受体亚型提供一个有用的工具。
