3,4-二羟基苯-α-甲基丙氨酸（α-甲基多巴）的药理作用，一种5-羟色氨酸脱羧酶抑制剂。
The pharmacological actions of 3,4-dihydroxyphenyl-alpha-methylalanine (alpha-methyldopa), an inhibitor of 5-hydroxytryptophan decarboxylase.
作者信息
SMITH S E
出版信息
Br J Pharmacol Chemother. 1960 Jun;15(2):319-27. doi: 10.1111/j.1476-5381.1960.tb01251.x.
alpha-Methyldopa (3,4-dihydroxyphenyl-alpha-methylalanine) is an inhibitor of 5-hydroxytryptophan decarboxylase which is effective in vitro and in vivo. The inhibition is complex and shows coenzyme reversal. Evidence is presented that it acts by coenzyme inactivation. Its administration to mice reduced brain 5-hydroxytryptamine but had no effect on noradrenaline. After repeated doses, intestinal 5-hydroxytryptamine concentrations were also reduced. Co-ordinated activity was diminished coincidently with the enzyme inhibition and the reduction in brain 5-hydroxytryptamine. Rectal temperatures were reduced and the possibility that this resulted from inactivity is discussed. Treated animals showed miosis and narrowing of the palpebral fissures. A comparison is drawn between the actions of alpha-methyldopa and reserpine. The present results support the idea that the sedative effects of both drugs are due to the fall in brain 5-hydroxytryptamine concentration that they produce.
α-甲基多巴（3,4-二羟基苯基-α-甲基丙氨酸）是5-羟色氨酸脱羧酶的抑制剂，在体内外均有效。这种抑制作用很复杂，表现出辅酶逆转。有证据表明它是通过辅酶失活起作用的。给小鼠服用它会降低脑内5-羟色胺，但对去甲肾上腺素没有影响。重复给药后，肠道内5-羟色胺浓度也会降低。协调活动随着酶抑制和脑内5-羟色胺的减少而同时减弱。直肠温度降低，并讨论了这是否是由于活动减少所致。经治疗的动物出现瞳孔缩小和睑裂变窄。对α-甲基多巴和利血平的作用进行了比较。目前的结果支持这样一种观点，即这两种药物的镇静作用都是由于它们所导致的脑内5-羟色胺浓度下降。
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