Tricyclic antidepressants: therapeutic properties and affinity for alpha-noradrenergic receptor binding sites in the brain.
Tricyclic antidepressants: therapeutic properties and affinity for alpha-noradrenergic receptor binding sites in the brain.
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三环类抗抑郁药：治疗特性和对大脑中α-去甲肾上腺素能受体结合位点的亲和力。
DOI：
10.1126/science.202024
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发表时间：
1978
期刊：
影响因子：
56.9
通讯作者：
SolomonH Snyder
中科院分区：
文献类型：
--
作者：
D. U'prichard;D. Greenberg;P. Sheehan;SolomonH Snyder
三环类抗抑郁药在引起精神运动激活、缓解激动抑郁状态以及引起镇静和低血压方面的能力各不相同。我们量化了三环抗抑郁药在竞争3h标记的WB-4101与大鼠脑膜α -去甲肾上腺素能受体位点结合时的相对效力。三环类药物对大脑α -去甲肾上腺素能受体的亲和力与这些药物缓解精神运动性躁动、诱导镇静和低血压的能力密切相关；这些亲和力也与引发精神运动激活的倾向呈负相关。
Tricyclic antidepressants vary in their capacity to cause psychomotor activation, to relieve agitated depressive states, and to cause sedation and hypotension. We have quantified relative potencies of tricyclic antidepressants in competing for the binding of 3H-labeled WB-4101 to alpha-noradrenergic receptor sites in rat brain membranes. Affinities of tricyclic drugs for alpha-noradrenergic receptor sites in the brain correlate well with the capacity of these agents to relieve psychomotor agitation and to induce sedation and hypotension; these affinities also correlate inversely with tendencies to elicit psychomotor activation.