Siever L J, Kafka M S, Insel T R, Lake C R, Murphy D L
Psychiatry Res. 1983 May;9(1):37-44. doi: 10.1016/0165-1781(83)90087-2.
Platelet alpha 2-adrenergic receptor number and physiologic responsiveness, as well as plasma norepinephrine (NE), were evaluated in psychiatric patients with major depressive disorder before and during chronic clorgyline treatment. The alpha 2-adrenergic receptor number was determined by measuring the binding of tritiated dihydroergocriptine (3H-DHE) to platelet membranes. Physiologic responsiveness was determined by measuring the response of cyclic adenosine 3'-5'-monophosphate (cAMP) to prostaglandin E1 (PGE1), and the inhibition of the PGE1-stimulated cAMP response by NE in intact platelets. No significant differences from pretreatment values were observed in platelet alpha 2-adrenergic binding or responsiveness during clorgyline treatment. Baseline platelet cAMP production and plasma NE levels were significantly decreased after chronic clorgyline treatment. Previous studies on animals and humans have suggested that brain alpha 2-adrenergic receptor responsiveness decreases during chronic clorgyline treatment. The present findings therefore suggest that such changes may represent adaptations induced by long-term clorgyline administration which may differ between the brain and the platelet, thus illustrating potential limitations of the study of platelet alpha 2-adrenergic receptors as a model for central alpha 2-adrenergic receptor adaptation.
在患有重度抑郁症的精神科患者中，于慢性氯吉兰治疗前及治疗期间，对血小板α2-肾上腺素能受体数量、生理反应性以及血浆去甲肾上腺素（NE）进行了评估。通过测量氚标记双氢麦角隐亭（3H-DHE）与血小板膜的结合来确定α2-肾上腺素能受体数量。通过测量环磷酸腺苷（cAMP）对前列腺素E1（PGE1）的反应以及NE对完整血小板中PGE1刺激的cAMP反应的抑制作用来确定生理反应性。在氯吉兰治疗期间，血小板α2-肾上腺素能结合或反应性与治疗前值相比未观察到显著差异。慢性氯吉兰治疗后，基线血小板cAMP产生和血浆NE水平显著降低。先前对动物和人类的研究表明，在慢性氯吉兰治疗期间脑α2-肾上腺素能受体反应性降低。因此，目前的研究结果表明，此类变化可能代表长期给予氯吉兰所诱导的适应性改变，而这种改变在脑和血小板之间可能有所不同，从而说明了将血小板α2-肾上腺素能受体研究作为中枢α2-肾上腺素能受体适应性模型的潜在局限性。
