Mason G A, Walker C H, Little K Y
Department of Psychiatry, School of Medicine, University of North Carolina at Chapel Hill 27599-7250.
Psychopharmacology (Berl). 1993;110(1-2):110-4. doi: 10.1007/BF02246958.
The effects of seven consecutive daily injections of desmethylimipramine (DMI 20 mg/kg) and propranolol (PRO 10 mg/kg) on 3H-dihydroalprenolol (3H-DHA) and 3H-ketanserin (3H-KET) binding in rat brain were examined. Analyses of saturation binding data using the iterative, nonlinear curve-fitting program LIGAND revealed that PRO increased, while DMI reduced, 3H-DHA binding site density in cerebral cortex without altering receptor affinity, as previously reported. DMI reduced 3H-KET binding site density without changing affinity, and PRO produced the same effect. In cerebral cortex and probably in hippocampus and striatum, DMI and PRO administered together increased the density of 3H-DHA binding sites (beta-adrenergic receptors) and reduced their affinity. This combination of drugs reduced the density of 3H-KET binding sites (5-HT2 receptors) in cerebral cortex, but did not change their affinity. These findings indicate a need for additional studies on the interactions of DMI and PRO and related drugs because of implications for the treatment of depressed patients with cardiovascular disorders.
研究了连续7天每日注射去甲丙咪嗪（DMI，20毫克/千克）和普萘洛尔（PRO，10毫克/千克）对大鼠脑内3H-二氢阿普洛尔（3H-DHA）和3H-酮色林（3H-KET）结合的影响。使用迭代非线性曲线拟合程序LIGAND对饱和结合数据进行分析，结果显示，如先前报道的那样，PRO增加而DMI降低了大脑皮质中3H-DHA结合位点的密度，且不改变受体亲和力。DMI降低了3H-KET结合位点的密度但不改变亲和力，PRO也产生了相同的效果。在大脑皮质以及可能在海马体和纹状体中，一起给予DMI和PRO会增加3H-DHA结合位点（β-肾上腺素能受体）的密度并降低其亲和力。这种药物组合降低了大脑皮质中3H-KET结合位点（5-HT2受体）的密度，但不改变其亲和力。这些发现表明，由于对患有心血管疾病的抑郁症患者的治疗有影响，需要对DMI和PRO以及相关药物的相互作用进行更多研究。
