Walsh S L, Gilson S F, Jasinski D R, Stapleton J M, Phillips R L, Dannals R F, Schmidt J, Preston K L, Grayson R, Bigelow G E
Department of Psychiatry, Johns Hopkins University School of Medicine, Baltimore, MD.
Neuropsychopharmacology. 1994 May;10(3):157-70. doi: 10.1038/npp.1994.18.
Buprenorphine is a mixed opioid agonist-antagonist, which acts as a partial mu agonist and a kappa antagonist. The present study evaluated the acute effects of buprenorphine on cerebral glucose metabolism (CMRglc) in six human substance abusers using a double-blind, placebo-controlled, counterbalanced, crossover design. Each subject participated in two positron emission tomographic (PET) studies, 1 week apart, following the injection of buprenorphine (1 mg, intramuscularly) and placebo. Buprenorphine significantly reduced CMRglc and the regional cerebral metabolic rate for glucose (rCMRglc) by up to 32% in all but three of 22 bilateral and in 4 midline regions (p < .05). No region showed an increase in rCMRglc. Buprenorphine also produced miosis, respiratory depression, and subjective ratings of euphoria and sedation in comparison to placebo (p < .05). These observations extend previous findings of reduced CMRglc following acute treatment with morphine and other nonopioid euphorigenic drugs.
丁丙诺啡是一种混合阿片类激动剂-拮抗剂，它作为一种部分μ激动剂和κ拮抗剂发挥作用。本研究采用双盲、安慰剂对照、平衡、交叉设计，评估了丁丙诺啡对6名人类药物滥用者脑葡萄糖代谢（CMRglc）的急性影响。在注射丁丙诺啡（1毫克，肌肉注射）和安慰剂后，每名受试者相隔1周参与两项正电子发射断层扫描（PET）研究。丁丙诺啡使22个双侧区域中的22个区域以及4个中线区域中的3个区域外的所有区域的CMRglc和局部脑葡萄糖代谢率（rCMRglc）显著降低高达32%（p <.05）。没有区域显示rCMRglc增加。与安慰剂相比，丁丙诺啡还产生了瞳孔缩小、呼吸抑制以及欣快感和镇静的主观评分（p <.05）。这些观察结果扩展了先前关于吗啡和其他非阿片类致欣快药物急性治疗后CMRglc降低的研究发现。
