Hart Damyan W, Alonso-Caraballo Yanaira, Hornback Britta, Robert Angel, Brickner Megan A, Esguerra Manuel, Childers Wayne E, Abou-Gharbia Magid, Thomas Mark J
Department of Neuroscience, University of Minnesota, Minneapolis, Minnesota, USA.
Medical Discovery Team on Addiction, University of Minnesota, Minneapolis, Minnesota, USA.
Brain Behav. 2025 Jul;15(7):e70616. doi: 10.1002/brb3.70616.
Despite the widespread impact of opioid use disorder, pharmacological options for treatment remain limited. Recent studies find that cocaine exposure decreases the expression of the glutamate transporter GLT-1 in the nucleus accumbens (NAc) and that treatment with the beta-lactam antibiotic ceftriaxone rescues this loss of expression and reduces cue-induced reinstatement to cocaine self-administration. The novel beta-lactam derivative MC-100093 (093) lacks antimicrobial properties but crosses the blood-brain barrier more rapidly and retains the beneficial effects of ceftriaxone following cocaine. However, 093 effects following oxycodone exposure have not been examined.
We used intravenous self-administration (IVSA) of oxycodone in rats to test if 093 can attenuate oxycodone seeking. Membrane expression of GLT-1 in the NAc was investigated using western blots. Conditioned place preference (CPP) was used to test the effect of oxycodone and cocaine alone on GLT-1 expression.
We find that 093 injections following IVSA of oxycodone in rats did not reduce cue-induced reinstatement. Interestingly, western blot analysis revealed that 093 failed to upregulate the expression of GLT-1 in the NAc of oxycodone-exposed animals. Follow-up CPP experiments suggest that oxycodone exposure alone does not decrease GLT-1 expression as cocaine does.
Our results indicate that drug-specific reductions in NAc GLT-1 expression may be necessary for 093's efficacy. Further investigation into 093 and other opioids is needed to fully understand their relationship with GLT-1 expression and beta-lactams.
尽管阿片类药物使用障碍具有广泛影响,但治疗的药理学选择仍然有限。最近的研究发现,接触可卡因会降低伏隔核(NAc)中谷氨酸转运体GLT-1的表达,而使用β-内酰胺抗生素头孢曲松治疗可挽救这种表达缺失,并减少线索诱导的可卡因自我给药复吸。新型β-内酰胺衍生物MC-100093(093)没有抗菌特性,但能更快穿过血脑屏障,并在接触可卡因后保留头孢曲松的有益效果。然而,尚未研究093在接触羟考酮后的作用。
我们在大鼠中使用羟考酮静脉自我给药(IVSA)来测试093是否能减弱对羟考酮的寻求行为。使用蛋白质免疫印迹法研究NAc中GLT-1的膜表达。条件性位置偏爱(CPP)用于测试单独使用羟考酮和可卡因对GLT-1表达的影响。
我们发现,在大鼠中对羟考酮进行IVSA后注射093并没有减少线索诱导的复吸。有趣的是,蛋白质免疫印迹分析显示,093未能上调接触羟考酮动物的NAc中GLT-1的表达。后续的CPP实验表明,单独接触羟考酮不会像可卡因那样降低GLT-1的表达。
我们的结果表明,NAc中GLT-1表达的药物特异性降低可能是093发挥疗效所必需的。需要对093和其他阿片类药物进行进一步研究,以充分了解它们与GLT-1表达和β-内酰胺的关系。