Higgins Guy A, Carroll Nicole K, Brown Matt, MacMillan Cam, Silenieks Leo B, Thevarkunnel Sandy, Izhakova Julia, Magomedova Lilia, DeLannoy Ines, Sellers Edward M
InterVivo Solutions Inc., Fergus, ON, Canada.
Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON, Canada.
Front Pharmacol. 2021 Feb 26;12:640241. doi: 10.3389/fphar.2021.640241. eCollection 2021.
Long term benefits following short-term administration of high psychedelic doses of serotonergic and dissociative hallucinogens, typified by psilocybin and ketamine respectively, support their potential as treatments for psychiatric conditions such as major depressive disorder. The high psychedelic doses induce perceptual experiences which are associated with therapeutic benefit. There have also been anecdotal reports of these drugs being used at what are colloquially referred to as "micro" doses to improve mood and cognitive function, although currently there are recognized limitations to their clinical and preclinical investigation. In the present studies we have defined a low dose and plasma exposure range in rats for both ketamine (0.3-3 mg/kg [10-73 ng/ml]) and psilocybin/psilocin (0.05-0.1 mg/kg [7-12 ng/ml]), based on studies which identified these as sub-threshold for the induction of behavioral stereotypies. Tests of efficacy were focused on depression-related endophenotypes of anhedonia, amotivation and cognitive dysfunction using low performing male Long Evans rats trained in two food motivated tasks: a progressive ratio (PR) and serial 5-choice (5-CSRT) task. Both acute doses of ketamine (1-3 mg/kg IP) and psilocybin (0.05-0.1 mg/kg SC) pretreatment increased break point for food (PR task), and improved attentional accuracy and a measure of impulsive action (5-CSRT task). In each case, effect size was modest and largely restricted to test subjects characterized as "low performing". Furthermore, both drugs showed a similar pattern of effect across both tests. The present studies provide a framework for the future study of ketamine and psilocybin at low doses and plasma exposures, and help to establish the use of these lower concentrations of serotonergic and dissociative hallucinogens both as a valid scientific construct, and as having a therapeutic utility.
分别以裸盖菇素和氯胺酮为代表的血清素能和分离性致幻剂高剂量短期给药后的长期益处,支持了它们作为治疗重度抑郁症等精神疾病的潜在药物。高剂量致幻剂会引发与治疗益处相关的感知体验。也有传闻称,这些药物以通俗所说的“微剂量”使用时,可改善情绪和认知功能,不过目前其临床和临床前研究存在公认的局限性。在本研究中,我们基于确定这些剂量低于诱发行为刻板症阈值的研究,确定了大鼠体内氯胺酮(0.3 - 3毫克/千克[10 - 73纳克/毫升])和裸盖菇素/脱磷酸裸盖菇素(0.05 - 0.1毫克/千克[7 - 12纳克/毫升])的低剂量和血浆暴露范围。疗效测试集中于使用表现不佳的雄性长爪沙鼠进行两项食物动机任务训练后出现的与抑郁相关的内表型,即快感缺失、动机缺乏和认知功能障碍:渐进比率(PR)任务和系列5选(5 - CSRT)任务。急性剂量的氯胺酮(1 - 3毫克/千克腹腔注射)和裸盖菇素(0.05 - 0.1毫克/千克皮下注射)预处理均增加了获取食物的断点(PR任务),并提高了注意力准确性和冲动行为指标(5 - CSRT任务)。在每种情况下,效应大小适中,且主要限于被归类为“表现不佳”的测试对象。此外,两种药物在两项测试中均呈现出相似的效应模式。本研究为未来低剂量和血浆暴露情况下氯胺酮和裸盖菇素的研究提供了框架,并有助于确立使用这些较低浓度的血清素能和分离性致幻剂作为一种有效的科学构建,以及具有治疗效用。