Abstract：
The development of lysergic acid diethylamide (LSD) derivatives and analogs continues to inform the design of novel receptor probes and potentially new medicines. On the other hand, a number of newly developed LSD derivatives have also emerged as recreational drugs, leading to reports of their detection in some countries. One position in the ergoline scaffold of LSD that is frequently targeted is the N1-position; numerous N1-alkylcarbonyl LSD derivatives have been reported where the acyl chain is attached to the indole nitrogen, for example, in the form of linear n-alkane substituents, which represent higher homologs of the prototypical 1-acetyl-N,N-diethyllysergamide (1A-LSD, ALD-52). In this study, 1-hexanoyl-LSD (1H-LSD, SYN-L-027), a novel N1-acyl LSD derivative, was characterized analytically using standard techniques, followed by evaluation of its in vivo behavioral effects using the mouse head-twitch response (HTR) assay in C57BL/6J mice. 1H-LSD induced the HTR, with a median effective dose (ED50) of 192.4 μg/kg (equivalent to 387 nmol/kg), making it roughly equipotent to ALD-52 when tested previously under similar conditions. Similar to other N1-acylated analogs, 1H-LSD is anticipated to by hydrolyzed to LSD in vivo and acts as a prodrug. It is currently unknown whether 1H-LSD has appeared as on the research chemical market or is being used recreationally.
摘要：
麦角酰二乙胺（LSD）衍生物和类似物的开发继续为新型受体探针和潜在新药的设计提供信息。另一方面,许多新开发的LSD衍生物也成为娱乐性药物，导致在一些国家发现它们的报告。经常靶向的LSD麦角林支架中的一个位置是N1位置；已经报道了许多N1-烷基羰基LSD衍生物，其中酰基链连接到吲哚氮上，例如,以直链正烷烃取代基的形式，代表原型1-乙酰基-N的更高同系物，N-二乙基磺胺（1A-LSD，ALD-52)。在这项研究中,1-己酰基-LSD(1H-LSD,SYN-L-027),一种新的N1-酰基LSD衍生物，使用标准技术进行分析表征，然后在C57BL/6J小鼠中使用小鼠头部抽搐反应（HTR）测定法评估其体内行为效果。1H-LSD诱导HTR，中位有效剂量（ED50）为192.4μg/kg（相当于387nmol/kg），使其大致等效的ALD-52时，以前在类似的条件下测试。类似于其他N1-酰化类似物，预期1H-LSD在体内水解为LSD并充当前药。目前尚不清楚1H-LSD是否已经出现在研究化学品市场上或正在娱乐使用。
