Lane Sd, Green Ce, Steinberg Jl, Ma L, Schmitz Jm, Rathnayaka N, Bandak Sd, Ferre S, Moeller Fg
Center for Neurobehavioral Research on Addiction, Department of Psychiatry and Behavioral Sciences, University of Texas Health Science Center at Houston, USA.
J Addict Res Ther. 2012 Mar 28;S1. doi: 10.4172/2155-6105.S1-009.
A(2A) receptor antagonists have been proposed as therapeutic tools for dopaminergically-relevant diseases, including Parkinson's disease and substance dependence. The acute subjective and cardiovascular effects of a novel, selective adenosine A(2A) receptor antagonist (SYN115) were examined. Across an 8-hour experimental testing day, 22 non-treatment seeking cocaine-dependent subjects received either placebo capsules (PO) at both the AM and PM dosing times (Plc/Plc, N = 9), or placebo in the AM and 100 mg SYN115 in the PM (Plc/SYN115, N =13). Cardiovascular measures (HR, BP) were obtained across the test day, and subjective effects (ARCI, VAS) were obtained once before and once after the AM and PM doses (four time points total). There were no between-group effects on cardiovascular function, however subjective effects consistent with stimulation were observed on the VAS scales in the SYN115 group. In cocaine-dependent subjects, SYN115 may produce stimulant-like effects through a unique mechanism of action. Due to known monoamine dysfunction related to chronic cocaine use, these effects may be specific to this population relative to healthy control or other patient populations.
A（2A）受体拮抗剂已被提议作为治疗与多巴胺能相关疾病的工具，包括帕金森病和物质依赖。研究了一种新型选择性腺苷A（2A）受体拮抗剂（SYN115）的急性主观和心血管效应。在一个长达8小时的实验测试日中，22名未寻求治疗的可卡因依赖者在上午和下午给药时间分别接受安慰剂胶囊（PO）（安慰剂/安慰剂组，N = 9），或上午接受安慰剂，下午接受100毫克SYN115（安慰剂/SYN115组，N = 13）。在整个测试日获取心血管指标（心率、血压），并在上午和下午给药前和给药后各获取一次主观效应（成瘾研究临床印象量表、视觉模拟量表）（共四个时间点）。两组之间在心血管功能上没有差异，但在SYN115组的视觉模拟量表上观察到了与兴奋一致的主观效应。在可卡因依赖者中，SYN115可能通过独特的作用机制产生类似兴奋剂的效应。由于已知与长期使用可卡因相关的单胺功能障碍，相对于健康对照或其他患者群体，这些效应可能对此人群具有特异性。
