Barber D A, Tackett R L
Cardiovascular Pharmacodynamics Laboratory, College of Pharmacy, University of Georgia, Athens 30602.
Life Sci. 1992;51(16):1269-76. doi: 10.1016/0024-3205(92)90016-i.
Norcocaine is the N-demethylated metabolite of cocaine. It is present in the CNS and is reported to be pharmacologically active. The present study was designed to evaluate the cardiovascular actions of norcocaine following central administration. Wistar Kyoto (WKY) rats were anesthetized with pentobarbital and instrumented for measurement of blood pressure and renal and hindlimb blood flow (via Doppler flowprobes). A cerebroventricular cannula was placed in the lateral ventricle for drug administration. Cocaine or norcocaine was administered centrally in a dose range of 0.025 to 4.0 mg/kg. Under the above experimental conditions, 4.0 mg/kg of norcocaine decreased blood pressure without a significant change in either hind limb or renal blood flow. Central administration of cocaine also produced a similar depressor response. In conscious, unrestrained rats, cocaine produced a pressor response while norcocaine did not significantly alter blood pressure. The depressor response to both cocaine and norcocaine in the anesthetized animal is speculated to be due to the local anesthetic properties of the drugs.
去甲可卡因是可卡因的N-去甲基代谢产物。它存在于中枢神经系统中，据报道具有药理活性。本研究旨在评估中枢给药后去甲可卡因的心血管作用。用戊巴比妥麻醉Wistar Kyoto（WKY）大鼠，并安装测量血压以及肾和后肢血流量的仪器（通过多普勒血流探头）。将脑室套管置于侧脑室用于给药。可卡因或去甲可卡因以0.025至4.0mg/kg的剂量范围进行中枢给药。在上述实验条件下，4.0mg/kg的去甲可卡因可降低血压，而后肢或肾血流量均无明显变化。中枢给予可卡因也产生了类似的降压反应。在清醒、不受约束的大鼠中，可卡因产生升压反应，而去甲可卡因未显著改变血压。推测麻醉动物对可卡因和去甲可卡因的降压反应是由于药物的局部麻醉特性。
