Lal J, Krutak-Krol H, Domino E F
Arzneimittelforschung. 1986 Jul;36(7):1075-8.
The possible antitussive effects of dextrorphan (the (+) isomer of levorphanol) and phencyclidine (PCP) were compared to well known antitussive properties of dextromethorphan in the post-halothane anesthetized decerebrate cat in which cough was elicited by direct electrical stimulation of the cough center. Dextrorphan, when injected i.a. (0.05-0.32 mg kg-1) or i.v. (1 to 3 mg kg-1), PCP i.a. (0.1-0.32 mg kg-1) or i.v. (1.0 mg kg-1) had no effect on electrically elicited cough. After i.v. administration, dextrorphan caused a variable effect on respiration but did not have any respiratory effect with i.a. administration of the drug. PCP injection i.a. at 0.32 mg kg-1 severely inhibited respiration though coughing could still be elicited. But i.v. administration of 1.0 mg/kg-1 suppressed both cough and respiration for several hours. Dextromethorphan inhibited cough upon both i.a. and i.v. injection. The mean effective i.a. dose was 0.063 mg kg-1. A ten times higher dose was necessary (0.65 mg kg-1) for cough suppression by the i.v. route. It is concluded from the i.a./i.v. ratio that dextromethorphan has specific central antitussive activity not possessed by dextrorphan and PCP.
在氟烷麻醉后的去大脑猫中,通过直接电刺激咳嗽中枢引发咳嗽,比较了右啡烷(左啡诺的(+)异构体)和苯环己哌啶(PCP)可能的镇咳作用与右美沙芬已知的镇咳特性。右啡烷腹腔注射(0.05 - 0.32毫克/千克)或静脉注射(1至3毫克/千克)、PCP腹腔注射(0.1 - 0.32毫克/千克)或静脉注射(1.0毫克/千克)对电诱发的咳嗽均无影响。静脉给药后,右啡烷对呼吸有不同影响,但腹腔给药时对呼吸无任何影响。腹腔注射0.32毫克/千克的PCP虽仍能诱发咳嗽,但严重抑制呼吸。而静脉注射1.0毫克/千克则会在数小时内同时抑制咳嗽和呼吸。右美沙芬腹腔注射和静脉注射均能抑制咳嗽。腹腔注射的平均有效剂量为0.063毫克/千克。通过静脉途径抑制咳嗽则需要高十倍的剂量(0.65毫克/千克)。从腹腔注射/静脉注射的剂量比得出结论,右美沙芬具有右啡烷和PCP所不具备的特异性中枢镇咳活性。