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d-尼古丁对豚鼠和兔离体气管和支气管中1-异构体诱发反应的抑制作用。

Inhibitory effects of d-nicotine on the responses evoked by 1-isomer in trachea and bronchus isolated from guinea-pig and rabbit.

作者信息

Funayama N, Shinkai M, Takayanagi I

机构信息

Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.

出版信息

Gen Pharmacol. 1995 Sep;26(5):977-81. doi: 10.1016/0306-3623(94)00294-w.

Abstract
  1. The effects of d-nicotine on the responses induced by 1-isomer were studied in tracheae and bronchi isolated from guinea-pigs and rabbits. In guinea-pigs trachea 1-nicotine produced a biphasic response consisting of initial contraction and following relaxation. In other airway preparations 1-nicotine produced only contraction. 2. d-Nicotine did not produce any responses except for the case of guinea-pig trachea. d-isomer produced only relaxation and relative potency was approximately 0.44 in guinea-pig trachea. 3. Pretreatment with d-nicotine (30-300 microM) reduced concentration response curves for 1-isomer in a non-competitive manner in all preparations used in this study. 4. 1-nicotine at the concentration of 3 microns, which did not produce any response itself, reduced the concentration response curve of 1-nicotine in guinea-pig trachea. 5. Inhibition by d-nicotine or 1-nicotine (3 microM) of the concentration-response curve of 1-nicotine may be due to desensitization of nicotine receptors.
摘要
  1. 在从豚鼠和兔子分离出的气管和支气管中研究了d-尼古丁对1-异构体诱导反应的影响。在豚鼠气管中,1-尼古丁产生双相反应,包括初始收缩和随后的舒张。在其他气道制剂中,1-尼古丁仅产生收缩。2. 除豚鼠气管外,d-尼古丁未产生任何反应。d-异构体仅产生舒张,在豚鼠气管中的相对效价约为0.44。3. 用d-尼古丁(30 - 300微摩尔)预处理以非竞争性方式降低了本研究中使用的所有制剂中1-异构体的浓度反应曲线。4. 浓度为3微米的1-尼古丁本身不产生任何反应,但降低了豚鼠气管中1-尼古丁的浓度反应曲线。5. d-尼古丁或1-尼古丁(3微米)对1-尼古丁浓度反应曲线的抑制可能是由于尼古丁受体的脱敏。

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