EFFECTS OF PHENCYCLIDINE AND ITS DERIVATIVES ON ENTERIC NEURONES
EFFECTS OF PHENCYCLIDINE AND ITS DERIVATIVES ON ENTERIC NEURONES
复制标题
苯环利定及其衍生物对肠神经元的影响
DOI：
--
复制
发表时间：
1982
影响因子：
7.3
通讯作者：
S. Zukin
中科院分区：
文献类型：
--
作者：
A. Gintzler;R. Zukin;S. Zukin
1测定N-（1-苯基环己基）哌啶（PCP）及相关药物对豚鼠离体完整回肠的作用。2 1-1-（2-噻吩基）环己基哌啶（TCP）、PCP和氯胺酮降低了离体豚鼠回肠完整节段电诱导收缩（0.1 Hz）的高度。3单纯麻醉性拮抗剂纳洛酮预处理可使收缩高度（0.1Hz）的抑制逆转30%~ 40%。该纳洛酮可逆组分显示与吗啡交叉耐受。4 PCP预处理导致乙酰胆碱（ACh）的剂量反应曲线向右移动，与对照剂量反应曲线不平行。因此，PCP不会以严格的阿托品样竞争方式与毒蕈碱胆碱受体相互作用。在豚鼠纵行肌-肌间神经丛制备物的匀浆中检测到5个[3 H]-PCP结合位点。[6]与[3 H]-五氯苯酚竞争结合的各种五氯苯酚衍生物的亲和力常数和效力排序表明，这些结合位点与中枢神经系统中发现的结合位点非常相似。7这些数据表明，豚鼠离体回肠可用作研究苯环己哌啶作用机制的体外系统。
1 The effects of N‐(1‐phenylcyclohexyl) piperidine (PCP) and related drugs on isolated intact segments of the guinea‐pig ileum were determined. 2 1–1‐(2‐Thienyl) cyclohexylpiperidine (TCP), PCP and ketamine decreased the height of electrically induced contractions (0.1 Hz) of intact segments of isolated guinea‐pig ileum. 3 Thirty to forty percent of the inhibition of contraction height (0.1 Hz) was reversed by pretreatment with the pure narcotic antagonist, naloxone. This naloxone‐reversible component showed cross‐tolerance with morphine. 4 PCP pretreatment caused a shift to the right in the dose‐response curve to acetylcholine (ACh) that was not parallel with the control dose‐response curve. Thus PCP does not interact with the muscarinic cholinoceptor in a strictly atropine‐like competitive fashion. 5 Binding sites for [3H]‐PCP were detected in homogenates of the guinea‐pig longitudinal muscle‐myenteric plexus preparation. 6 The affinity constants and the rank order of potencies of various PCP derivatives competing with [3H]‐PCP for binding suggest that these binding sites are very similar to those found in the central nervous system. 7 These data suggest that the guinea‐pig isolated ileum may be used as an in vitro system for studying the mechanism of action of phencyclidines.
大鼠小脑中苯环己哌啶衍生物的构效关系。
DOI：
10.1016/0091-3057(86)90055-9
发表时间：
1986
期刊：
Pharmacology, biochemistry, and behavior
影响因子：
--
作者：
Pang,K;Johnson,SW;Maayani,S;Freedman,R
通讯作者：
Freedman,R