The pharmacology of 1-(1-phenylcyclohexyl) piperidine-HCl.
The pharmacology of 1-(1-phenylcyclohexyl) piperidine-HCl.
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1-(1-苯基环己基)哌啶盐酸盐的药理学。
DOI：
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发表时间：
1959
影响因子：
3.5
通讯作者：
B. Bohner
中科院分区：
文献类型：
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作者：
G. Chen;C. Ensor;D. Russell;B. Bohner
1-（1-苯基环己基）哌啶·盐酸盐（PCP）主要通过刺激或抑制作用作用于中枢神经系统。体征和症状根据动物种类和剂量的不同而有很大差异。在大鼠和小鼠中观察到的活动过度更为显著;在所有剂量水平下，也可在这些动物中检测到一定程度的中枢抑制，表现为四肢肌肉协调丧失。在鸽子、豚鼠、仓鼠、兔子、猫、狗和猴子中，五氯苯酚在低剂量下产生镇静或镇定作用，在较高剂量下产生全身麻醉的僵硬样反应。鸽子、豚鼠、狗和猴子在接受五氯苯酚的剂量高于全身麻醉的剂量时会发生惊厥。另一方面，在兔子、猫、仓鼠、青蛙或鱼中，在很宽的剂量范围内使用该化合物时，未明显观察到惊厥或兴奋。PCP对电或戊四氮诱发的小鼠强直-伸肌癫痫发作有显著的抑制作用，对咖啡因诱发的癫痫发作有轻微的抑制作用，但对士的宁诱发的癫痫发作无效。PCP在非木僵或非麻醉剂量水平下不是镇痛剂。它具有局部麻醉活性，约为可卡因的一半或普鲁卡因的两倍。它对骨骼肌无肾上腺素能阻滞、神经节阻滞、抗胆碱能、抗组胺或抑制作用。在麻醉剂量下，五氯苯酚对呼吸和血压没有明显的抑制作用;事实上，这种药物会使血压略有升高。在高毒性剂量水平下，它会引起呼吸抑制、低血压和心动过缓。这种影响是暂时的。在神经毒性剂量下，PCP对未孕猫或孕猫的胃肠动力和子宫对肾上腺素的反应均无影响。从药理学结果的角度讨论了PCP对中枢神经系统的一些可能的作用部位。
1-(1-Phenylcyclohexyl)piperidine · HCl (PCP) acts principally on the central nervous system either by stimulation or by depression. Signs and symptoms vary considerably according to species of animals and dosage. Hyperactivity is more prominently observed in rats and mice; a certain degree of central depression, as manifested by the loss of muscle coordination of the limbs, may be detected also in these animals at all dose levels. In pigeons, guinea pigs, hamsters, rabbits, cats, dogs and monkeys, PCP produces a quieting or calming effect at low doses and a cataleptoid response to general anesthesia at higher levels. Convulsive seizures occur in pigeons, guinea pigs, dogs and monkeys receiving PCP at doses higher than those for general anesthesia. On the other hand, convulsion or excitement is not clearly noticed in rabbits, cats, hamsters, frogs or fish with this compound at a very wide range of doses. PCP is very effective in abolishing the electrically-or pentylenetetrazol-induced tonic-extensor seizures in mice, is slightly effective in suppressing caffeine-induced seizures but ineffective against those induced by strychnine. PCP is not an analgesic agent at noncataleptoid or nonanesthetic dose levels. It possesses a local anesthetic activity approximitely one-half that of cocaine or twice that of procaine. It is devoid of an adrenergic blocking, a ganglionic blocking, an anticholinergic, an antihistaminic, or a depressant action on skeletal muscles. Respiration and blood pressure are not markedly suppressed by PCP at anesthetic dosages; in fact the blood pressure is slightly elevated by the drug. At highly toxic dose levels, it will cause a suppression of respiration, hypotension and bradycardia. Such effects are transitory. Neither the gastrointestinal motility nor the response of the nonpgregnant or the pregnant cat uteri to epinephrine are affected by PCP at neurotoxic dosages. Some possible sites of action of PCP on the central nervous system are discussed from the standpoint of the pharmacological results presented.