• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.284-284
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• 1994

Pentazocine은 opioid 수용체에 대한 흥분작용과 길항작용을 겸유한 opioid계 약물로 알려져 있다. 본 연구에서 흰쥐 적출 관류부신 으로 부터 pentazocine의 catecholamine (CA) 분비작용을 관찰하여 그 기전을 규명하고 또한 다른 opioid의 작용과 비교하여 얻어진 결과는 다음과 같다. Pentazocine (30-300$\mu\textrm{g}$)을 부신정맥내에 주사하였을때 현저한 용량 의존성의 CA 분비 작용을 나타내었다. Pentazocine의 이러한 CA 분비작용은 chlorisondamine ($10^{-6}$M), naloxone (1.22 $\times$ $10^{-7}$M), morphine (1.73 $\times$ $10^{-5}$M). enkephalin (9.68 $\times$$10^{-6}$M), nicardipine ($10^{-6}$M) 및 TMB-8 ($10^{-5}$M)등의 전처치로 뚜렷이 억제되었으나 pirenzepine (2 $\times$ $10^{-6}$M)의 전처치에 의해서는 영향을 받지 않았다. $Ca^{++}$-free Krebs 용액으로 30분간 관류한 후에 pentazocine의 CA 분비작용은 현저한 감소를 나타내었다. Pentazocine (1.75 $\times$ $10^{-4}$M)을 20분간 관류시킨 후에 ACh (5.32 $\times$ $10^{-3}$M)과 DMPP ($10^{-4}$M)에 의한 CA 분비작용이 의의있게 감약되었다.

• Journal of Ginseng Research
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• v.16 no.2
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• pp.93-98
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• 1992

This study examined the Influence of ginseng total saponins (GTS) on the analgestic action and tolerance development of pentazocine in mice. Pentazocine prolonged the latency to response in the tail flick rather than in the tail pinch test. The analgesic effect of pentaEocine was antagonized by naloxone and completely eliminated by pretreatment u·ith f-chlorophenylalanine (PCPA). GTS provented the pentasocine-incuced analgesia ann inhibited the development of tolerance to pentazocine. The antagonistic effect of GTS on the pentazocine-induced analgesia was abolished by 5-HTP, but not by L-DOPA. These results suggest that GTS inhibits the analgesic action of pentazocine by the interaction with serotonergic neuron.

• The Korean Journal of Pharmacology
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• v.9 no.1
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• pp.47-51
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• 1973

A benzomorphan derivative, pentazocine has both opioid agonistic actions and weak narcotic antagonistic activity. In this paper, authors attempted to study the dose response of pentazocine on the blood sugar level, serum transaminase and alkaline phosphatase activity in rabbits. Eighteen rabbits were devided into 3 groups, and each group were injected with pentazocine 5mg, 15mg, and 30mg/kg respectively. And metabolic effects were investigated measuring the change of blood sugar contents, serum transaminase (S-GOT, S-GPT) activities and alkaline phosphatase activities in rabbits. The results were obtained as follows; 1. Pentazocine significantly increased the blood sugar content in rabbits. 2. Pentazocine significantly increased the serum GOT activity but in the serum GPT activity, it significantly increased in large dose. 3. Pentazocine significantly increased serum alkaline phosphatase activity.

• The Korean Journal of Pharmacology
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• v.30 no.3
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• pp.299-311
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• 1994

The present study was attempted to investigate whether pentazocine, which is known to possess both opioid agonistic and antagonistic properties, produces catecholamines (CA) secretion from the isolated perfused rat adrenal gland, and to establish the mechanism of its action, and also to compare its action with that of some opioids. Pentazocine (30 to 300 ug) injected into an adrenal vein caused a dose-dependent secretory response of CA from the rat adrenal medulla. The pentazocine-evoked secretion of CA was remarkably diminished by the preloading with chlorisondamine $(10^{-6}\;M)$, naloxone $(1.22{\times}10^{-7}\;M)$, morphine $(1.7{\times}10^{-5}\;M)$, met-enkephalin $(9.68{\times}10^{-6}\;M)$, nicardipine $(10^{-6}\;M)$ and TMB-8 $(10^{-5}\;M)$ while was not influenced by the pretreatment of pirenzepine $(2{\times}10^{-6}\;M)$. The perfusion of $Ca^{++}$-free Krebs solution for 30 min into the gland also led to the marked reduction in CA secretion evoked by pentazocine. Furthermore, the CA release evoked by ACh and/or DMPP was greatly inhibited by the pretreatment with pentazocine $(1.75{\times}10^{-4}\;M)$ for 20 min. From these experimental results, it is thought that pentazocine causes markedly the increased secretion of CA from the isolated perfused rat adrenal medulla by a calcium-dependent exocytotic mechanism. The secretory effect of pentazocine appears to be mediated through activation of opioid receptors located on adrenal chromaffin cells, which may be also associated with stimulation of cholinergic nicotinic receptors.

• The Korean Journal of Pharmacology
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• v.19 no.1
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• pp.115-122
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• 1983

The influences of diazepam and naloxone on the increase of plasma corticosterone level induced by morphine, pentazocine, ACTH, or picrotoxin were investigated in male mice. The results obtained were summarized as follows: 1) The increase induced by morphine or pentazocine of plasma corticosterone level was not affected by naloxone pretreatment but markedly suppressed by diazepam pretreatment. 2) The increase induced by ACTH of plasma corticosterone level was not affected by diazepam or naloxone pretreatment. 3) The picrotoxin markedly increased plasma corticosterone level, and the inceease was not affected by diazepam or naloxone pretreatment. This above results suggest that the increase induced by opioids of plasma corticosterone level seems to be rather related with other than opiate- or GABArerecptor.

• The Korean Journal of Pain
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• v.5 no.2
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• pp.213-220
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• 1992

The sciatic nerves of anesthetized rabbits were exposed and stimulated by a nerve stimulator in order to observe the myoneural response. These rabbits were divided into three groups and respectively injected with morphine (Group 1), meperidine(Group 2) and pentazocine (Group 3). The sciatic nerves were stimulated periodically and gait changes were observed to see the myoneural activity after the injections. When the distal part of the sciatic nerves were stimulated by the nerve stimulator after the respective drug injections, the normal muscle twitch responses were observed in all the progressional stages of Group 1. However, in Group 2 and 3, the muscle twitch responses decreased gradually, finally disappearing after approximately 10 minutes in these two groups. Complete motor paralysis continued for about 60 minutes. The muscle reactions returned to normal approximately 90 minutes after injection. Specimens drug-injected tissues were severed 4 hours, 24 hours and 1 week after injection respectively. These tissue were investigated under light as well as electron microscopy. The tissue revealed rare to moderate vacuolizations scattered in the axons of the myelinated and unmyelinated nerves of some of the specimens; however, there were no significant pathologic lesions. These results provide evidence that neurophysiologically, meperidine and pentazocine have a local anesthetic-like effect such as motor paralysis, but morphine does not. In addition, the results indicated that neurohistologically, the three narcotics have no significant toxic effects on the nerve tissue.

• The Korean Journal of Pharmacology
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• v.7 no.1
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• pp.21-27
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• 1971

The effects of 5 different drugs (amphetamine, caffeine, serotonin, sod. salicylate and pentazocine) on the duration of action of two barbiturates (thiopental and pentobarbital) and an intravenous anesthetic (propanidid) were determined in rats. Duration of action was determined by the time elapsing between loss and return of the righting reflexes. All drugs were injected intraperitoneally except propanidid which was administered by the intravenous route. Preliminary experiments indicated that at a dose of 40 mg/kg either of the two barbiturates or propanidid produced loss of the righting reflexes without death. At this dose, however, the duration of action of propanidid was extremely short. However, this dose was selected for subsequent studies. 1. At the dose employed amphetamine shortened the sleeping time of three compounds. 2. Caffeine and theophylline shortened the sleeping time of thiopental and prolonged the duration of action of pentobarbital. 3. Serotonin had no effect on duration of action of the barbiturates but prolonged the sleeping time produced by propanidid. 4. Sod. salicylate significantly prolonged the sleeping time of the barbiturates whereas pentazocine exhibited this effect only in relation to thiopental.

• Toxicological Research
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• v.5 no.1
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• pp.17-25
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• 1989

Chronic adminstraction of morphine to adult male rats has long been known to lower hepatic cytochrome p-450 content and its dependent mixed-function oxidase activity. Following the treatment of adult male rats with morphine, pethidine pentazocine and codeine and also by concomitant adminstration of naloxone activities of microsomal electron transfer in the adult male rats were examined. In present study, the acute treatment of mature male rats with a dose of narcotic drugs higher than that used chronically also reduces their hepatic cytochrome p-450.

• Journal of the Korean Chemical Society
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• v.54 no.4
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• pp.363-373
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• 2010

Computational studies were carried out on the opiates morphine, heroin, codeine, pentazocine, and buprenorphine, under the density functional theory. The geometric parameters of the pharmacophore and substituents were evaluated at the B3LYP/6-31+G(d) level of theory. The electronic structure calculations were performed using the same hybrid functional at the B3LYP/6-311++G (d,p) level of theory. The atomic charges were obtained by Mulliken population analysis. Given the reported biological activity, calculated partition coefficients, and electronic and geometric analysis, pentazocine and buprenorphine were chosen as models for proposed analogues. These analogues were then studied and compared with the model molecules. The study reveals that the geometry and electronic structure of the pharmacophore remains consistent in the presence of different substituents. Because the proposed analogues preserve the studied properties of the model molecules, it is likely that these analogues display biological activity.