The circadian changes in elimination and absorption of amitriptyline after its intravenous and intragastric administration in rats were investigated. The values of such parameters as: AUC, MRT, t1/2, Cl, Vd, k(a) for amitriptyline change in the circadian rhythm. The fastest elimination of amitriptyline was observed in the dark phase (the acrophases for clearance were ca. 11 p.m. for iv administration and ca. 10 p.m. for po administration). The maximal value of clearance corresponds to the minimal values of MRT and t1/2. The acrophase for the constant absorption rate (po) falls at 7 p.m. Cyclic changes were not observed as far as the bioavailability is concerned.
{"title":"Circadian changes in the elimination of amitriptyline in rats.","authors":"A Rutkowska, W Piekoszewski, J Brandys","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The circadian changes in elimination and absorption of amitriptyline after its intravenous and intragastric administration in rats were investigated. The values of such parameters as: AUC, MRT, t1/2, Cl, Vd, k(a) for amitriptyline change in the circadian rhythm. The fastest elimination of amitriptyline was observed in the dark phase (the acrophases for clearance were ca. 11 p.m. for iv administration and ca. 10 p.m. for po administration). The maximal value of clearance corresponds to the minimal values of MRT and t1/2. The acrophase for the constant absorption rate (po) falls at 7 p.m. Cyclic changes were not observed as far as the bioavailability is concerned.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"671-7"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12480603","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The effects of levoprotiline (LEV), a (-)-enantiomer of oxaprotiline (OXA) and a clinically effective antidepressant, on the binding parameters of hippocampal 5-HT1A and cortical 5-HT2 receptors of rats were compared with those of (+)-enantiomer of OXA ((+)-OXA), imipramine and mianserin. Both LEV and (+)-OXA displayed in vitro some affinity for 5-HT1A receptors labelled with [3H]-8-OH-DPAT, and for 5-HT2 receptors labelled with [3H]-ketanserin. Repeated administration of LEV, for 14 days led to a marked increase in the number of 5-HT1A binding sites in the rat hippocampus, with no change in the KD values. (+)-OXA, imipramine and mianserin produced similar effects on 5-HT1A binding parameters. The number of 5-HT2 receptors was increased after two weeks of LEV administration, not altered after (+)-OXA, and decreased after imipramine or mianserin. The number of [3H]-ketanserin binding sites was decreased after four weeks of (+)-OXA administration, but not altered after LEV. The specific binding of [3H]-ketanserin in the rat cerebral cortex was decreased after repeated treatment with LEV and (+)-OXA (ex vivo). In competition studies the affinity of serotonin for [3H]-ketanserin binding sites was decreased in LEV- and increased in (+)-OXA-treated rats. The results suggest that LEV similarly to other antidepressants increases the number of 5-HT1A receptors, however without common alteration in 5-HT2 receptor number and function.
{"title":"Changes in the rat brain 5-HT1A and 5-HT2 receptors after chronic administration of levoprotiline, (+)-oxaprotiline and other antidepressant drugs.","authors":"V Klimek, J Zak-Knapik, C Cannizzaro","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The effects of levoprotiline (LEV), a (-)-enantiomer of oxaprotiline (OXA) and a clinically effective antidepressant, on the binding parameters of hippocampal 5-HT1A and cortical 5-HT2 receptors of rats were compared with those of (+)-enantiomer of OXA ((+)-OXA), imipramine and mianserin. Both LEV and (+)-OXA displayed in vitro some affinity for 5-HT1A receptors labelled with [3H]-8-OH-DPAT, and for 5-HT2 receptors labelled with [3H]-ketanserin. Repeated administration of LEV, for 14 days led to a marked increase in the number of 5-HT1A binding sites in the rat hippocampus, with no change in the KD values. (+)-OXA, imipramine and mianserin produced similar effects on 5-HT1A binding parameters. The number of 5-HT2 receptors was increased after two weeks of LEV administration, not altered after (+)-OXA, and decreased after imipramine or mianserin. The number of [3H]-ketanserin binding sites was decreased after four weeks of (+)-OXA administration, but not altered after LEV. The specific binding of [3H]-ketanserin in the rat cerebral cortex was decreased after repeated treatment with LEV and (+)-OXA (ex vivo). In competition studies the affinity of serotonin for [3H]-ketanserin binding sites was decreased in LEV- and increased in (+)-OXA-treated rats. The results suggest that LEV similarly to other antidepressants increases the number of 5-HT1A receptors, however without common alteration in 5-HT2 receptor number and function.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"549-60"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12480796","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The present paper reports on the synthesis and preliminary pharmacological properties of N-[beta-hydroxy-gamma-(N-phenylpiperazinepropyl)]-2- pyrrolidinone (MG-1). MG-1 was obtained by aminolysis of 1-(beta, gamma-epoxypropyl)-2-pyrrolidinone and N-phenylpiperazine. Its structure was established by elemental and spectral analyses (IR, UV, MS, 1H, 13C, 2D H-H and 2D C-H NMR). The antiarrhythmic activity of MG-1 was investigated on mice, rats and guinea pigs, using several models of arrhythmia. MG-1 attenuated or prevented the adrenaline- and barium chloride-induced arrhythmia. MG-1 demonstrated potent local anesthetic properties and depressed the depolarization phase of the action potential of cardiac cells. These results indicate that MG-1 possesses antiarrhythmic activity.
{"title":"Synthesis, physicochemical and preliminary pharmacological properties of N-[beta-hydroxy-gamma-(N-phenylpiperazinepropyl)]-2-pyrrolidinone.","authors":"B Malawska, M Gorczyca, B Filipek","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The present paper reports on the synthesis and preliminary pharmacological properties of N-[beta-hydroxy-gamma-(N-phenylpiperazinepropyl)]-2- pyrrolidinone (MG-1). MG-1 was obtained by aminolysis of 1-(beta, gamma-epoxypropyl)-2-pyrrolidinone and N-phenylpiperazine. Its structure was established by elemental and spectral analyses (IR, UV, MS, 1H, 13C, 2D H-H and 2D C-H NMR). The antiarrhythmic activity of MG-1 was investigated on mice, rats and guinea pigs, using several models of arrhythmia. MG-1 attenuated or prevented the adrenaline- and barium chloride-induced arrhythmia. MG-1 demonstrated potent local anesthetic properties and depressed the depolarization phase of the action potential of cardiac cells. These results indicate that MG-1 possesses antiarrhythmic activity.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"561-74"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12480800","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The present review primarily summarizes the cellular and molecular biology of MEL synthesis by the vertebrate retina, and the nature of MEL signal generated in this tissue. Additionally, the current status of retinal MEL receptors as well as physiological roles of this indoleamine within the eye are discussed.
{"title":"Melatonin in vertebrate retina: biosynthesis, receptors and functions.","authors":"J B Zawilska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The present review primarily summarizes the cellular and molecular biology of MEL synthesis by the vertebrate retina, and the nature of MEL signal generated in this tissue. Additionally, the current status of retinal MEL receptors as well as physiological roles of this indoleamine within the eye are discussed.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"627-54"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12512669","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
A Siemieniuk, H Szałkowska-Pagowska, S Lochyński, K Piatkowski, B Filipek, J Krupińska, R Czarnecki, T Librowski, S Białas
A few derivatives of natural, bicyclic monoterpenes, which are propranolol analogs, were synthetized. Those compounds were studied pharmacologically in order to determine their toxicity, antiarrhythmic activity in selected experimental models of arrhythmia, the local anesthetic effect and influence on the cardiovascular system. The tested compounds showed a less potent or similar toxicity towards reference drugs, were devoid of an antiarrhythmic activity in the model of barium arrhythmia, yet some of them (compounds 9 and 12) increased the arrhythmogenic dose of strophanthin. All the compounds studied had a local anesthetic effect stronger than lidocaine in infiltration anesthesia, and compound 8--also in surface anesthesia.
{"title":"Propranolol analogs containing natural monoterpene structures: synthesis and pharmacological properties.","authors":"A Siemieniuk, H Szałkowska-Pagowska, S Lochyński, K Piatkowski, B Filipek, J Krupińska, R Czarnecki, T Librowski, S Białas","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A few derivatives of natural, bicyclic monoterpenes, which are propranolol analogs, were synthetized. Those compounds were studied pharmacologically in order to determine their toxicity, antiarrhythmic activity in selected experimental models of arrhythmia, the local anesthetic effect and influence on the cardiovascular system. The tested compounds showed a less potent or similar toxicity towards reference drugs, were devoid of an antiarrhythmic activity in the model of barium arrhythmia, yet some of them (compounds 9 and 12) increased the arrhythmogenic dose of strophanthin. All the compounds studied had a local anesthetic effect stronger than lidocaine in infiltration anesthesia, and compound 8--also in surface anesthesia.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"575-93"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12480601","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The metabolism of phenacetin in vivo and in vitro at different periods of day was investigated in rats. In rats maintained on standard LD conditions the disappearance rate of phenacetin from blood and activity of phenacetin O-deethylase in liver were the highest in the morning and the lowest in the evening. Continuous illumination, adrenalectomy, phenobarbital or proadifen abolished this difference. It is postulated that these circadian changes of microsomal metabolism of phenacetin in rats liver are not fully responsible for the rhythmical changes in the antipyretic action of this drug that was observed previously. The mechanisms of this phenomenon are discussed.
{"title":"Circadian variations of phenacetin metabolism in rats in vivo and in vitro.","authors":"A Starek","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The metabolism of phenacetin in vivo and in vitro at different periods of day was investigated in rats. In rats maintained on standard LD conditions the disappearance rate of phenacetin from blood and activity of phenacetin O-deethylase in liver were the highest in the morning and the lowest in the evening. Continuous illumination, adrenalectomy, phenobarbital or proadifen abolished this difference. It is postulated that these circadian changes of microsomal metabolism of phenacetin in rats liver are not fully responsible for the rhythmical changes in the antipyretic action of this drug that was observed previously. The mechanisms of this phenomenon are discussed.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"663-70"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12480605","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Circadian changes in cytochrome P-450 and cytochrome b5 content and activity of NADPH-cytochrome P-450 and NADH-cytochrome b5 reductases have been studied in rat liver microsomes in season autumn. The obtained results indicate, that cytochrome P-450 in 6-month-old animals shows 12 h rhythm, but in older ones 24 h rhythm. NADPH-cytochrome P-450 reductase activity shows 24 h rhythm in oldest animals only. Cytochrome b5 and its reductase has 24 h rhythm in all examined groups of rats.
{"title":"Circadian changes of cytochrome P-450-dependent monooxygenase system in the rat liver.","authors":"A Plewka, P Czekaj, M Kamiński, D Plewka","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Circadian changes in cytochrome P-450 and cytochrome b5 content and activity of NADPH-cytochrome P-450 and NADH-cytochrome b5 reductases have been studied in rat liver microsomes in season autumn. The obtained results indicate, that cytochrome P-450 in 6-month-old animals shows 12 h rhythm, but in older ones 24 h rhythm. NADPH-cytochrome P-450 reductase activity shows 24 h rhythm in oldest animals only. Cytochrome b5 and its reductase has 24 h rhythm in all examined groups of rats.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"655-61"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12480538","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The in vivo effects of GABA-ergic drugs on the activity of serotonin N-acetyltransferase (NAT) and hydroxyindole-O-methyltransferase (HIOMT), two enzymes involved in melatonin biosynthesis, were investigated in light-exposed chicken retina. The ip administration of muscimol and baclofen (direct agonists of GABA-A and GABA-B receptors, respectively), aminooxyacetic acid (an inhibitor of GABA transaminase), and nipecotic acid (an inhibitor of GABA reuptake), significantly increased the retinal NAT activity by 50-100%. Similar rises in NAT activity were observed following intraocular treatment of ether-anesthetized chickens with muscimol, baclofen and GABA. In contrast to NAT, there was no effect of the tested drugs on the retinal HIOMT activity. Aminophylline (a phosphodiesterase inhibitor) markedly elevated the retinal NAT activity, and a combined treatment with the GABA-ergic drugs and aminophylline resulted in additive effects. The actions of both muscimol and baclofen were antagonized by picrotoxin and bicuculline (two GABA-A receptor blockers), whereas the effect of baclofen was not changed by a selective GABA-B receptor blocker, CGP 35,348. Melatonin given ip significantly raised NAT activity, and its combination with muscimol further stimulated the enzyme. Picrotoxin and bicuculline given to chickens during the dark phase of 12 h light--12 h dark illumination cycle significantly suppressed the nocturnal NAT activity in retina. Neither GABA nor muscimol and baclofen significantly affected basal and forskolin (1 microM)-stimulated adenylate cyclase activity in vitro in light-exposed chicken retina. It is concluded that a GABA signal (acting through type A of GABA receptors) plays an important role in a complex mechanism regulating the rhythmic melatonin biosynthesis in vertebrate retina.
研究了gaba能药物对光暴露鸡视网膜中参与褪黑素生物合成的血清素n -乙酰转移酶(NAT)和羟吲哚- o -甲基转移酶(HIOMT)活性的影响。服用muscimol和baclofen(分别是GABA- a和GABA- b受体的直接激动剂)、氨基乙酸(GABA转氨酶抑制剂)和尼哌酸(GABA再摄取抑制剂),可显著提高视网膜NAT活性50-100%。在用muscimol、巴氯芬和GABA对乙醚麻醉的鸡进行眼内处理后,也观察到类似的NAT活性升高。与NAT相比,被试药物对视网膜HIOMT活性没有影响。氨茶碱(一种磷酸二酯酶抑制剂)可显著提高视网膜NAT活性,gaba能药物与氨茶碱联合治疗可产生叠加效应。两种GABA-A受体阻滞剂(picrotoxin和bicuculline)均可拮抗muscimol和巴氯芬的作用,而选择性GABA-B受体阻滞剂CGP 35,348则不能改变巴氯芬的作用。褪黑素可显著提高NAT活性,与muscimol联合使用可进一步刺激NAT活性。在12 h光照-12 h光照周期的黑暗阶段给予鸡微腐毒素和双曲碱,可显著抑制视网膜夜间NAT活性。GABA、muscimol和巴氯芬均未显著影响光暴露鸡视网膜中基底和福斯克林(1微米)刺激的腺苷酸环化酶活性。综上所述,GABA信号通过GABA受体a型发挥作用,在脊椎动物视网膜节律性褪黑激素生物合成的复杂调控机制中发挥重要作用。
{"title":"The role of GABA-ergic signal in the regulation of melatonin biosynthesis in vertebrate retina.","authors":"A Kazula, J Z Nowak","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The in vivo effects of GABA-ergic drugs on the activity of serotonin N-acetyltransferase (NAT) and hydroxyindole-O-methyltransferase (HIOMT), two enzymes involved in melatonin biosynthesis, were investigated in light-exposed chicken retina. The ip administration of muscimol and baclofen (direct agonists of GABA-A and GABA-B receptors, respectively), aminooxyacetic acid (an inhibitor of GABA transaminase), and nipecotic acid (an inhibitor of GABA reuptake), significantly increased the retinal NAT activity by 50-100%. Similar rises in NAT activity were observed following intraocular treatment of ether-anesthetized chickens with muscimol, baclofen and GABA. In contrast to NAT, there was no effect of the tested drugs on the retinal HIOMT activity. Aminophylline (a phosphodiesterase inhibitor) markedly elevated the retinal NAT activity, and a combined treatment with the GABA-ergic drugs and aminophylline resulted in additive effects. The actions of both muscimol and baclofen were antagonized by picrotoxin and bicuculline (two GABA-A receptor blockers), whereas the effect of baclofen was not changed by a selective GABA-B receptor blocker, CGP 35,348. Melatonin given ip significantly raised NAT activity, and its combination with muscimol further stimulated the enzyme. Picrotoxin and bicuculline given to chickens during the dark phase of 12 h light--12 h dark illumination cycle significantly suppressed the nocturnal NAT activity in retina. Neither GABA nor muscimol and baclofen significantly affected basal and forskolin (1 microM)-stimulated adenylate cyclase activity in vitro in light-exposed chicken retina. It is concluded that a GABA signal (acting through type A of GABA receptors) plays an important role in a complex mechanism regulating the rhythmic melatonin biosynthesis in vertebrate retina.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"611-25"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12480600","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
J L Mokrosz, S Charakchieva-Minol, M H Paluchowska, M T Cegła
The effect of a steric hindrance around the protonation center of the model 4-substituted 1-(3-chlorophenyl)-piperazines 1-9 and 11-14 on their affinity for 5-HT1A and 5-HT2 receptor sites was investigated. Additional evidence for hydrophobic interactions between the N-4 hydrocarbon substituents and 5-HT1A receptors has been presented. However, the hydrophobic forces play a minor role in stabilization of the bioactive complex with 5-HT2 receptors. It has also been found that even bulky substituents around the protonation center of 1-aryl-piperazines are well tolerated at both 5-HT1A and 5-HT2 sites.
{"title":"Structure-activity relationship studies of CNS agents. Part VIII. Bulk tolerance around the protonation center of 4-substituted 1-(3-chlorophenyl)piperazines at 5-HT1A and 5-HT2 receptors.","authors":"J L Mokrosz, S Charakchieva-Minol, M H Paluchowska, M T Cegła","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The effect of a steric hindrance around the protonation center of the model 4-substituted 1-(3-chlorophenyl)-piperazines 1-9 and 11-14 on their affinity for 5-HT1A and 5-HT2 receptor sites was investigated. Additional evidence for hydrophobic interactions between the N-4 hydrocarbon substituents and 5-HT1A receptors has been presented. However, the hydrophobic forces play a minor role in stabilization of the bioactive complex with 5-HT2 receptors. It has also been found that even bulky substituents around the protonation center of 1-aryl-piperazines are well tolerated at both 5-HT1A and 5-HT2 sites.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 6","pages":"595-607"},"PeriodicalIF":0.0,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12480798","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M J Klin, A Wystrychowski, E Grzebieniak, A Sobczak, R Bochenek, W Wesołowski, Z S Herman
Our studies showed that the nifedipine in daily doses of 30 mg/kg given to rabbits treated with a diet containing 1% cholesterol for 6 months, decreased cholesterol content in aorta homogenates, urine excretion of desmosines and prolonged partial thromboplastin time, while it did not alter serum lipids. These results may have some value for understanding of the antiatherogenic mechanism of nifedipine.
{"title":"Influence of nifedipine on aortal cholesterol content, blood coagulation and elastin metabolism in cholesterol-fed rabbits.","authors":"M J Klin, A Wystrychowski, E Grzebieniak, A Sobczak, R Bochenek, W Wesołowski, Z S Herman","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Our studies showed that the nifedipine in daily doses of 30 mg/kg given to rabbits treated with a diet containing 1% cholesterol for 6 months, decreased cholesterol content in aorta homogenates, urine excretion of desmosines and prolonged partial thromboplastin time, while it did not alter serum lipids. These results may have some value for understanding of the antiatherogenic mechanism of nifedipine.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"461-8"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471921","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}