Polish journal of pharmacology (Pol J Pharmacol)

Publications in this journal

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  Available from: krakow.pl

  Article: Comparative pharmacokinetics of propranolol and atenolol in primary hyperlipidemia.

  Bogumiła Telatyńska, Jerzy Wójcicki, Marek Droździk, Barbara Gawrońska-Szklarz, Violetta Sulzyc-Bielicka, Rozalia Sterna
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  ABSTRACT: The study was aimed to examine the effects of different types of hyperlipidemia on the pharmacokinetics of lipophilic propranolol and hydrophilic atenolol. Thirty subjects were divided into four study groups: normolipemics, hypercholesterolemics, hypertriglyceridemics, and patients with mixed form of hyperlipidemia. The drugs were administered orally at a single dose of 80 mg for propranolol and 100 mg for atenolol, using a cross-over study design. Pharmacokinetic parameters of the drugs were calculated using a noncompartmental open model. The results of the present study demonstrated a possible influence of dyslipidemia on pharmacokinetics of both the lipophilic and hydrophilic drugs. As for the lipophilic drug propranolol, a significant decrease in elimination rate constant was found (from 0.24 +/- 0.08 h(-1) to 0.16 +/- 0.04 h(-1), p < 0.03) in comparison to normolipemic subjects. In the case of the hydrophilic atenolol, the most marked alterations were also seen in subjects with mixed form of hyperlipidemia, especially significantly lower values of area under the concentration-time curve (8950.8 +/- 2060.5 ng/ml x h and 6715.4 +/- 1813.8 ng/ml x h, p < 0.05) as well as higher elimination rate constant (0.08 +/- 0.03 h(-1) and 0.13 +/- 0.05 h(-1), p < 0.05) in comparison with the controls, respectively. Total body clearance per kg of body weight of propranolol as well as atenolol was not influenced by dyslipidemias. The results of the study indicate that lipid metabolism disturbances might to some extent influence the pharmacokinetics of propranolol and atenolol, with the most significant alterations seen in the patients with mixed form of hyperlipidemia.
  Polish journal of pharmacology 01/2003; 55(1):81-9.
• Article: Professor Zdzislaw Kleinrok--the 50th anniversary of his scientific activity

  M Wielosz
  Polish journal of pharmacology 02/2000; 52(1):53-4.
• Article: Professor Jerzy Maj--the 50th anniversary of his scientific activity

  Disciples
  Polish journal of pharmacology 02/2000; 52(1):1-2.
• Article: Nitric oxide donors antagonize N-nitro-L-arginine and haloperidol catalepsy: potential implication for the treatment of Parkinsonism?

  P Krzaścik, W Kostowski
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  ABSTRACT: Nitric oxide (NO) synthase inhibitor, N-nitro-L-arginine (NNLA) produced dose-dependent, long-lasting catalepsy in rats, the effect being attenuated by NO donors L-arginine and molsidomine. Catalepsy induced by haloperidol (0.4 mg/kg i.p.), D2 receptor antagonist, was reduced dose-dependently by molsidomine (10.0-100.0 mg/kg) and by L-arginine at a dose of 100.0 mg/kg. Low, non-cataleptic doses of NNLA (0.1 mg/kg) and haloperidol (0.1 mg/kg) given in combination produced a marked and long-lasting catalepsy. The results suggest that NO plays a role in NNLA-induced catalepsy as well as in catalepsy elicited by haloperidol.
  Polish journal of pharmacology 09/1997; 49(4):263-6.
• Article: Behavioral activity of 1S,3R-ACPD, an agonist of metabotropic glutamate receptors.

  A Zalewska, K Wiśniewski
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  ABSTRACT: The influence of intracerebroventricular (i.c.v.) injections of 1-aminocyclopentane-1,3-dicarboxylic acid (1S,3R-ACPD), an agonist of metabotropic glutamate receptors, on the activity of the central nervous system was examined in rats. 1S,3R-ACPD at the i.c.v. doses of 100 and 200 nmole significantly decreased apomorphine-induced stereotypy, and at a dose 200 nmole significantly diminished catalepsy caused by haloperidol, two behavioral symptoms controlled mainly by central dopaminergic system. The tested compound had no influence on the locomotor and exploratory activity of rats estimated in open field. 1S,3R-ACPD significantly improved acquisition at the i.c.v. dose of 100 nmole, and consolidation of information at the i.c.v. doses of 100 and 200 nmole. The tested compound had no influence on retention processes in passive avoidance situation. This compound also did not improve recognition memory tested in the object recognition test. These results indicated that 1S,3R-ACPD improved memory motivated affectively but had no influence on recognition memory and the diminished dopaminergic transmission.
  Polish journal of pharmacology 09/1997; 49(4):239-48.
• Article: Effects of dopaminergic agonists and antagonists on the serum prolactin levels in alcoholized rats.

  J Samochowiec, Z Kleinrok, E Jagiełło-Wójtowicz, J Horodnicki, H Rommelspacher, L G Schmidt
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  ABSTRACT: A single dose of ethanol (1 g/kg p.o.) significantly decreased, whereas higher doses of ethanol (2 or 3 g/kg p.o.) significantly increased the serum prolactin (PRL) concentration. Administration of ethanol at a dose of 2 g/kg p.o. for 4 weeks did not affect this parameter but the ethanol withdrawal syndrome caused a significant rise in the serum PRL level. Chronic studies showed that D1-dopaminergic agonist SKF 38390 (2.5 mg/kg) significantly raised serum PRL levels in rats. This effect was reversed by long-lasting treatment of rats with ethanol and ethanol withdrawal. Pimozide (1 mg/kg), D2 antagonist, increased PRL in those rats. On the other hand, D1-antagonist SCH 23390 (0.5 mg/kg) and D2-agonist PPHT (0.5 mg/kg) were without effect in rats administered ethanol for a long period of time. In rats with ethanol withdrawal syndrome, administration of D1-antagonist SCH 23390 (0.5 mg/kg) also did not affect the serum PRL concentrations. However, D1-agonist SKF 38393 (2.5 mg/kg) and D2-antagonist pimozide (1 mg/kg) increased the serum PRL level in rats with ethanol withdrawal syndrome, whereas D2 agonist PPHT (2 mg/kg) decreased PRL level in serum. Thus, the acute effect of ethanol on PRL level appears to be dose-dependent. It seems that chronic ethanol administration and its withdrawal especially affected D1 receptor.
  Polish journal of pharmacology 09/1997; 49(4):221-7.
• Article: Professor Dr. Józef Hano (1906-1997).

  J Maj, E Przegaliński
  Polish journal of pharmacology 09/1997; 49(4):185-90.
• Article: Diversity of dopamine receptors: new molecular and pharmacological developments.

  D S Hartman, F Lanau
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  ABSTRACT: Five distinct dopamine (DA) receptors, named D1-D5, are expressed in the central nervous system where they control motor function, emotional states, and endocrine physiology. With the production of receptor-specific knockout mice and the development of receptor subtype specific ligands, our understanding of dopaminergic systems in the brain is expanding rapidly. In some of the more recent developments, the D4R has been shown to be activated by all three catecholamine neurotransmitters: DA, epinephrine, and norepinephrine. This functional activation by multiple neurotransmitters provides a novel mechanism for integration of catecholamine signaling. In addition, the D4R was reported last year to show genetic linkage to a personality trait called novelty seeking, and now has been implicated in the manifestation of attention deficit hyperactivity disorder, which affects 3-6% of school age children. New evidence has emerged indicating that yet another DA receptor subtype may exist which has D1-like pharmacology but couples to phosphoinositol turnover, which may be of particular importance in the light of recent studies which show decreased D1-like receptor density in brain from schizophrenic patients. This review will cover these and other new developments in the area of DA receptors which have important implications for the understanding of human behavior and disease.
  Polish journal of pharmacology 09/1997; 49(4):191-9.
• Article: Nitric oxide donation and nitrite assays in the presence of thiols and albumin as determined by Griess' and Werringloer's methods.

  J Robak, E Marcinkiewicz, Z Michalska, R J Gryglewski
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  ABSTRACT: Nitric oxide (NO) or nitrite (NO2-) were assayed using the Werringloer's method or the Griess' method, respectively, in the presence or absence of various thiols, amino acids, or albumin. This has been done because both methods are used to determine the generation of endogenous NO from L-arginine or exogenous NO from drugs in vivo, paying little attention to biological constituents which may affect results of these assays. Albumin, reduced glutathione (GSH), cysteine and N-acetylcysteine, but not other amino acids lowered the amount of NO2- as detected by Griess' method no matter whether sodium nitrite or 3-morpholinosydnonimine (SIN-1) were used as a source of NO2-. This happened probably because at low pH of the reaction mixture the corresponding nitrosothiols were formed and thus NO2- was not accessible for detection. However, this phenomenon was not seen when instead of SIN-1 another NO donor--S-nitroso-N-acetylpenicillamine (SNAP) was used. SNAP is a nitrosothiol itself and physiological low molecular thiols (e.g. GSH or cysteine) displaced NO from SNAP. An increase in the amount of released NO was detectable by both Werringloer's and Griess' methods. Only the presence of 700 microns of albumin steadily suppressed the detection of NO or NO2- no matter what was the source of these species. It is concluded that low molecular thiols and albumin may differently influence the detection of both NO and NO2- which derive from various NO donors or sodium nitrite.
  Polish journal of pharmacology 09/1997; 49(4):255-62.
• Article: Effects of repeated MK-801 administration on the glutamate receptor gene expression in the rat hippocampus.

  W Lasoń, J Turchan, B Przewłocka, D Labuz, R Przewłocki
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  ABSTRACT: Effects of acute and chronic treatment with the noncompetitive NMDA receptor antagonist MK-801 on the NMDAR1 and GluR2 (flip and flop) receptor mRNA levels were estimated in the rat hippocampal formation. An in situ hybridization study showed that a single injection of MK-801 increased the NMDAR1 mRNA level in the CA1 region after 3 and 24 h, and in the CA3 one after 3 h, whereas chronic administration of the drug increased the mRNA level in the dentate gyrus and CA1 at the latter time. The level of the flip version of GluR2 mRNA was decreased in the CA3 region, and dentate gyrus at 3 and 24 h following acute MK-801 administration. Chronic MK-801 administration decreased GluR2 flip mRNA level in the dentate gyrus at 3 and 24 h, and in the CA1 region at 3 h only. On the other hand, chronic, but not acute, MK-801 administration elevated the GluR2 flop mRNA level in the CA1 region and dentate gyrus 24 h after the last drug injection. In summary, the above data indicate that both acute and chronic MK-801 administration affect the NMDAR1 and GluR2 receptor gene expression in the rat hippocampal formation in a time- and region-specific manner. These changes may, in turn, influence the glutamatergic transmission and/or susceptibility to the EAA-mediated excitotoxicity of hippocampal neurons.
  Polish journal of pharmacology 09/1997; 49(4):249-53.
• Article: Characterization of opiate binding sites on the goldfish (Carassius auratus L.) pronephric leukocytes.

  S Józefowski, B Płytycz
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  ABSTRACT: The head kidney is the main lymphopoietic organ of teleost fish. It is the source of leukocytes inhabiting the peritoneal cavity during an experimental peritoneal inflammation (Gruca et al., Folia Biol.-Kraków, 1997, 44, 137-142). The number of elicited peritoneal leukocytes is significantly lower in the goldfish with concomitant morphine injection than in their counterparts injected with the irritant only. Morphine may act directly on the head kidney leukocytes, as they are equipped with the selective naloxone-binding sites (Chadzińska et al., Arch. Immunol. Ther. Exp., 1997, in press). Further characterization of these opioid receptors (by radioligand binding techniques) indicates that the goldfish head kidney leukocytes possess at least two different opiate-binding sites: the [3H]naloxone binding site with a KD = 87 +/- 2.1 nM and Bmax = 298 +/- 15 fmol/mg protein; and the second, the [3H]naltrindole binding site with a KD = 37 +/- 5.5 nM and Bmax = 1,172 +/- 220 fmol/mg protein. The competition experiments with delta- (naltrindole), kappa- (nor-binaltorphimine) and mu- (cyprodime, naltrexone) selective ligands suggest that the naloxone-binding site is similar to mu 3 receptors described by Stefano et al. (Proc. Nat. Acad. Sci. USA, 1993, 90 11099-11103). Low affinity binding of selective ligands excludes the presence of neuronal-type mu- and delta-opioid receptors on goldfish leukocytes.
  Polish journal of pharmacology 09/1997; 49(4):229-37.
• Article: Dopamine D4-like receptors in vertebrate retina: does the retina offer a model for the D4-receptor analysis?

  J B Zawilska, J Z Nowak
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  ABSTRACT: Dopamine is a major catecholamine in vertebrate retina. The amine is localized, depending on the species, in a subset of amacrine and/or interplexiform cells. The dopamine-containing cells in retina are activated upon light exposure, with resulting increase in the amine synthesis and release. Dopamine, acting as a light-adaptive signal, controls many aspects of retinal physiology; among its diverse effects is modulation of the night-driven melatonin biosynthesis, which occurs in photoreceptors. Activation of dopamine receptors belonging to D2-family, localized on photoreceptors, rapidly suppresses the nocturnal cyclic AMP-dependent activity of serotonin N-acetyltransferase (NAT), a key regulatory enzyme in melatonin biosynthesis. Convincing evidence indicates that these NAT activity-modulating receptors represent the D4-subtype dopamine receptors, which--most probably indirectly--control in a negative manner the activity of intraphotoreceptor Ca2+/calmodulin-dependent adenylyl cyclase. This article reviews current knowledge on dopamine D4-subtype receptors, with a special emphasis to their function in vertebrate retina. In addition, some findings resulting from our recent experiments with newly synthesized D4-receptor-selective ligands are presented and discussed. It is proposed that the avian retina, with its ability to synthesize melatonin in a dopamine-sensitive manner (via D4-like dopamine receptor), may offer a suitable specific in vivo model which allows to study potential ligands (both agonists and antagonists) of the D4-subtype dopamine receptor.
  Polish journal of pharmacology 09/1997; 49(4):201-11.
• Article: Potential role of 5-HT2 and D2 receptor interaction in the atypical antipsychotic action of the novel succimide derivative, perospirone.

  Y Ohno, K Ishida-Tokuda, T Ishibashi, H Sakamoto, R Tagashira, T Horisawa, K Yabuuti, K Matsumoto, A Kawabe, M Nakamura
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  ABSTRACT: The pharmacological profile of the novel serotonin-dopamine antagonists (SDA)-type antipsychotic, perospirone, was compared with other SDA and typical antipsychotics, and a potential role of 5-HT2 and D2 receptor interaction in the atypical antipsychotic property of SDA was discussed based on the findings with selective 5-HT2 antagonists. Our study revealed that perospirone, like other SDA, differed from the typical antipsychotics by exhibiting 1) putative anxiolytic and/or antidepressant actions in some animal models (e.g., conditioned fear stress-induced freezing model and rat social interaction), 2) reduced extrapyramidal side effects (EPS) liability (catalepsy and bradykinesia induction), 3) weaker blocking actions at striatal D2 receptors as revealed by c-fos expression and dopamine turnover and 4) lower propensity to induce supersensitivity of dopamine receptors after repeated treatments (e.g., dopamine agonist-induced stereotyped behavior and vacuous chewing movement). The 5-HT2 antagonists mimicked the action of SDA antipsychotics in the animal models of mood disorder. In addition, combined treatments of 5-HT2 antagonists with typical antipsychotic could attenuate EPS induction and striatal c-fos expression associated with D2 receptor blockade, and could prevent the sensitization of D1 receptor function after repeated treatments. These findings suggest that the blockage of 5-HT2 receptors contributes to the broad efficacy profile of SDA (i.e., antipsychotic and mood stabilizing actions) and may counteract the D2 (and/or D1) blocking activities of antipsychotics in the striatum to reduce EPS.
  Polish journal of pharmacology 09/1997; 49(4):213-9.
• Article: The role of calcium channel entry blocker in experimental ischemia-reperfusion-induced intestinal injury

  Mocan H, Gedik Y, Erduran E, Mocan ZM, Okten A, Gacar N, Pul N
  Polish journal of pharmacology 01/1995; 47(2):179-183.
• Article: Endothelial receptor defense in advanced atherosclerosis

  Pandolfo L, Ragazzi E, Chinellato A, Froldi G, Caparrotta L, Aliev G, Fassina G
  Polish journal of pharmacology 04/1994; 46(4):350-351.
• Article: Inhibition of human platelet cathepsin A by non-steroidal anti-inflammatory drugs--in vitro study.

  H Ostrowska
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  ABSTRACT: Since the lysosomal proteases appear at site of inflammation they may be a target for non-steroidal anti-inflammatory drugs (NSAIDs). In in vitro study the inhibition of human platelet cathepsin A by NSAIDs was found. Indomethacin, phenacetin and aminophenazone were the most potent inhibitors of cathepsin A. Acetylsalicylic acid added to platelet lysate inhibited cathepsin A in the same extent as salicylate. The inhibition was time-dependent and reversed after dialysis. Mixed type of inhibition by salicylate was shown.
  Polish journal of pharmacology 48(1):113-6.
• Article: Professor Jerzy L. Mokrosz, D.Sc., Ph.D. (1949-1996).

  J Maj
  Polish journal of pharmacology 48(2):125-8.
• Article: 5-HT3 receptors and central effects of ethanol.

  W Kostowski
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  ABSTRACT: This review discusses recent experimental findings in serotonin-3 (5-HT3) receptors and ethanol (EtOH) research. The role of these receptors in central effects of EtOH including the effects of 5-HT3 agonists and antagonists on EtOH intake, rewarding and aversive properties of EtOH and EtOH interoceptive cue is reviewed. It is now recognized that 5-HT3 receptors while involved in EtOH intake, EtOH tolerance and withdrawal and rewarding mechanisms do not play an important role in aversive effects of EtOH and EtOH discriminative stimulus. 5-HT3 receptors involved in EtOH consumption are supposedly located on dopaminergic neurons in the nucleus accumbens.
  Polish journal of pharmacology 48(3):243-54.
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  Available from: krakow.pl

  Article: Pentoxifylline does not affect nociception if administered postoperatively.

  A M Szczepanik, J Wordliczek, W Serednicki, M Siedlar, A Czupryna
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  ABSTRACT: Proinflammatory cytokines, such as tumor necrosis factor alpha (TNF-alpha), interleukin-1 (IL-1) and interleukin-6 (IL-6), act as mediators of post-injury inflammation and increase pain sensitivity. Pentoxifylline (PTX) has the property of inhibiting TNF-alpha, IL-1, and IL-6 production. Previous studies revealed that the pre-injury or preoperative administration of PTX inhibited consequent hyperalgesia or postoperative pain. The aim of the study was to determine, if postoperative PTX administration affects postoperative pain. A group of 40 patients undergoing laparotomic cholecystectomy received postoperatively PTX at 10 mg/kg or placebo directly after the termination of general anesthesia. There were no differences in postoperative pain, analgesic drug requirement or TNF-alpha and IL-6 serum levels between the groups.
  Polish journal of pharmacology 56(5):611-6.