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  • 1
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 48 (1987), S. 0 
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: Sodium-dependent high-affinity choline uptake was measured in various regions of the brains of rats irradiated for 45 min with either pulsed or continuous-wave low-level microwaves (2, 450 MHz; power density, 1 mW/cm2; average whole-body specific absorption rate, 0.6 W/kg). Pulsed microwave irradiation (2-μs pulses, 500 pulses/s) decreased choline uptake in the hippocampus and frontal cortex but had no significant effect on the hypothalamus, stria-turn, and inferior colliculus. Pretreatment with a narcotic antagonist (naloxone or naltrexone; 1 mg/kg i.p.) blocked the effect of pulsed microwaves on hippocampal choline uptake but did not significantly alter the effect on the frontal cortex. Irradiation with continuous-wave microwaves did not significantly affect choline uptake in the hippocampus, striatum, and hypothalamus but decreased the uptake in the frontal cortex. The effect on the frontal cortex was not altered by pretreatment with narcotic antagonist. These data suggest that exposure to low-level pulsed or continuous-wave microwaves leads to changes in cholinergic functions in the brain.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 553 (1989), S. 0 
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1520-6904
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 80 (1959), S. 0 
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1432-2072
    Keywords: TRH ; MK-771 ; Antimuscarinic ; Atropine ; Scopolamine ; Analeptic effect ; Barbiturate ; Pentobarbital
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract In the rat, the antimuscarinics atropine and scopolamine amine failed to block the reduction in pentobarbital-induced sleep time produced by either thyrotropin-releasing hormone (TRH) or MK-771 (a TRH analog). Previous reports have indicated that the marked analeptic effect produced by TRH is antagonized by such agents. It is not clear at this time whether the difference between our findings and these previous studies indicates a reduced sensitivity of cholinergic receptors in the rat to muscarinic blockade, a different neurochemical mechanism of action of TRH in the rat, or other unknown factors.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 82 (1984), S. 335-337 
    ISSN: 1432-2072
    Keywords: Apomorphine ; Haloperidol ; Ethanol ; Hypothermia ; Acute treatment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Apomorphine-induced hypothermia was studied in rats pretreated with a dose of apomorphine (1 mg/kg, IP), haloperidol (0.25 mg/kg, IP), ethanol (3 g/kg, PO), or apomorphine+ethanol. Pretreatment with apomorphine attenuated the hypothermic response, pretreatment with either haloperidol or ethanol potentiated it, and pretreatment with apomorphine together with ethanol did not alter it. These data show that an acute treatment with a dopaminergic drug can alter the responsiveness of the dopaminergic thermoregulatory system, and also that ethanol has an inhibitory effect on the dopamine mechanism.
    Type of Medium: Electronic Resource
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  • 7
    ISSN: 1432-2072
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1573-904X
    Keywords: O-acyl-propranolol ; stereoselective hydrolysis ; intestinal mucosa ; carboxylesterase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The aim of this study is to investigate species differences in the stereoselective hydrolysis for propranolol ester prodrugs in mammalian intestinal mucosa and Caco-2 cells. Methods. Hydrolase activities for propranolol prodrugs and p-nitro-phenylacetate in man (age: 51−71 years), the beagle dog (age: 4 years) and Wistar rat (age: 8 weeks) intestinal mucosa, and also in Caco-2 cells (passage between 60−70) were estimated by determining the rate of production of propranolol and p-nitrophenol, respectively. Results. The hydrolase activities for both propranolol prodrugs and p-nitrophenylacetate were in the order of man 〉 rat 〉〉 Caco-2 cells 〉 dog for intestinal microsomes, and rat 〉 Caco-2 cells = man 〉 dog for intestinal cytosol. Dog microsomes showed stereoselective hydrolysis for propranolol prodrugs, but not those from human or rat. Interestingly, both subcellular fractions of Caco-2 cells showed remarkable R-enantioselectivity except acetyl propranolol. Enzyme kinetic experiments for each enantiomer of butyryl propranolol in microsomes revealed that dog possesses both low and high affinity hydrolases. Both Km and Vmax values in rat were largest among examined microsomes, while Vmax/Km was largest in man. Finally, it was shown that the carboxylesterases might contribute to the hydrolysis of propranolol prodrug in all species by inhibition experiments. Conclusions. The hydrolase activities for propranolol prodrugs and p-nitrophenylacetate in intestinal mucosa showed great species differences and those in human intestine were closer to those of rat intestine than dog intestine or Caco-2 cells.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Chirality 9 (1997), S. 661-666 
    ISSN: 0899-0042
    Keywords: esterase ; O-acyl-propranolol ; substrate specificity ; structure activity relationship ; in vitro degradation ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Species differences and substrate specificities for the stereoselective hydrolysis of fifteen O-acyl propranolol (PL) prodrugs were investigated in pH 7.4 Tris-HCl buffer and rat and dog plasma and liver subfractions. The (R)-isomers were preferentially converted to propranolol (PL) in both rat and dog plasma with the exception of isovaleryl-PL in rat plasma, although the hydrolytic activities of prodrugs in rat plasma were 5-119-fold greater than those in dog plasma. The prodrugs with promoieties (C(=O)CH(R)CH3) based on propionic acid showed marked preference for hydrolysis of the (R)-enantiomers in plasma from both species (R/S ratio 2.5-18.2). On the other hand, the hepatic hydrolytic activities of prodrugs were greater in dog than rat, especially in cytosolic fractions. The hydrolytic activity was predominantly located in microsomes of the liver in rat, while the cytosol also contributed to hepatic hydrolysis in dog. Hepatic microsomal hydrolysis in dog showed a preference for the (R)-isomers except acetyl- and propionyl-PL. Interestingly, in rat liver all types of prodrugs with substituents of small carbon number showed (S)-preference for hydrolysis. The hydrolyses of (R)- and (S)-isomers of straight chain acyl esters in rat liver microsomes were linearly and parabolically related with the carbon number of substituents, respectively, while these relationships were linear for both isomers in dogs. Chirality 9:661-666, 1997. © 1997 Wiley-Liss, Inc.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Bioelectromagnetics 9 (1988), S. 355-362 
    ISSN: 0197-8462
    Keywords: microwaves ; choline uptake ; central nervous system ; radiation parameters ; Life and Medical Sciences ; Occupational Health and Environmental Toxicology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology , Physics
    Notes: Sodium-dependent high-affinity choline uptake was measured in the striatum, frontal cortex, hippocampus, and hypothalamus of rats after acute exposure (45 min) to pulsed (2 μs, 500 pps) or continuous-wave 2, 450-MHz microwaves in cylindrical waveguides (Guy et al.: Radio Science 14:63-74, 1979) or miniature anechoic chambers (Guy: Journal of Microwave Power 14:327-338, 1979). In all exposure conditions, the average whole-body specific absorption rate was at 0.6 W/kg. Decrease in choline uptake was observed in the frontal cortex after microwave exposure in all of the above irradiation conditions. Regardless of the exposure system used, hippocampal choline uptake was decreased after exposure to pulsed but not continuous-wave microwaves. Striatal choline uptake was decreased after exposure to either pulsed or continuous-wave microwaves in the miniature anechoic chamber. No significant change in hypothalamic choline uptake was observed under any of the exposure conditions studied. We conclude that depending on the parameters of the radiation, microwaves can elicit specific and generalized biological effects.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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