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  • Electronic Resource  (47)
  • Analytical Chemistry and Spectroscopy  (33)
  • Rat  (6)
  • Biochemistry  (4)
  • Drug design  (4)
  • 1
    Electronic Resource
    Electronic Resource
    (±)-1-(2,5-Dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), a novel putative anxiolytic agent lacking affinity for benzodiazepine sites and serotonin-1A receptors (1996)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 354 (1996), S. 579-585 
    Details
    ISSN: 1432-1912
    Keywords: ALEPH-2 Serotonin receptor binding ; Anxiolytics ; Serotonin syndrome ; Phenylisopropylamines ; Rat ; Hypothermia ; Psychedelics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Serotonergic behavioral responses, effects on motor activity and core temperature, and binding properties of the novel putative anxiolytic amphetamine derivative (±)1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), were examined in rodents in order to elucidate the mechanism underlying its anxiolytic-like effect. After peripheral administration in rats, ALEPH-2 induced some symptoms of the serotonergic syndrome, e.g. forepaw treading and flat body posture. Additionally, a decrease in motor activity was observed. No significant effects on the number of head shakes were observed after injection, although high inter-subject variability was noted. Higher doses of ALEPH-2, in the range exhibiting anxiolytic properties (4mg/kg), elicited significant hypothermia in mice. The affinity of the drug for 5-HT2A/2C receptors ([3H]ketanserin sites) was in the nanomolar range (Ki = 173 nM), whereas for 5-HT1A, benzodiazepine sites, and GABAA receptors, the affinity was micromolar or lower. Based on these results the mechanism of action and the anxiolytic-like properties of ALEPH-2 are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00170831
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    (±)-1-(2,5-Dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2) a novel putative anxiolytic agent lacking affinity for benzodiazepine sites and serotonin-1A receptors (1996)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 354 (1996), S. 579-585 
    Details
    ISSN: 1432-1912
    Keywords: Key words ALEPH-2 ; Serotonin receptor binding ; Anxiolytics ; Serotonin syndrome ; Phenylisopropylamines ; Rat ; Hypothermia ; Psychedelics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Serotonergic behavioral responses, effects on motor activity and core temperature, and binding properties of the novel putative anxiolytic amphetamine derivative (±)1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), were examined in rodents in order to elucidate the mechanism underlying its anxiolytic-like effect. After peripheral administration in rats, ALEPH-2 induced some symptoms of the serotonergic syndrome, e.g. forepaw treading and flat body posture. Additionally, a decrease in motor activity was observed. No significant effects on the number of head shakes were observed after injection, although high inter-subject variability was noted. Higher doses of ALEPH-2, in the range exhibiting anxiolytic properties (4mg/kg), elicited significant hypothermia in mice. The affinity of the drug for 5-HT2A/2C receptors ([3H]ketanserin sites) was in the nanomolar range (Ki=173 nM), whereas for 5-HT1A, benzodiazepine sites, and GABAA receptors, the affinity was micromolar or lower. Based on these results the mechanism of action and the anxiolytic-like properties of ALEPH-2 are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00170831
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Evolutionary algorithms in computer-aided molecular design (1996)
    Springer
    Journal of computer aided molecular design 10 (1996), S. 337-358 
    Details
    ISSN: 1573-4951
    Keywords: Genetic algorithms ; Evolutionary programming ; Evolution strategies ; Drug design ; Molecular modelling ; Protein folding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary In recent years, search and optimisation algorithms inspired by evolutionary processes have been applied with marked success to a wide variety of problems in diverse fields of study. In this review, we survey the growing application of these ‘evolutionary algorithms’ in one such area: computer-aided molecular design. In the course of the review, we seek to summarise the work to date and to indicate where evolutionary algorithms have met with success and where they have not fared so well. In addition to this, we also attempt to discern some future trends in both the basic research concerning these algorithms and their application to the elucidation, design and modelling of chemical and biochemical structures.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00124503
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  • 4
    Electronic Resource
    Electronic Resource
    PRO_LIGAND: An approach to de novo molecular design. 3. A genetic algorithm for structure refinement (1995)
    Springer
    Journal of computer aided molecular design 9 (1995), S. 139-148 
    Details
    ISSN: 1573-4951
    Keywords: Drug design ; De novo design ; Genetic algorithms
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary Recently, the development of computer programs which permit the de novo design of molecular structures satisfying a set of steric and chemical constraints has become a burgeoning area of research and many operational systems have been reported in the literature. Experience with PRO_LIGAND—the de novo design methodology embodied in our in-house molecular design and simulation system PRO-METHEUS—has suggested that the addition of a genetic algorithm (GA) structure refinement procedure can ‘add value’ to an already useful tool. Starting with the set of designed molecules as an initial population, the GA can combine features from both high- and low-scoring structures and, over a number of generations, produce individuals of better score than any of the starting structures. This paper describes how we have implemented such a procedure and demonstrates its efficacy in improving two sets of molecules generated by different de novo design projects.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00124404
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  • 5
    Electronic Resource
    Electronic Resource
    PRO_LIGAND: An approach to de novo molecular design. 1. Application to the design of organic molecules (1995)
    Springer
    Journal of computer aided molecular design 9 (1995), S. 13-32 
    Details
    ISSN: 1573-4951
    Keywords: Drug design ; De novo design ; Enzyme inhibitors ; Graph theory
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary An approach to de novo molecular design, PRO_LIGAND, has been developed that, in the environment of a large, integrated molecular design and simulation system, provides a unified framework for the generation of novel molecules which are either similar or complementary to a specified target. The approach is based on a methodology that has proved to be effective in other studies-placing molecular fragments upon target interaction sites-but incorporates many novel features such as the use of a rapid graph-theoretical algorithm for fragment placing, a generalised driver for structure generation which offers a large variety of fragment assembly strategies to the user and the pre-screening of library fragments. After a detailed description of the relevant modules of the package, PRO_LIGAND's efficacy in aiding rational drug design is demonstrated by its ability to design mimics of methotrexate and potential inhibitors for dihydrofolate reductase and HIV-1 protease.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00117275
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  • 6
    Electronic Resource
    Electronic Resource
    Active-site-directed 3D database searching: Pharmacophore extraction and validation of hits (1996)
    Springer
    Journal of computer aided molecular design 10 (1996), S. 397-416 
    Details
    ISSN: 1573-4951
    Keywords: Drug design ; Lead generation ; Thrombin inhibitors ; Scoring function
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary Two new computational tools, PRO_PHARMEX and PRO_SCOPE, for use in active-site-directed searching of 3D databases are described. PRO_PHARMEX is a flexible, graphics-based program facilitating the extraction of pharmacophores from the active site of a target macromolecule. These pharmacophores can then be used to search a variety of databases for novel lead compounds. Such searches can often generate many ‘hits’ of varying quality. To aid the user in setting priorities for purchase, synthesis or testing, PRO_SCOPE can be used to dock molecules rapidly back into the active site and to assign them a score using an empirical scoring function correlated to the free energy of binding. To illustrate how these tools can add value to existing 3D database software, their use in the design of novel thrombin inhibitors is described.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00124472
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  • 7
    Electronic Resource
    Electronic Resource
    Effects of nicotine on the acoustic startle reflex amplitude in rats (1991)
    Springer
    Psychopharmacology 104 (1991), S. 244-248 
    Details
    ISSN: 1432-2072
    Keywords: Nicotine ; Startle ; Reflex ; Sensorimotor reactivity ; Rat ; Attention
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The acoustic startle reflex was used to measure changes in sensorimotor reactivity in response to nicotine administration and cessation. Male rats received saline, 6 mg/kg/day or 12 mg/kg/day nicotine delivered subcutaneously by osmotic minipumps. The pumps delivered their contents during a 10-day period of implantation, after which time they were explanted. Animals were tested for startle reflex amplitudes using two levels of white noise bursts prior to pump implantation, on days 1 and 7 of nicotine or saline administration, and on several days following drug cessation. Nicotine produced a dose-dependent increase in startle amplitude during the period of administration that decreased during cessation. Results are interpreted in terms of nicotine's actions to enhance attentional processes.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02244186
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  • 8
    Electronic Resource
    Electronic Resource
    The tanycyte of the rat median eminence (1979)
    Springer
    Cell & tissue research 200 (1979), S. 329-334 
    Details
    ISSN: 1432-0878
    Keywords: Median eminence ; Axon terminals ; Tanycytes ; Electron microscopy ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary The present ultrastructural study proves the existence of nerve terminals closely apposed to the plasmalemmata of tanycytes in the rat median eminence. Several of these “axo-tanycytic” endings display remarkable accumulations of agranular endoplasmic reticulum in the form of pleomorphic vesicles which are closely apposed on either side of the plasma membrane of each cell compartment. Some of these vesicular profiles give the impression of structural continuity across both membrane systems. This phenomenon is discussed in the context of being a potential substratum for communication between both cell compartments.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00236425
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  • 9
    Electronic Resource
    Electronic Resource
    In vitro analysis of the cellular localization of luteinizing hormone releasing factor (LRF) in the basal hypothalamus of the rat (1974)
    Springer
    Cell & tissue research 149 (1974), S. 371-378 
    Details
    ISSN: 1432-0878
    Keywords: LRF ; Hypothalamic localization ; Rat ; Ependyma ; Glia ; Light and electron microscopic Autoradiography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary Light and electron microscopic autoradiographic analysis of the medial basal hypothalamus of rat brains incubated for 30 and 60 minutes in tritiated luteinizing releasing factor (3H-LRF) revealed selective uptake in the form of silver grains over specialized ependyma (tanycytes) and perivascular glial cells in the palisade-contact zone of the median eminence. The functional capacity of tanycytes and glia are discussed in light of these data.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00226771
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  • 10
    Electronic Resource
    Electronic Resource
    Ultrastructural changes in the median eminence of the rat following deafferentation of the basal hypothalamus (1970)
    Springer
    Cell & tissue research 105 (1970), S. 1-32 
    Details
    ISSN: 1432-0878
    Keywords: Median eminence ; Rat ; Deafferentation ; Ultrastructure
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary This report concerns a light and electron microscopic investigation of the median eminence and dorsal infundibular stem of the rat following surgical isolation (deafferentation). Using a modification of the Halász technique, the basal hypothalamus, including the arcuate nucleus and median eminence were surgically isolated from surrounding structures. Special attention was directed to the contact (external) zone of the median eminence and rostral infundibulum where tuberohypophyseal axons as well as ependymal cell processes abut upon the abluminal basement membrane of the portal perivascular space. The results of this study to date suggest that 9, 20, and 40 days following surgical isolation, there is a distinct increase in the population of tuberohypophyseal dense core vesicles. It is suggested that deafferentation abolishes inhibitory and excitatory input that serves to modify the cellular dynamics of tuberohypophyseal neurosecretory elements. Comments are also made on the presence of cistern-like structures in the lateral median eminence; the presence of vesicle-like inclusions in terminal ependymal processes is discussed in relationship to the role that ependyma may play in linking the third ventricle with the adenohypophysis.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00340562
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