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  • 1995-1999  (3)
  • 1985-1989
  • Hypothalamus  (2)
  • Action potential prolongation  (1)
  • 1
    ISSN: 1432-1912
    Keywords: Key words Ca2+-sensitizing action ; Stereoselectivity ; Positive inotropic effect ; Action potential prolongation ; Delayed rectifier current ; IKr block ; Guinea pig cardiac myocytes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The thiadiazinone derivative [+]-EMD 60263 ((+)-5-(1-(α-ethylimino-3,4-dimethoxybenzyl)-1,2,3,4- tetrahydroquinoline-6-yl)-6-methyl-3,6-dihydro-2H-1,3,4 -thiadiazine-2-on) is a Ca2+-sensitizing agent with only minor phosphodiesterase inhibitory activity. Our aim was to characterize the inotropic and electrophysiological effects of [+]-EMD 60263 and its enantiomer [-]-EMD 60264 in several cardiac muscle preparations. The Ca2+-sensitizing activity resided in the [+]-enantiomer only. [+]-EMD 60263 (3 µM) shifted the EC50 of Ca2+ for contractile activation of skinned fibers of pig heart from 2.41 µM to 0.73 µM, whereas [-]-EMD 60264 (30 µM) was ineffective. In Langendorff-perfused guinea pig hearts, [+]-EMD 60263 and [-]-EMD 60264 induced concentration-dependent positive and negative inotropic effects, respectively; both enantiomers reduced spontaneous heart rate but did not influence perfusion pressure. The maximum increase in force of human atrial trabeculae was 35 % of pre-drug control with [+]-EMD 60263 in comparison to 113 % with forskolin. In guinea-pig papillary muscles, [+]-EMD 60263 and [-]-EMD 60264 had opposite inotropic responses, however, both agents similarly prolonged action potential duration. Both enantiomers concentration-dependently blocked the rapidly activating component IKr of the delayed rectifier in guinea-pig myocytes. The block saturated at potentials positive to +30 mV, closely resembling the effects of the antiarrhythmic agent E-4031 which had been originally used to define IKr. It is concluded, that the positive inotropic action of [+]-EMD 60263 can be explained by prevalence of the Ca2+-sensitizing effect. The accompanying prolongation in action potential duration is caused by block of the IKr component of the delayed rectifier. While the inotropic effects are stereoselective, most of the electrophysiological actions are clearly independent of sterical configuration. The combination of Ca2+-sensitizing with class-III antiarrhythmic action may provide an interesting pharmacological profile of potential therapeutic use.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-0878
    Keywords: Osmoregulation ; fos immunocytochemistry ; Hypothalamus ; Vasotocin ; Domestic hen Gallus domesticus ; Japanese quail Coturnix japonica ; Ring dove Streptopelia risoria ; Zebra finch, Taenopygia guttata
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Domestic hens were injected intraperitoneally with hypertonic or isotonic saline and killed 0.5, 1, 2, 6, 12 and 24 h later. Japanese quail, Ring doves and Zebra finches were treated in the same way and killed 2 h later. Using fos immunocytochemistry, fos-positive cells were visualized in the preoptic-anterior hypothalamus. In all species, two hours after treatment with hypertonic but not with isotonic saline, a prominent cluster of fos-positive cells was seen close to the mid-line, dorsal to the anterior part of the third ventricle, in and around the nucleus commissurae pallii. The cell cluster was associated with the dorsal region of the organum vasculosum laminae terminalis and passed caudo-dorsally above the anterior commissure into the area of the subfornical organ, spreading diffusely into the nucleus septalis medialis and the nucleus dorsomedialis anterior thalami. The maximal expression of c-fos was seen 2 h after treatment with hypertonic saline: weak fos immunoreactive product was seen at 0.5, 1 h and 6 h but not after 12 and 24 h. In all birds, 2 h after treatment with hypertonic but not with isotonic saline, fos-positive cells were also seen in the nucleus paraventricularis and nucleus supraopticus. Double immunocytochemistry in the domestic hen with an antibody to vasotocin showed that these fos-positive cells were classical magnocellular vasotocinergic neurones. This study extends earlier studies in birds using lesioning and electrophysiological techniques to identify the precise cellular localization of the avian “osmoreceptive complex” projected onto a stereotaxic atlas.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-0878
    Keywords: Key words: Osmoregulation ; fos immunocytochemistry ; Hypothalamus ; Vasotocin ; Domestic hen Gallus domesticus ; Japanese quail Coturnix japonica ; Ring dove Streptopelia risoria ; Zebra finch ; Taenopygia guttata
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract. Domestic hens were injected intraperitoneally with hypertonic or isotonic saline and killed 0.5, 1, 2, 6, 12 and 24 h later. Japanese quail, Ring doves and Zebra finches were treated in the same way and killed 2 h later. Using fos immunocytochemistry, fos-positive cells were visualized in the preoptic-anterior hypothalamus. In all species, two hours after treatment with hypertonic but not with isotonic saline, a prominent cluster of fos-positive cells was seen close to the mid-line, dorsal to the anterior part of the third ventricle, in and around the nucleus commissurae pallii. The cell cluster was associated with the dorsal region of the organum vasculosum laminae terminalis and passed caudo-dorsally above the anterior commissure into the area of the subfornical organ, spreading diffusely into the nucleus septalis medialis and the nucleus dorsomedialis anterior thalami. The maximal expression of c-fos was seen 2 h after treatment with hypertonic saline: weak fos immunoreactive product was seen at 0.5, 1 h and 6 h but not after 12 and 24 h. In all birds, 2 h after treatment with hypertonic but not with isotonic saline, fos-positive cells were also seen in the nucleus paraventricularis and nucleus supraopticus. Double immunocytochemistry in the domestic hen with an antibody to vasotocin showed that these fos-positive cells were classical magnocellular vasotocinergic neurones. This study extends earlier studies in birds using lesioning and electrophysiological techniques to identify the precise cellular localization of the avian ”osmoreceptive complex” projected onto a stereotaxic atlas.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
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