Library

feed icon rss

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
  • 1
    ISSN: 1432-1041
    Keywords: Esmolol ; β1-Adrenoceptor antagonist ; tricresylphosphate ; pharmacokinetics ; effect kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The effects of esmolol at different rates of infusion (100, 250 and 500 μg·kg−1 BW·min−1) were compared with β-adrenoceptor occupancy (β1 and β2, estimated by a subtype selective radioreceptor assay) and plasma concentrations of esmolol and its acid metabolite were measured by HPLC. Up to a rate of infusion of esmolol of 500 μg·kg−1 BW·min−1 there was a maximal β1-receptor occupancy of 84.7% while β2-receptor occupancy was below the detection limit; confirming the β1 selectivity of esmolol. Exercise-induced increases in heart rate and systolic blood pressure were reduced by esmolol in a dose-dependent manner. The estimated EC50 values of rate of infusion for the reduction in heart rate and systolic blood pressure during exercise were 113 and 134 μg·kg−1 BW · min−1, respectively. Additionally, heart rate and systolic blood pressure were reduced moderately at rest. Because of the short elimination half-life of esmolol caused by the rapid hydrolysis to its acid metabolite, 45 min after end of infusion high plasma concentrations of the metabolite (maximally 80 μg·ml−1) but no esmolol were detectable. Since no in vivo effects have been observed, despite the presence of high plasma concentrations of the metabolite, the metabolite did not participate in the observed effects up to an infusion rate of esmolol of 500 μg·kg−1 BW·min−1. The plasma concentrations of antagonist detected by radioreceptor assay and plasma concentrations of esmolol detected by HPLC showed a good correlation (r=0.97). Since the cardiovascular effects, determined before and 45 min after termination of infusion of esmolol were similar, it can be concluded that the observed effects on heart rate and systolic blood pressure are exclusively mediated by esmolol.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 43 (1992), S. 157-159 
    ISSN: 1432-1041
    Keywords: Methylprednisolone aceponate ; New topical glucocorticosteroid ; efficacy ; vasoconstrictor assay ; Poison Ivy Test
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Topical glucocorticosteroids are useful in the treatment of various skin diseases. Although many corticosteroids are available today, there is still a need for highly potent compounds with minimal adverse effects. Methylprednisolone aceponate (MPA) has recently been synthesized. Its activity has been evaluated using the vasoconstrictor assay and the poison ivy test (rhus dermatitis) in 19/20 healthy volunteers of either sex. Comparable blanching was found with MPA in a cream vehicle, in an ointment and a fatty ointment. Vasoconstriction and suppression of experimentallyinduced poison ivy contact dermatitis were dose-dependent in the concentration range 0.01% to 0.5% MPA. Concentrations of MPA of at least 0.05% were significantly active. Following the highest dose, blanching was close to the maximum which can be obtained. This finding, and the improvement of rhus dermatitis, suggest that MPA belongs to the highly potent local glucocorticosteroids.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Research in experimental medicine 160 (1973), S. 307-316 
    ISSN: 1433-8580
    Keywords: Insulin secretion ; Cyclic AMP ; Analogs of cyclic AMP ; Insulinsekretion ; 3′,5′-AMP ; 3′,5′-AMP-Analoga
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Außer Adenosin-3′,5′-monophosphat (3′,5′-AMP) wurde Guanosin-3′,5′-monophosphat (3′,5′-GMP) als zweites cyclisches Nucleotid-3′,5′-monophosphat im Organismus verschiedener Tierarten nachgewiesen. An Ratten wurde untersucht, ob diese Substanz ebenso wie 3′,5′-AMP an der Steuerung der Insulinsekretion beteiligt sein könnte. Die vorliegenden Resultate sprechen nicht für diese Möglichkeit. Während bei adrenalektomierten, mit einem Glucocorticoid substituierten Ratten nach i.v. Injektion von 20 mg/kg Dibutyryl-3′,5′-AMP oder Monobutyryl-3′,5′-AMP eine deutliche Steigerung der Insulinkonzentration im Serum des Pfortaderblutes nachweisbar war, wurde ein derartiger Effekt weder unter dem Einfluß von 20 mg/kg Dibutyryl-3′,5′-GMP noch gleicher Dosen der Monobutyrylderivate von bisher in der Natur nicht nachgewiesenen Cyclophosphaten (Inosin-3′,5′-monophosphat, Uridin-3′,5′-monophosphat) beobachtet.
    Notes: Summary Besides cyclic AMP (cAMP), a second cyclic nucleotide, cyclic GMP (cGMP), has been identified in tissues of several animal species. In rats it was investigated whether this nucleotide might be involved in the regulation of insulin secretion. The results obtained do not support this possibility. Whereas i.v. injection of 20 mg/kg body weight dibutyryl-cAMP or monobutyryl-cAMP was followed by an increase of serum insulin concentration in the portal vein blood of adrenalectomized, glucocorticoid treated rats, no similar effects could be measured under the influence of same doses of either dibutyryl-cGMP, or monobutyryl derivatives of cyclic IMP and cyclic UMP the natural occurance of which has not yet been shown.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...