Library

X
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
    Electronic Resource
    Electronic Resource
    Stereoselective inhibition of monoamine oxidase and semicarbazide-sensitive amine oxidase by 4-dimethylamino-2,α-dimethylphenethylamine (FLA 336) (1984)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 327 (1984), S. 279-284 
    Details
    ISSN: 1432-1912
    Keywords: Monoamine oxidase ; Benzylamine ; Amiflamine ; Clorgyline ; Amine oxidase ; Semicarbazide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The in vitro inhibition by amiflamine [FLA 336(+)] and related compounds of the activity of rat monoamine oxidase (MAO)-A and-B, rat semicarbazide sensitive amine oxidase (SSAO) and human platelet poor plasma benzylamine oxidase was studied. Amiflamine was an MAO-A selective inhibitor, but also inhibits SSAO with both a reversible (competitive, K i=200 μmol/l) and a small time-dependent component which was irreversible in nature. The optical isomer FLA 336(−) was ten times less potent towards MAO-A. However, this compound was much more potent an inhibitor of SSAO (competitive, K i=4.6 μmol/l). The amiflamine metabolites FLA 788(+) and FLA 668(+) inhibited SSAO, but only at concentrations considerably higher than required for MAO-A inhibition. Ex vivo experiments indicated that there was no significant irreversible inhibition of rat heart and lung SSAO after both single and repeated administration of amiflamine at doses up to 20 times higher than required for inhibition of MAO-A within central serotoninergic neurones.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00506237
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 2
    Electronic Resource
    Electronic Resource
    Inhibition of monoamine oxidase and semicarbazide-sensitive amine oxidase by mexiletine and related compounds (1984)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 327 (1984), S. 273-278 
    Details
    ISSN: 1432-1912
    Keywords: Monoamine oxidase ; Benzylamine ; Mexiletine ; Clorgyline ; Amine oxidase ; Semicarbazide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The in vitro inhibition by mexiletine and related compounds of the activity of rat brain, heart and lung mono-amine oxidase-A (MAO-A), rat brain MAO-B, human platelet-poor plasma benzylamine oxidase and a clorgyline-resistant, semicarbazide-sensitive amine oxidase (SSAO) distinct from both MAO and benzylamine oxidase has been studied. The compounds were most active towards MAO-A and SSAO. IC50 values for mexiletine towards rat heart MAO-A and SSAO were 10 μmol/l and 320 μmol/l, respectively. Replacement of the para-hydrogen atom in the mexiletine aromatic ring by bromine increased potency towards both MAO-A and SSAO. Replacement of the ortho-methyl group in the mexiletine aromatic ring by hydrogen increased the potency towards SSAO alone. FLA 1042, with both these substitutions, was found to be a reversible mixed-type inhibitor of both MAO-A (K i slope 1.4 μmol/l, K i int 24 μmol/l) and of SSAO (K i slope 12 μmol/l, K i int 6 μmol/l).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00506236
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...