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  • 1
    Electronic Resource
    Electronic Resource
    Inhibition of Monoamine Oxidase Selectively in Brain Monoamine Nerves Using the Bioprecursor (E-β-Fluoromethylene-m-Tyrosine (MDL 72394), a Substrate for Aromatic L-Amino Acid Decarboxylase (1985)
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 45 (1985), S. 0 
    Details
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: (E)-β-Fluoromethylene-m-tyrosine (FMMT) is a dual-enzyme-activated inhibitor of monoamine oxidase (MAO). The compound is not an inhibitor per se but is decarboxylated by aromatic L-amino acid decarboxylase (AADC) to yield a potent enzyme-activated irreversible inhibitor of MAO, (E)-β-fluoromethylene-m-tyramine, which shows some selectivity for inhibition of MAO type A. Decarboxylation of FMMT was demonstrated in vitro using hog kidney AADC and in vivo in rats by the ability of α-monofluoromethyldopa (MFMD), a potent inhibitor of AADC, to prevent MAO inhibition produced by FMMT. In isolated synaptosomes. FMMT was decarboxylated by AADC, and, furthermore, the compound was actively transported into these isolated nerve endings. An active transport into the CNS has also been demonstrated in vivo by performing competition experiments with leucine. To demonstrate that FMMT is preferentially decarboxylated within monoamine nerves of the CNS, the nigrostriatal 3,4-dihydroxyphenylethylamine (dopamine) pathway of rats was unilaterally lesioned with 6-hydroxydopamine or infused with MFMD. Under these conditions, MAO inhibition produced by orally administered FMMT in the striatum ipsilateral to the lesion or infusion was markedly attenuated. Combination of FMMT with an inhibitor of extracerebral AADC, such as carbidopa, protected peripheral organs against the MAO inhibitory effects and concomitantly enhanced MAO inhibition in the CNS. Such combinations had a greatly reduced propensity to augment the cardiovascular effects of intraduodenally administered tyramine, when compared with FMMT given alone or with clorgyline, a selective inhibitor of MAO type A. The results obtained with FMMT suggest the possibility of achieving selective inhibition of MAO within monoamine nerves of the CNS and, further, suggest that combination of FMMT with an inhibitor of extracerebral AADC will reduce the propensity of this inhibitor to produce adverse interactions with tyramine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1471-4159.1985.tb10543.x
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  • 2
    Electronic Resource
    Electronic Resource
    (E)-2-(3,4-dimethoxyphenyl)-3-fluoroallylamine: a selective, enzyme-activated inhibitor of type B monoamine oxidase (1984)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 27 (1984), S. 9-10 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00367a002
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Effects on migraine headache of MDL 72,222, an antagonist at neuronal 5-HT receptors. Double-blind, placebo-controlled study (1985)
    USA/Oxford, UK : Blackwell Science Ltd
    Cephalalgia 5 (1985), S. 0 
    Details
    ISSN: 1468-2982
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: -3a-yl 3,5-dichlorobenzoate), a novel agent with antagonist activity at neuronal 5-HT receptors, was tested as an acute treatment for migraine pain under double-blind, placebo-controlled conditions. Forty-seven patients with common (n = 29) or classical (n = 8) migraine or mixed type with or without a psychogenic component (n = 10) received 20–40 mg MDL 72,222 (n = 24) or placebo (n = 23) intravenously during the headache phase of a migraine attack. MDL 72,222 was consistently superior to placebo in rapidly alleviating the migraine pain. The treatment was remarkably well tolerated. The results are consistent with the hypothesis that the pain of migraine is related to activation of neuronal 5-HT receptors and suggest that compounds such as MDL 72,222, which block neuronal 5-HT receptors, could be useful new therapeutic agents for the management of migraine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1468-2982.1985.0502079.x
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  • 4
    Electronic Resource
    Electronic Resource
    Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor (1988)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 31 (1988), S. 1087-1093 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00401a007
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    Paper (German National Licenses)
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  • 5
    Electronic Resource
    Electronic Resource
    The functional consequences of inhibition of monoamine oxidase type B: comparison of the pharmacological properties ofl-deprenyl and MDL 72145 (1985)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 331 (1985), S. 186-193 
    Details
    ISSN: 1432-1912
    Keywords: Monoamine oxidase B inhibition ; l-Deprenyl ; MDL 72145 ; Pharmacological effects ; Amphetamine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 1. The pharmacological properties of two selective inhibitors of monoamine oxidase (MAO) type B,l-deprenyl and MDL 72145 [(E)-2-(3,4-dimethyoxyphenyl)-3-fluoroallylamine, HCl], have been investigated in rats and mice in relation to their effects on MAO. 2. Selective inhibition of MAO B achieved following 18 h pretreatment withl-deprenyl and/or MDL 72145 did not per se lead to prominent pharmacological activity; no effects were seen in the mouse “Behavioural Despair” test, hypothermia induced by reserpine in mice was neither prevented nor reversed and there was no change in the cardiovascular responsiveness of the pithed rat to tyramine, noradrenaline or stimulation of the spinal sympathetic outflow. 3. l-Deprenyl differed from MDL 72145 in that short term treatment with this drug caused positive effects in the “Behavioural Despair” test, reversal of reserpine hypothermia, indirect sympathomimetic stimulation of blood pressure and heart rate in the pithed rat and ipsilateral rotation in rats with unilateral nigro-striatal lesions. Qualitatively similar effects were seen with dexamphetamine. 4. The marked difference between the pharmacological effects of MDL 72145 andl-deprenyl despite equivalent inhibition of MAO B suggests that many of the pharmacological actions ofl-deprenyl result from its amphetaminelike sympathomimetic properties. MDL 72145 can, therefore, be considered a more reliable tool with which to explore the functional importance of MAO B inhibition in experimental animals and man.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00634237
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  • 6
    Electronic Resource
    Electronic Resource
    The cardiovascular effects of selective adenosine A1 and A2 receptor agonists in the pithed rat: no role for glibenclamide-sensitive potassium channels (1993)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 347 (1993), S. 192-196 
    Details
    ISSN: 1432-1912
    Keywords: Adenosine receptors ; Potassium channels ; CPA ; CGS 21680 ; Glibenclamide ; Rat cardiovascular system
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The cardiovascular effects of N6-cyclopentyladenosine (CPA), a selective adenosine A1 receptor agonist and 2-[p-carboxyethyl)phenylethylamino]-5′-N-ethylcarboxamidoadenosine (CGS 21680), a selective A2 receptor agonist have been investigated in the pithed rat with blood pressure raised to normal levels with angiotensin II. Cumulative intravenous administration of CPA, 0.3–10 μg/kg, induced dose-related falls in blood pressure and heart rate; over the same dose range CGS 21680 induced hypotension but no bradycardia. Pretreatment with a maximally effective dose of the A1/A2 receptor antagonist 8-(p-sulphophenyl) theophylline (8-SPT) blocked the bradycardiac effects of CPA (92-fold) more effectively than its hypotensive activity (5.1-fold); the vasodepressor effects of CGS 21680 were blocked 19-fold by 8-SPT. Glibenclamide, a blocker of ATP-sensitive potassium (K infATP sup+ ) channels, administered intravenously at 20 mg/kg markedly attenuated the vasodepressor effects of the potassium channel opener, (−)-(3S,4R)-3,4-dihydro-3-hydroxy-2,2-dimethyl-4-(3-oxo-cyclopent-1-enyloxy)2-H-1-benzopyran-6-carbonitrile (SDZ PCO 400). In contrast, neither the hypotensive nor the bradycardic effects of CPA nor the fall in blood pressure following CGS 21680 was significantly affected by pretreatment with glibenclamide. These results indicate that a significant component of the blood pressure fall induced by CPA and CGS 21680 in the pithed rat with blood pressure supported by angiotensin II occurs by a mechanism which is insensitive to 8-SPT and unlikely, therefore, to be mediated by A1 or A2 receptors. Moreover, in contrast to the prevailing literature, the cardiovascular effects arising from adenosine receptor activation in this model are not mediated by glibenclamide-sensitive, K infATP sup+ channels.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00169266
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  • 7
    Electronic Resource
    Electronic Resource
    5-Hydroxytryptamine (5-HT) and the initiation of migraine: new perspectives (1994)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 350 (1994), S. 225-229 
    Details
    ISSN: 1432-1912
    Keywords: Migraine ; Nitric oxide ; Endothelium ; 5-HT2C Receptors ; 5-HT2B Receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The hypothesis that 5-hydroxytryptamine (5-HT) acting through 5-HT2c receptors is a key factor in the initiation of migraine has been re-evaluated in the light of recent basic and clinical scientific developments. The key findings are that nitric oxide is an important trigger for migraine, that 5-HT2B/5-HT2C receptors are present on endothelial cells and trigger nitric oxide release when activated and that supersensitivity of the 5-HT2B/5-HT2C receptor is a neurochemical feature predisposing to headache. Taken together the data bring new perspectives to the role of 5-HT acting through 5-HT2C (or closely similar) receptors in the initiation of migraine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00175026
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  • 8
    Electronic Resource
    Electronic Resource
    5-Hydroxytryptamine (5-HT) and the initiation of migraine: new perspectives (1994)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 350 (1994), S. 225-229 
    Details
    ISSN: 1432-1912
    Keywords: Key words: Migraine – Nitric oxide – Endothelium – 5-HT2C Receptors – 5-HT2B Receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract. The hypothesis that 5-hydroxytryptamine (5-HT) acting through 5-HT2C receptors is a key factor in the initiation of migraine has been re-evaluated in the light of recent basic and clinical scientific developments. The key findings are that nitric oxide is an important trigger for migraine, that 5-HT2B/5-HT2C receptors are present on endothelial cells and trigger nitric oxide release when activated and that supersensitivity of the 5-HT2B/5-HT2C receptor is a neurochemical feature predisposing to headache. Taken together the data bring new perspectives to the role of 5-HT acting through 5-HT2C (or closely similar) receptors in the initiation of migraine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00175026
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