Výsledky vyhledávání - "K. D. Haegele"

A cardioselective, hydrophilic N,N,N-trimethylethanaminium .alpha.-tocopherol analog that reduces myocardial infarct size

Autor: E. R. Wagner, M. A. Petty, J. Dow, Joseph Wagner, J. M. Grisar, W. De Jong, K. D. Haegele, Frank Bolkenius

Publikováno v: Journal of Medicinal Chemistry. 34:257-260

The alpha-tocopherol analogue 3,4-dihydro-6-hydroxy-N,N,N,2,5,7,8- heptamethyl-2H-1-benzopyran-2-ethanaminium 4-methylbenzenesulfonate (1a, MDL 73404) and its O-acetate 1b (MDL 74270) were synthesized. Compound 1a was found to be hydrophilic (log P =

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::549304761bc0ba92021f0f638f78db93
https://doi.org/10.1021/jm00105a040

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Absorption of angiotensin II antagonists in Ussing chambers, Caco-2, perfused jejunum loop and in vivo: importance of drug ionisation in the in vitro prediction of in vivo absorption

Autor: M, Boisset, R P, Botham, K D, Haegele, B, Lenfant, J I, Pachot

Publikováno v: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 10(3)

The aims of this study were (i) to compare the absorption of three closely related inhibitors of angiotensin II, RU60018, RU60079 and HR720, in various in vitro and in vivo models, and (ii) to explain the differences in the results and to assess the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::071f9bb39aa4ef7a06f33427b0550820
https://pubmed.ncbi.nlm.nih.gov/10767599

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Pharmacokinetics and pharmacodynamics of the acetylcholinesterase inhibitor 2,2,2-trifluoro-1-(3-trimethylsilylphenyl) ethanone in dog. Potential for transdermal patch delivery

Autor: J, Dow, B D, Dulery, J M, Hornsperger, G F, Di Francesco, P, Keshary, K D, Haegele

Publikováno v: Arzneimittel-Forschung. 45(12)

MDL 73,745 (2,2,2-trifluoro-1-(3-trimethylsilylphenyl) ethanone, CAS 132236(18-1) is a novel tight-binding inhibitor of acetylcholinesterase (AChE), which is in development as a potential therapeutic compound in the symptomatic treatment of Alzheimer

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::1a052ca23850bfab5851fc5b02361185
https://pubmed.ncbi.nlm.nih.gov/8595078

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Selectivity of MDL 72,974A for MAO-B inhibition based on substrate and metabolite concentrations in plasma

Autor: N D, Huebert, V, Schwach, C, Hinze, K D, Haegele

Publikováno v: Progress in brain research. 106

Plasma concentrations of 3,4-dihydroxyphenylethylglycol (DOPEG), noradrenaline (NA), adrenaline (A), 3,4-dihydroxyphenylalanine (DOPA), 3,4-dihydroxyphenylacetic acid (DOPAC), dopamine (DA) and phenylethylamine (PEA) were analyzed in samples taken pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::7f7351df92bb6452baf373c51c6a5713
https://pubmed.ncbi.nlm.nih.gov/8584649

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Novel carbamate metabolites of mofegiline, a primary amine monoamine oxidase B inhibitor, in dogs and humans

Autor: J, Dow, F, Piriou, E, Wolf, B D, Dulery, K D, Haegele

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 22(5)

Mofegiline or MDL 72,974A ((E)-4-fluoro-beta-fluoromethylene benzene butanamine hydrochloride) is a selective enzyme-activated irreversible inhibitor of monoamine oxidase B, which is under development for use in the treatment of Parkinson's disease.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::92b50f27e2d698bc53a134ce5bce3a75
https://pubmed.ncbi.nlm.nih.gov/7835226

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Vigabatrin: Design und Entwicklung eines rational erdachten Therapeutikums

Autor: K. D. Haegele

Publikováno v: Vigabatrin ISBN: 9783540548652

Die Entdeckung des Vorkommens von γ-Aminobuttersaure (GABA) und ihrer herausragenden Funktion als inhibitorischer Neurotransmitter im Zentralnervensystem erfolgte in den 50er Jahren (Awapara et al. 1950; Roberts u. Frankel 1950; Elliot u. Florey 195

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::77efea0fe2fa47c89b95d5cd2d47b39f
https://doi.org/10.1007/978-3-642-77131-6_1

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Pharmacokinetics of and monoamine oxidase B inhibition by (E)-4-fluoro-beta-fluoromethylene benzene butanamine in man

Autor: B D, Dulery, J, Schoun, M, Zreika, J, Dow, N, Huebert, C, Hinze, K D, Haegele

Publikováno v: Arzneimittel-Forschung. 43(3)

MDL 72974A ((E)-4-fluoro-beta-fluoromethylene benzene butanamine HCl salt, CAS 120635-25-8) is a new irreversible inhibitor of the B form of monoamine oxidase (MAO-B). MDL 72974A's pharmacokinetic parameters were evaluated after administration of a s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::a616fc1df6777c2b89c05043ddb40767
https://pubmed.ncbi.nlm.nih.gov/8489556

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MDL 72,974A: a selective MAO-B inhibitor with potential for treatment of Parkinson's disease

Autor: M G, Palfreyman, I A, McDonald, M, Zreika, G, Cremer, K D, Haegele, P, Bey

Publikováno v: Journal of neural transmission. Supplementum. 40

MDL 72,974A [(E)-2-(4-fluorophenethyl)-3-fluoroallylamine, hydrochloride] was designed to be a selective, mechanism-based irreversible inhibitor of monoamine oxidase type B (MAO-B). The compound is a potent, selective MAO-B inhibitor in vitro and in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::9696a2e33fd8339b5ea890e2e4eeb813
https://pubmed.ncbi.nlm.nih.gov/8294896

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