- Long term storage inducer
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PROBLEM TO BE SOLVED: To provide a long-term memory inducing agent.SOLUTION: A long-term memory inducing agent comprises a compound represented by the formula I, pharmaceutically acceptable salt thereof, or solvate thereof.SELECTED DRAWING: None
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- Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine
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For further development of successors of Agomelatine through modulation of its pharmacokinetic properties, we report herein the design, synthesis and pharmacological results of a new family of melatonin receptor ligands. Issued from the introduction of quinazoline and phthalazine scaffolds carrying an ethyl amide lateral chain and a methoxy group as bioisosteric ligands analogues of previously developed Agomelatine. The biological activity of the prepared analogues was compared with that of Agomelatine. Quinazoline and phthalazine rings proved to be a versatile scaffold for easy feasible MT1 and MT2 ligands. Potent agonists with sub-micromolar binding affinity were obtained. However, the presence of two nitrogen atoms resulted in compounds with lower affinity for both MT1 and MT2, in comparison with the parent compound, balanced by the exhibition of good pharmacokinetic properties.
- Bolteau, Rapha?l,Descamps, Florian,Ettaoussi, Mohamed,Caignard, Daniel H.,Delagrange, Philippe,Melnyk, Patricia,Yous, Sa?d
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- LONG-TERM MEMORY INDUCING AGENT
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[Problem] To provide a method for inducing a long-term memory in a subject need thereof. [Solution to problem] A method for inducing a long-term memory, comprising a step of administering a compound represented by Formula I below, a pharmaceutically accep
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- Online H/D exchange liquid chromatography as a support for the mass spectrometric identification of the oxidation products of melatonin
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The hydrogen-deuterium exchange of protonated melatonin and its in vitro oxidation end-products have been examined by liquid chromatography coupled with ion-trap mass spectrometry. Specific H/D scrambling of protons in the C2 and C4 positions of the indol
- Collin, Fabrice,Bonnefont-Rousselot, Dominique,Yous, Said,Marchetti, Catherine,Jore, Daniel,Gardes-Albert, Monique
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experimental part
p. 318 - 329
(2010/06/13)
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- Kynurenamines as neural nitric oxide synthase inhibitors
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To find new compounds with potential neuroprotective activity, we have designed, synthesized, and characterized a series of neural nitric oxide synthase (nNOS) inhibitors with a kynurenamine structure. Among them, N-[3-(2-amino-5-methoxyphenyl)-3-oxopropy
- Entrena, Antonio,Camacho, M. Encarnación,Carrión, M. Dora,López-Cara, Luisa C.,Velasco, Guillermo,Léon, Josefa,Escames, Germaine,Acu?a-Castroviejo, Dario,Tapias, Víctor,Gallo, Miguel A.,Vivó, Antonio,Espinosa, Antonio
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p. 8174 - 8181
(2007/10/03)
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- Radioimmunoassay of N-acetyl-N-formyl-5-methoxykynuramine (AFMK): A melatonin oxidative metabolite
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N-acetyl-N-formyl-5-methoxykynuramine (AFMK) is a melatonin metabolite identified in rat brain by Hirata et al. (The Journal of Biological Chemistry 249 (1974) 1311). Since no assay has been described for its routine measurement, we have developed and val
- Harthe, Catherine,Claudy, Daniele,Dechaud, Henri,Vivien-Roels, Berthe,Pevet, Paul,Claustrat, Bruno
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p. 1587 - 1597
(2008/01/27)
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- The synthesis of the kynurenamines K1 and K2, metabolites of melatonin
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An efficient synthesis of the kynurenamines K1 and K2, the major brain and antioxidant metabolites of melatonin 1 is described. Regioselective lithiation of tert-butyl(4-methoxyphenyl) carbamate and iodination provided the (2-iodoary
- Amiet, Gary,Hügel, Helmut M.,Nurlawis, Faizul
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p. 495 - 497
(2007/10/03)
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- In vitro and in vitro formation of two new metabolites of melatonin
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A partially purified enzyme from rabbit brain catalyzed the oxygenative cleavage of the pyrrole moiety of melatonin yielding N(γ) acetyl N2 formyl 5 methoxykynurenamine, which was further degraded to N(γ) acetyl 5 methoxykynurenamine by the action of formamidase. Authentic samples of these two metabolites were synthesized by ozonolysis of melatonin and were shown to be indistinguishable from the enzymic products. When [14C] melatonin was injected intracisternally, the major metabolite in the rat brain was shown to be N(γ) acetyl 5 methoxykynurenamine. The results indicate that these two new metabolites are involved in the major metabolic pathway of melatonin in the central nervous system.
- Hirata,Hayaishi,Tokuyama,Senoh
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p. 1311 - 1313
(2007/10/16)
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