Non-endogenous, constitutively activated human serotonin...

Chemistry: natural resins or derivatives; peptides or proteins; – Proteins – i.e. – more than 100 amino acid residues

Reexamination Certificate

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C536S023500, C435S069100, C435S320100, C435S325000

Reexamination Certificate

active

10980560

ABSTRACT:
Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2Aand human 5-HT2Creceptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2Areceptors. Yet further disclosed is a new class of compounds which act at the 5HT2Areceptors.

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Soresnon et al., “Characterization of the 5-HT2Receptor Antagonist MDL 100907 as a Putative Atypical Antipsychotic: Behavioral, Electrophysiological and Neurochemical Studies,”J. Pharacol. Exp. Ther., 1993, 266(2), 684-691.
White, E., “Deamination of Amines. 2-Phenylethyl Benzoate Via the Nitrosoamide Decomposition,”Org. Syn. Coll., 1973, vol. 5, 336-339.
Barluenga. J. et al., “A New and Specific Method for the Monomethylation of Primary Amines,”J. Chem. Soc. Chem. Commun., 1984, 20, 1334-1335.
Batey, R.A. et al., “An Efficient New Protocol for the Formation of Unsymmetrical Tri-and Tetrasubstituted Ureas,”Tetra. Lett., 1988, 39, 6267-6270.
Bernatowicz, M. et al., “A Comparison of Acid Labile Linkage Agents for the Synthesis of Peptide C-Terminal Amides,”Tetra. Lett., 1989, 30(35), 4645-4648.
Carter, H.E. et al., “Carbobenzoxy Chloride and Derivatives,”Org. Syn. Coll., 1955, vol. 3, 167-169.
Casey, C. et al., “Constitutively Active Mutant 5HT2ASerotonin Receptors: Inverse Agonist Activity of Classical 5HT2AAntagonists,”Society for Neuroscience Abstracts, 1996, 22(3), Abstract No. 699.10.
Gutsche, C.D. et al., “2-Phenylcycloheptanone,”Org. Syn. Coll., 1963, vol. 4, 780-783.
Herrick-Davis, K. et l., “Activating Mutations of the Serotonin 5-HT2CReceptor,”J. Neurochem., 1997, 69(3), 1138-1144.
Herrick-Davis, K. et l., “Constitutively Active 5HT2C Serotonin Receptor Created by Site-Directed Mutagenesis,”Society for Neuroscience Abstracts, 1996, 22(3), Abstract No. 699.18.
Konig, W. et al., “A New Method for Synthesis of Peptides: Activation of the Carboxyl Group with Dicyclohexylcarbodiimide Using 1-Hydroxybenzotrialzoles as Additives,”Chem. Ber., 1970, 103, 788-798 (English Abstract included).
Marchini, P. et al., “Sodium Borohydride-Carboxylic Acid Systems. Useful Reagents for the Alkylation of Amines,”J. Org. Chem., 1975, 40(23), 3453-3456.
Sahgal, A. (ed.), “Practical behavioral neuroscience: problems, pitfalls and suggestions,” inBehavioral Neuroscience: A Practical Approach, IRL Press, New York, 1993, vol. 1, 1-8.
Sheehan, J.C. et al., “1-Ethyl-3-(3-Dimethylamiono)Proplycarbodiimide Hydrochloride and Methiodide,”Org. Syn. Coll., 1973, vol. 5, 555-558.
Soresnon et al., “Characterization of the 5-HT2Receptor Antagonist MDL 100907 as Putative Atypical Antipsychotic: Behavioral, Electrophysiological and Neurochemical Studies,”J. Pharacol. Exp. Ther., 1993, 266(2), 684-691.
White, E., “Deamination of Amines. 2-Phenylethyl Benzoate Via the Nitrosoamide Decomposition,”Org. Syn. Coll., 1973, vol. 5, 336-339.

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