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    New rat melatonin receptor MT1 nucleic acid, polypeptide, and antibodies, useful e.g. for drug screening and for detecting MT1 expression
    82.
    发明专利
    New rat melatonin receptor MT1 nucleic acid, polypeptide, and antibodies, useful e.g. for drug screening and for detecting MT1 expression 未知

    公开(公告)号：FR2835847A1

    公开(公告)日：2003-08-15

    申请号：FR0201559

    申请日：2002-02-08

    Applicant: SERVIER LAB

    Inventor： BARRET PERRY ,  HAZLERIGG DAVID ,  MORGAN PETER ,  AUDINOT VALERIE ,  GALIZZI JEAN PIERRE ,  RODRIGUEZ MARIANNE ,  BOUTIN JEAN ALBERT ,  DELAGRANGE PHILIPPE

    IPC: C07K14/72 ,  C12N15/12 ,  C07H21/00 ,  C07K14/705 ,  C07K16/28 ,  C12N15/63 ,  C12Q1/68 ,  G01N33/543 ,  G01N33/68

    Abstract: A nucleic acid (I) that encodes the rat MT1 melatonin receptor and comprises a 1661 bp sequence (S1) fully defined in the specification, is new. Independent claims are also included for: (1) a nucleic acid (Ia) that: (a) hybridizes to (I) under stringent conditions and encodes a polypeptide with essentially the same properties as MT1; or (b) is deduced from a 363 amino acid sequence (S2) fully defined in the specification; (2) an antisense nucleic acid (Ib) that is a single strand able to hybridize under stringent conditions with the coding strand of (I) or (Ia), inhibiting its expression; (3) a recombinant vector that contains (I) or (Ia); (4) a host cell transformed with the vector of (3); (5) a polypeptide (II) encoded by (I) or (Ia) or its fragments which: (a) has MT-1-like activity; (b) is able to stimulate G protein directly; or (c) is able to inhibit an agonist; (6) primers for amplifying sequences that encode (II); (7) hybridization probes for specific recognition of MT1-encoding sequences; (8) an antibody (Ab) directed against (II), and its fragments; (9) identifying (M1) molecules that bind to MT1 receptors; (10) identifying (M2) agonists or antagonists of MT1 receptors; (11) a DNA chip comprising (I) or (Ia); (12) a kit for detecting an anomalous structure of MT1, comprising Ab or (II); and (13) a protein chip comprising Ab, (II) or its fragments.

    86.
    发明专利
    未知

    公开(公告)号：BRPI0717528A2

    公开(公告)日：2013-10-22

    申请号：BRPI0717528

    申请日：2007-10-17

    Applicant: SERVIER LAB

    Inventor： MARCHAND PASCAL ,  BABONNEAU VINCENT ,  PIESSARD SYLVIE ,  DUFLOS MURIEL ,  BOUTIN JEAN-ALBERT ,  AUDINOT VALERIE ,  DELAGRANGE PHILIPPE ,  CAIGNARD DANIEL-HENRI

    IPC: C07D209/32 ,  A61K31/4045

    Abstract: Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably alkyl; NR 2R 35-8 membered heterocycle, preferably piperidinyl; and n : 2-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1> 2> 5>I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.

    90.
    发明专利
    未知

    公开(公告)号：NO20091779L

    公开(公告)日：2009-05-06

    申请号：NO20091779

    申请日：2009-05-06

    Applicant: SERVIER LAB

    Inventor： AUDINOT VALERIE ,  BOUTIN JEAN ALBERT ,  MARCHAND PASCAL ,  BADONNEAU VINCENT ,  PIESSARD SYLVIE ,  DUFLOS MURIEL ,  DELAGRANGE PHILIPPE ,  GAIGNARD DANIEL-HENRI

    IPC: C07D209/32

    Abstract: Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably alkyl; NR 2R 35-8 membered heterocycle, preferably piperidinyl; and n : 2-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1> 2> 5>I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.

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