WO2001090163A3 - Use of the gabab receptor in assays to identify gamma hydroxybutyrate agonists, antagonists, and allosteric modulators of agonists - Google Patents

Use of the gabab receptor in assays to identify gamma hydroxybutyrate agonists, antagonists, and allosteric modulators of agonists Download PDF

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Publication number
WO2001090163A3
WO2001090163A3 PCT/CA2001/000770 CA0100770W WO0190163A3 WO 2001090163 A3 WO2001090163 A3 WO 2001090163A3 CA 0100770 W CA0100770 W CA 0100770W WO 0190163 A3 WO0190163 A3 WO 0190163A3
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WO
WIPO (PCT)
Prior art keywords
agonists
antagonists
assays
gabab receptor
allosteric modulators
Prior art date
Application number
PCT/CA2001/000770
Other languages
French (fr)
Other versions
WO2001090163A2 (en
Inventor
Gordon Yiu Kon Ng
Original Assignee
Merck Frosst Canada Inc
Gordon Yiu Kon Ng
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Frosst Canada Inc, Gordon Yiu Kon Ng filed Critical Merck Frosst Canada Inc
Publication of WO2001090163A2 publication Critical patent/WO2001090163A2/en
Publication of WO2001090163A3 publication Critical patent/WO2001090163A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70571—Receptors; Cell surface antigens; Cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/94—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving narcotics or drugs or pharmaceuticals, neurotransmitters or associated receptors
    • G01N33/9406—Neurotransmitters
    • G01N33/9426—GABA, i.e. gamma-amino-butyrate
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Medicinal Chemistry (AREA)
  • Hematology (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Cell Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Microbiology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Toxicology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Biotechnology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Genetics & Genomics (AREA)
  • Neurology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

An unexpected and novel mechanism of action for gamma hydroxybutyrate (GHB) has been discovered: agonist activity at the functional GABAB receptor. The discovery of this mechanism of action allows for the development of assays for the identification of modulators, such as agonists and antagonists, of GHB.
PCT/CA2001/000770 2000-05-25 2001-05-24 Use of the gabab receptor in assays to identify gamma hydroxybutyrate agonists, antagonists, and allosteric modulators of agonists WO2001090163A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20703200P 2000-05-25 2000-05-25
US60/207,032 2000-05-25

Publications (2)

Publication Number Publication Date
WO2001090163A2 WO2001090163A2 (en) 2001-11-29
WO2001090163A3 true WO2001090163A3 (en) 2002-08-01

Family

ID=22768928

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA2001/000770 WO2001090163A2 (en) 2000-05-25 2001-05-24 Use of the gabab receptor in assays to identify gamma hydroxybutyrate agonists, antagonists, and allosteric modulators of agonists

Country Status (1)

Country Link
WO (1) WO2001090163A2 (en)

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
FEIGENBAUM JEFFERY J ET AL: "Gamma hydroxybutyrate is not a GABA agonist.", PROGRESS IN NEUROBIOLOGY (OXFORD), vol. 50, no. 1, 1996, pages 1 - 7, XP002194210, ISSN: 0301-0082 *
KAUPMANN K ET AL: "EXPRESSION CLONING OF GABAB RECEPTORS UNCOVERS SIMILARITY TO METABOTROPIC GLUTAMATE RECEPTORS", NATURE, MACMILLAN JOURNALS LTD. LONDON, GB, vol. 386, March 1997 (1997-03-01), pages 239 - 246, XP002924147, ISSN: 0028-0836 *
LOBINA CARLA ET AL: "Contribution of GABAA and GABAB receptors to the discriminative stimulus produced by gamma-hydroxybutyric acid.", PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, vol. 64, no. 2, October 1999 (1999-10-01), pages 363 - 365, XP002194209, ISSN: 0091-3057 *
SNEAD O C: "RELATION OF THE 3HGAMMA-HYDROXYBUTYRIC ACID (GHB) BINDING SITE TOTHE GAMMA-AMINOBUTYRIC ACID B (GABAB) RECEPTOR IN RAT BRAIN", BIOCHEMICAL PHARMACOLOGY, PERGAMON, OXFORD, GB, vol. 52, no. 8, 1996, pages 1235 - 1243, XP000876992, ISSN: 0006-2952 *

Also Published As

Publication number Publication date
WO2001090163A2 (en) 2001-11-29

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