Use of GABAB receptor agonists in the screening of compounds which are reflux inhibitors
AssigneeAstraZeneca AB
InventorsPaul L. R. Andrews, Anders Lehmann
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Abstract
The present invention relates to the use of GABAB receptor agonists for the inhibition of transient lower esophageal sphincter relaxations, and for the treatment of gastro-esophageal reflux disease.
Claims4
A method for screening test compounds for their potential to inhibit transient lower esophageal sphincter relaxations, comprising the steps of:
- (a) transfecting a cultured cell with a nucleotide sequence encoding a GABAB receptor, so that the GABAB receptor is expressed on the surface of the cell;
- (b) contacting a test compound with the cell;
- (c) determining whether the test compound activates the GABAB receptor;
- and
- (d) identifying a compound that activates the GABAB receptor in step (c) as one that has the potential to inhibit transient lower esophageal sphincter relaxations.
A method for screening test compounds for their potential to inhibit transient lower esophageal sphincter relaxations, comprising the steps of:
- (a) transfecting a cultured cell with a nucleotide sequence encoding a GABAB receptor selected from the group consisting of GABABR1a and GABABR1b, so that the GABAB receptor is expressed on the surface of the cell;
- (b) contacting a test compound with the cell;
- (c) determining whether the test compound activates the GABAB receptor;
- and
- (d) identifying a compound that activates the GABAB receptor in step (c) as one that has the potential to inhibit transient lower esophageal sphincter relaxations.
A method for screening test compounds for their ability to inhibit transient lower esophageal sphincter relaxations, comprising the steps of:
- (a) transfecting a cultured cell with a nucleotide sequence encoding a GABAB receptor, so that the GABAB receptor is expressed on the surface of the cell;
- (b) contacting a test compound with the cell;
- (c) determining whether the test compound activates the GABAB receptor;
- (d) administering a test compound determined to activate the GABAB receptor in step (c) to a mammal;
- and
- (e) determining whether transient lower esophageal sphincter relaxations are inhibited in the mammal as a result of the administration of the test compound in step (c).
A method for screening test compounds for their ability to inhibit transient lower esophageal sphincter relaxations, comprising the steps of:
- (a) transfecting a cultured cell with a nucleotide sequence encoding a GABAB receptor selected from the group consisting of GABABR1a and GABABR1b, so that the GABAB receptor is expressed on the surface of the cell;
- (b) contacting a test compound with the cell;
- (c) determining whether the test compound activates the GABAB receptor;
- (d) administering a test compound determined to activate the GABAB receptor in step (c) to a mammal;
- and
- (e) determining whether transient lower esophageal sphincter relaxations are inhibited in the mammal as a result of the administration of the test compound in step (c).
Dependencies are inferred from the claim text.