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AssigneeSynaptic Pharmaceutical Corporation
InventorsJonathan A. Bard, Theresa Branchek, Richard L. Weinshank
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This invention provides an isolated nucleic acid encoding a mammalian 5-HT4B receptor and an isolated nucleic acid encoding a human 5-HT4B receptor, an isolated protein which is a mammalian 5-HT4B receptor, vectors comprising an isolated nucleic acid encoding a mammalian 5-HT4B receptor, mammalian cells comprising such vectors, antibodies directed to the 5-HT4B receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian or human 5-HT4B receptor, antisense oligonucleotides complementary to any sequences of a nucleic acid which encodes a mammalian or human 5-HT4B receptor, and pharmaceutical compounds related to the human 5-HT4B receptor. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatments for alleviating abnormalities associated with a human 5-HT4B receptor.
An isolated nucleic acid molecule encoding a mammalian 5-HT4B receptor.
A isolated nucleic acid molecule which has a nucleic acid sequence which differs from the sequence of a nucleic acid molecule encoding a 5-HT4B receptor at one or more nucleotides and which does not encode a protein having 5HT4B receptor activity.
A nucleic acid probe comprising a nucleic acid molecule of at least 15 nucleotides capable of specifically hybridizing with a sequence included within the sequence of a nucleic acid molecule encoding a mammalian 5-HT4B receptor.
A nucleic acid probe comprising a nucleic acid molecule of at least 15 nucleotides capable of specifically hybridizing with a sequence included within the sequence of a nucleic acid molecule encoding a human 5-HT4B receptor.
An antisense oligonucleotide having a sequence capable of specifically binding to a mRNA molecule encoding a mammalian 5-HT4B receptor so as to prevent translation of the mRNA molecule.
An antisense oligonucleotide capable of specifically binding to a mRNA molecule encoding a human 5-HT4B receptor so as to prevent translation of the mRNA molecule.
An isolated mammalian 5-HT4B receptor protein.
An antibody directed to a mammalian 5-HT4B receptor or to a protein fragment of the mammalian 5-HT4B receptor.
An antibody directed to a human 5-HT4B receptor or to a protein fragment of the human 5-HT4B receptor.
A pharmaceutical composition comprising an amount of a substance effective to alleviate the abnormalities resulting from overexpression of a human 5-HT4B receptor and a pharmaceutically acceptable carrier.
A pharmaceutical composition comprising an amount of a substance effective to alleviate abnormalities resulting from underexpression of a human 5-HT4B receptor and a pharmaceutically acceptable carrier.
The transgenic non-human mammal of 55 wherein the transgenic non-human mammal is a mouse.
A method for determining the physiological effects of varying the levels of expression of a human 5-HT4B receptor which comprises producing a transgenic non-human mammal whose levels of expression of a human 5-HT4B receptor can be varied by use of an inducible promoter.
A method for determining the physiological effects of expressing varying levels of a human 5-HT4B receptor which comprises producing a panel of transgenic non-human mammals each expressing a different amount of a human 5-HT4B receptor.
A method for determining whether a compound not known to be capable of specifically binding to a human 5-HT4B receptor can specifically bind to the human 5-HT4B receptor, which comprises contacting a mammalian cell comprising a plasmid adapted for expression in a mammalian cell which plasmid further comprises DNA which expresses a human 5-HT4B receptor on the cell's surface with the compound under conditions permitting binding of ligands known to bind to a human 5-HT4B receptor, detecting the presence of any compound bound to the human 5-HT4B receptor, the presence of bound compound indicating that the compound is capable of specifically binding to the human 5-HT4B receptor.
A method of screening compound to identify drugs which interact with, and specifically bind to, a human 5-HT4B receptor on the surface of a cell, which comprises contacting a mammalian cell which comprises a plasmid adapted for expression in a mammalian cell which plasmid further comprises DNA which expresses a human 5-HT4B receptor on the cell's surface with a plurality of compounds, determining those compounds which bind to the human 5-HT4B receptor expressed on the cell surface of the mammalian cell, and thereby identifying compounds which interact with, and specifically bind to, the human 5-HT4B receptor.
A method for determining whether a compound not known to be capable of specifically binding to a human 5-HT4B receptor can specifically bind to a human 5-HT4B receptor, which comprises preparing a cell extract from mammalian cells, which comprise a plasmid adapted for expression in a mammal, which plasmid further comprises DNA which expresses a human 5-HT4B receptor on the cell's surface, isolating a membrane fraction from the cell extract, incubating the compound with the membrane fraction under conditions permitting binding of ligands known to bind to the human 5-HT4B receptor, detecting the presence of any bound compound, and thereby determining whether the compound is capable of specifically binding to the human 5-HT4B receptor.
A method for screening compounds to identify drugs that interact with, and specifically bind to, a human 5-HT4B receptor, which comprises preparing a cell extract from mammalian cells, which comprise a plasmid adapted for expression in a mammalian cell which plasmid further comprises DNA which expresses a human 5-HT4B receptor on the cell's surface, isolating a membrane fraction from the cell extract, incubating the membrane fraction with a plurality of compounds, determining those compounds which interact with and bind to the human 5-HT4B receptor, and thereby identifying compounds which interact with, and specifically bind to, the human 5-HT4B receptor.
A method for identify a compound which is not known to be capable of binding to the human 5-HT4B receptor activates the human 5-HT4B receptor on the surface of a mammalian cell or prevents a ligand which does so, which comprises contacting the mammalian cell which cell comprises a plasmid adapted for expression in the mammalian cell such plasmid further comprising DNA which expresses the human 5-HT4B receptor on the cell surface of the mammalian cell with the compound under conditions permitting activation of blockade of a functional response, determining whether the compound activates the human 5-HT4B receptor or prevents a ligand which does so, and thereby identifying the compound as a compound which interacts with, and activates the human 5-HT4B receptor or prevents the activation of the human 5-HT4B receptor by a ligand which does so.
A method for treating an abnormal condition related to an excess of activity of a human 5-HT4B receptor, which comprises administering a patient an amount of a pharmaceutical composition of claim 82, effective to reduce 5-HT4B activity as a result of naturally occurring substrate binding to and activating the 5-HT4B receptor.
A method for diagnosing a predisposition to a disorder associated with the expression of a human 5-HT4B receptor allele which comprises:
Dependencies are inferred from the claim text.