| 摘要 |
The present invention relates to a novel receptor in substantially pure form, to a soluble form of the receptor and it's use as a therapeutic agent, to a method of screening compounds useful in treating disorders by interacting with the receptor. A receptor in substantially pure form obtainable from rat forebrain tissue which is characterised in that: a) trans-(+)-6-acetyl-4S-(4-fluorobenzoylamino)-3,4-dihydro-2,2-dimethyl-2H-1benzopyran-3R-ol binds to it with a Kd of 40 nM for the rat forebrain tissue; b) trans-(+)-6-acetyl-4S-(4-fluorobenzoylamino)-3,4-dihydro-2,2-dimethyl-2H-1benzopyran-3R-ol binds to it with a Bmax of 220 pmol/g protein for rat forebrain tissue; c) (3S,4S)-6-acetyl-3,4-dihydro-2,2-dimethyl-4-(3-iodophenylcarbonylamino)-2H-benzo[b]pyran-3-ol binds to it with a Kd of 2nM for the rat forebrain tissue; d) (3S,4S)-6-acetyl-3,4-dihydro-2,2-dimethyl-4-(3-iodophenylcarbonylamino)-2H-benzo[b]pyran-3-ol binds to it with a Bmax of 220 pmol/g protein for rat forebrain tissue; and homologous receptors from other sources sharing at least 85 % homology with the rat forebrain tissue; wherein the receptors from rat forebrain tissue and the receptors from other sources have a molecular weight in the region of 130 Kd when analysed by SDS-gel electrophoresis.
|
